Any feedback?
Information on EC 2.5.1.21 - squalene synthase
for references in articles please use BRENDA:EC2.5.1.21Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
2.5.1.21 squalene synthaseIUBMB Comments
This microsomal enzyme catalyses the first committed step in the biosynthesis of sterols. The enzyme from yeast requires either Mg2+ or Mn2+ for activity. In the absence of NAD(P)H, presqualene diphosphate (PSPP) is accumulated. When NAD(P)H is present, presqualene diphosphate does not dissociate from the enzyme during the synthesis of squalene from farnesyl diphosphate (FPP) . High concentrations of FPP inhibit the production of squalene but not of PSPP .
Specify your search results
Word Map
- 2.5.1.21
-
farnesylation
- cholesterol
-
prenylation
- sterol
- ftase
- mevalonate
-
geranylgeranylation
-
isoprenoids
- leukemia
-
geranylgeranyltransferase
- pyrophosphate
- tipifarnib
- hmg-coa
- statin
- h-ras
-
peptidomimetic
-
epoxidase
- prenyltransferase
- dolichols
- rhob
-
isoprenylation
-
triterpene
- farnesol
-
3-hydroxy-3-methylglutaryl
- lamins
- ergosterol
-
cholesterol-lowering
- hmgcr
-
prelamin
-
p21ras
- lovastatin
-
hutchinson-gilford
- lanosterol
- manumycin
-
triterpenoids
- synthesis
-
progerin
-
farnesylpyrophosphate
- cis-prenyltransferase
- drug development
- oxidosqualene
-
ras-transformed
- medicine
-
ras-dependent
-
nonsterols
-
ras-mediated
-
withanolides
- srebp-2
-
ganoderic
- agriculture
- geranylgeraniol
- industry
- cycloartenol
-
non-thiol
- 2,3-oxidosqualene
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
Reaction Schemes
Synonyms
farnesyltransferase, squalene synthase, sqs, fdft1, squalene synthetase, farnesyl-diphosphate farnesyltransferase, sgsqs, ssase, sqase, tksqs1, 
more
topPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
farnesyl-diphosphate farnesyltransferase
-
-
-
-
farnesyldiphosphate:farnesyldiphosphate farnesyltransferase
-
-
-
-
farnesyltransferase
-
-
-
-
presqualene synthase
-
-
-
-
presqualene-diphosphate synthase
-
-
-
-
squalene synthase
-
-
-
-
squalene synthetase
-
-
-
-
synthase, squalene
-
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
alkenyl group transfer
-
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PATHWAY SOURCE
PATHWAYS
BRENDA
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SYSTEMATIC NAME
IUBMB Comments
(2E,6E)-farnesyl-diphosphate:(2E,6E)-farnesyl-diphosphate farnesyltransferase
This microsomal enzyme catalyses the first committed step in the biosynthesis of sterols. The enzyme from yeast requires either Mg2+ or Mn2+ for activity. In the absence of NAD(P)H, presqualene diphosphate (PSPP) is accumulated. When NAD(P)H is present, presqualene diphosphate does not dissociate from the enzyme during the synthesis of squalene from farnesyl diphosphate (FPP) [8]. High concentrations of FPP inhibit the production of squalene but not of PSPP [8].
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CAS REGISTRY NUMBER
COMMENTARY
9077-14-9
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
overexpression of the enzyme's C-terminal domain containing a hinge domain from fungi, not from animals or plants, leads to growth inhibition of wild-type yeast
-
additional information
-
overexpression of the enzyme's C-terminal domain containing a hinge domain from fungi, not from animals or plants, leads to growth inhibition of wild-type yeast
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Acidosis
[Inhibitory action of natural compounds of microbial origin on cholesterol metabolism]
Acquired Immunodeficiency Syndrome
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.
Acute Lung Injury
Streptococcal M1 protein triggers farnesyltransferase-dependent formation of CXC chemokines in alveolar macrophages and neutrophil infiltration in the lung.
Adenocarcinoma
A novel amplicon at 8p22-23 results in overexpression of cathepsin B in esophageal adenocarcinoma.
Adenocarcinoma
Enhanced Antiproliferative and Apoptotic Response of HT-29 Adenocarcinoma Cells to Combination of Photoactivated Hypericin and Farnesyltransferase Inhibitor Manumycin A.
Adenocarcinoma
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Adenocarcinoma
Phase II and pharmacodynamic study of the farnesyltransferase inhibitor R115777 as initial therapy in patients with metastatic pancreatic adenocarcinoma.
Adenocarcinoma
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Adenoma
Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone.
Adrenocortical Carcinoma
Identification of novel lipid metabolic biomarkers associated with poor adrenocortical carcinoma prognosis using integrated bioinformatics.
Alcohol-Related Disorders
The FIP study: a randomised, controlled trial of screening and recognition of psychiatric disorders.
Alzheimer Disease
Farnesyltransferase haplodeficiency reduces neuropathology and rescues cognitive function in a mouse model of Alzheimer disease.
Arrhythmias, Cardiac
Effects of sasanquasaponin on ischemia and reperfusion injury in mouse hearts.
Arrhythmogenic Right Ventricular Dysplasia
Chemical Genetics Reveals a Role of Squalene Synthase in TGF? Signaling and Cardiomyogenesis.
Arthritis
Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation.
Arthritis, Experimental
Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation.
Arthritis, Rheumatoid
Dichotomous versus semi-quantitative scoring of ultrasound joint inflammation in rheumatoid arthritis using novel individualized joint selection methods.
Asthma
Farnesyltransferase Inhibition Exacerbates Eosinophilic Inflammation and Airway Hyperreactivity in Mice with Experimental Asthma: The Complex Roles of Ras GTPase and Farnesylpyrophosphate in Type 2 Allergic Inflammation.
Asthma
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Astrocytoma
Establishment and characterization of a novel malignant astrocytoma cell line derived from a tumor removed in a patient with neurofibromatosis type 1.
Astrocytoma
In vitro and in vivo growth inhibition of human malignant astrocytoma cells by the farnesyltransferase inhibitor B1620.
Astrocytoma
The farnesyltransferase inhibitor L-744,832 inhibits the growth of astrocytomas through a combination of antiproliferative, antiangiogenic, and proapoptotic activities.
Atherosclerosis
Design of more potent squalene synthase inhibitors with multiple activities.
Atherosclerosis
Design of Novel Potent Antihyperlipidemic Agents with Antioxidant/Anti-inflammatory Properties: Exploiting Phenothiazine's Strong Antioxidant Activity.
Atherosclerosis
Developing potential agents against atherosclerosis: Design, synthesis and pharmacological evaluation of novel dual inhibitors of oxidative stress and Squalene Synthase activity.
Atherosclerosis
EP2306 [2-(4-biphenyl)-4-methyl-octahydro-1,4-benzoxazin-2-ol, hydrobromide], a novel squalene synthase inhibitor, reduces atherosclerosis in the cholesterol-fed rabbit.
Atherosclerosis
Farnesyltransferase inhibitor, manumycin a, prevents atherosclerosis development and reduces oxidative stress in apolipoprotein E-deficient mice.
Brain Neoplasms
Farnesyltransferase and geranylgeranyltransferase I inhibitors upregulate RhoB expression by HDAC1 dissociation, HAT association and histone acetylation of the RhoB promoter.
Brain Neoplasms
Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.
Breast Neoplasms
A phase I trial and pharmacokinetic study of tipifarnib, a farnesyltransferase inhibitor, and tamoxifen in metastatic breast cancer.
Breast Neoplasms
A phase II trial of capecitabine in combination with the farnesyltransferase inhibitor tipifarnib in patients with anthracycline-treated and taxane-resistant metastatic breast cancer: an Eastern Cooperative Oncology Group Study (E1103).
Breast Neoplasms
A phase II, randomized, blinded study of the farnesyltransferase inhibitor tipifarnib combined with letrozole in the treatment of advanced breast cancer after antiestrogen therapy.
Breast Neoplasms
Aromatase inhibitors: combinations with fulvestrant or signal transduction inhibitors as a strategy to overcome endocrine resistance.
Breast Neoplasms
Biomarkers of anticancer activity of R115777 (Tipifarnib, Zarnestra) in human breast cancer models in vitro.
Breast Neoplasms
Combination of farnesyltransferase and Akt inhibitors is synergistic in breast cancer cells and causes significant breast tumor regression in ErbB2 transgenic mice.
Breast Neoplasms
Enhancement of the antitumor activity of tamoxifen and anastrozole by the farnesyltransferase inhibitor lonafarnib (SCH66336).
Breast Neoplasms
Experimental, Clinical and Morphological Analysis of H-Ras Oncoproteins for Locally Advanced Breast Cancer.
Breast Neoplasms
Farnesyltransferase inhibitors and their potential in the treatment of breast carcinoma.
Breast Neoplasms
Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivo.
Breast Neoplasms
Higenamine enhances the antitumor effects of cucurbitacin B in breast cancer by inhibiting the interaction of AKT and CDK2.
Breast Neoplasms
Inhibition of transendothelial migration and invasion of human breast cancer cells by preventing geranylgeranylation of Rho.
Breast Neoplasms
Mini review: The FDA-approved prescription drugs that target the MAPK signaling pathway in women with breast cancer.
Breast Neoplasms
Phase II trial of the farnesyltransferase inhibitor tipifarnib plus fulvestrant in hormone receptor-positive metastatic breast cancer: New York Cancer Consortium Trial P6205.
Breast Neoplasms
Potentiation of nitric oxide-induced apoptosis of MDA-MB-468 cells by farnesyltransferase inhibitor: implications in breast cancer.
Breast Neoplasms
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Breast Neoplasms
Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.
Breast Neoplasms
Targeting downstream effectors of epidermal growth factor receptor/HER2 in breast cancer with either farnesyltransferase inhibitors or mTOR antagonists.
Breast Neoplasms
The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.
Breast Neoplasms
The use of molecular markers in farnesyltransferase inhibitor (FTI) therapy of breast cancer.
Breast Neoplasms
Tipifarnib plus tamoxifen in tamoxifen-resistant metastatic breast cancer: a negative phase II and screening of potential therapeutic markers by proteomic analysis.
Breast Neoplasms
vHTS and 3D-QSAR for the Identification of Novel Phyto-inhibitors of Farnesyltransferase: Validation of Ascorbic Acid inhibition of Farnesyltransferase in an Animal Model of Breast Cancer.
Bronchiectasis
Quantitative Computed Tomography Metrics From the Transplanted Lung can Predict Forced Expiratory Volume in the First Second After Lung Transplantation.
Burkitt Lymphoma
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
Carcinogenesis
Functional polymorphisms in inbred rat strains and their allele frequencies in commercially available outbred stocks.
Carcinogenesis
Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection.
Carcinogenesis
ras protein p21 processing enzyme farnesyltransferase in chemical carcinogen-induced murine skin tumors.
Carcinogenesis
Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors.
Carcinoid Tumor
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma
A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.
Carcinoma
A New Survival Model Based on Cholesterol Biosynthesis-Related Genes for Prognostic Prediction in Clear Cell Renal Cell Carcinoma.
Carcinoma
A Phase II Trial of Tipifarnib for Patients with Previously Treated, Metastatic Urothelial Carcinoma Harboring HRAS Mutations.
Carcinoma
Absence of the CAAX endoprotease Rce1: effects on cell growth and transformation.
Carcinoma
Atorvastatin inhibits pancreatic carcinogenesis and increases survival in LSL-Kras(G12D) -LSL-Trp53(R172H) -Pdx1-Cre mice.
Carcinoma
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Carcinoma
Expression of the farnesyltransferase beta-subunit gene in human ovarian carcinoma: correlation to K-ras mutation.
Carcinoma
Farnesyltransferase activity and mRNA expression in human skin basal cell carcinomas.
Carcinoma
Farnesyltransferase inhibitor SCH-66336 downregulates secretion of matrix proteinases and inhibits carcinoma cell migration.
Carcinoma
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Carcinoma
Farnesyltransferase inhibitors--a novel approach in the treatment of advanced pancreatic carcinomas.
Carcinoma
Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice.
Carcinoma
Lipid synthesis and processing proteins ABHD5, PGRMC1 and squalene synthase can serve as novel immunohistochemical markers for sebaceous neoplasms and differentiate sebaceous carcinoma from sebaceoma and basal cell carcinoma with clear cell features.
Carcinoma
Multiple squamous cell carcinomas of the skin after therapy with sorafenib combined with tipifarnib.
Carcinoma
Pancreatic cancer cell radiation survival and prenyltransferase inhibition: the role of K-Ras.
Carcinoma
Phase II study of the farnesyltransferase inhibitor lonafarnib with paclitaxel in patients with taxane-refractory/resistant nonsmall cell lung carcinoma.
Carcinoma
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
Carcinoma
Suppression of rho B expression in invasive carcinoma from head and neck cancer patients.
Carcinoma
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma
[Effects of farnesyltransferase silencing on the migration and invasion of tongue squamous cell carcinoma].
Carcinoma, Basal Cell
Farnesyltransferase activity and mRNA expression in human skin basal cell carcinomas.
Carcinoma, Basal Cell
Lipid synthesis and processing proteins ABHD5, PGRMC1 and squalene synthase can serve as novel immunohistochemical markers for sebaceous neoplasms and differentiate sebaceous carcinoma from sebaceoma and basal cell carcinoma with clear cell features.
Carcinoma, Hepatocellular
A Link between cholesterol levels and phenobarbital induction of cytochromes P450.
Carcinoma, Hepatocellular
ATF6? Stimulates Cholesterogenic Gene Expression and de Novo Cholesterol Synthesis.
Carcinoma, Hepatocellular
Pravastatin inhibited the cholesterol synthesis in human hepatoma cell line Hep G2 less than simvastatin and lovastatin, which is reflected in the upregulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase and squalene synthase.
Carcinoma, Hepatocellular
Rational Discovery of Novel Squalene Synthase Inhibitors through Pharmacophore Modelling.
Carcinoma, Hepatocellular
Regulation of squalene synthetase in human hepatoma cell line Hep G2 by sterols, and not by mevalonate-derived non-sterols.
Carcinoma, Hepatocellular
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Carcinoma, Hepatocellular
Subcellular localization of squalene synthase in human hepatoma cell line Hep G2.
Carcinoma, Hepatocellular
Syntheses and biological evaluation of novel quinuclidine derivatives as squalene synthase inhibitors.
Carcinoma, Hepatocellular
Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: enzyme inhibition and effects on plasma lipid levels.
Carcinoma, Hepatocellular
Targeting Cellular Squalene Synthase, an Enzyme Essential for Cholesterol Biosynthesis, Is a Potential Antiviral Strategy against Hepatitis C Virus.
Carcinoma, Hepatocellular
[Correlation between inhibitory effect of Manumycin on human hepatoma cancer cell HepG2 and Ras signal transduction pathway]
Carcinoma, Large Cell
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Carcinoma, Large Cell
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma, Neuroendocrine
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma, Non-Small-Cell Lung
In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines.
Carcinoma, Non-Small-Cell Lung
Ras homologue enriched in brain is a critical target of farnesyltransferase inhibitors in non-small cell lung cancer cells.
Carcinoma, Non-Small-Cell Lung
Relationship of SNP rs2645429 in Farnesyl-Diphosphate Farnesyltransferase 1 Gene Promoter with Susceptibility to Lung Cancer.
Carcinoma, Ovarian Epithelial
Ubiquitin specific peptidase 32 acts as an oncogene in epithelial ovarian cancer by deubiquitylating farnesyl-diphosphate farnesyltransferase 1.
Carcinoma, Renal Cell
BAI, a novel Cdk inhibitor, enhances farnesyltransferase inhibitor LB42708-mediated apoptosis in renal carcinoma cells through the downregulation of Bcl-2 and c-FLIP (L).
Carcinoma, Renal Cell
Multiple squamous cell carcinomas of the skin after therapy with sorafenib combined with tipifarnib.
Carcinoma, Small Cell
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Carcinoma, Squamous Cell
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Carcinoma, Squamous Cell
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma, Squamous Cell
[Effects of farnesyltransferase silencing on the migration and invasion of tongue squamous cell carcinoma].
Cardiomyopathies
Chemical Genetics Reveals a Role of Squalene Synthase in TGF? Signaling and Cardiomyogenesis.
Cardiovascular Diseases
A farnesyltransferase inhibitor prevents both the onset and late progression of cardiovascular disease in a progeria mouse model.
Cardiovascular Diseases
New applications of squalene synthase inhibitors: Membrane cholesterol as a therapeutic target.
Cardiovascular Diseases
Squalene synthase: a critical enzyme in the cholesterol biosynthesis pathway.
Cardiovascular Diseases
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.
Cardiovascular Diseases
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Cataract
Identification of Differential Gene Expression Pattern in Lens Epithelial Cells Derived from Cataractous and Noncataractous Lenses of Shumiya Cataract Rat.
Cataract
Lanosterol synthase mutations cause cholesterol deficiency-associated cataracts in the Shumiya cataract rat.
Cataract
Lens cholesterol biosynthesis inhibition: A common mechanism of cataract formation in laboratory animals by pharmaceutical products.
Central Nervous System Neoplasms
Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.
Chagas Disease
Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
Chagas Disease
In vitro and in vivo activities of E5700 and ER-119884, two novel orally active squalene synthase inhibitors, against Trypanosoma cruzi.
Chondrodysplasia Punctata
Genetic disorders of cholesterol biosynthesis in mice and humans.
Colonic Neoplasms
Cellular effects of a new farnesyltransferase inhibitor, RPR-115135, in a human isogenic colon cancer cell line model system HCT-116.
Colonic Neoplasms
In vitro and in vivo evaluation of two rational-designed nonpeptidic farnesyltransferase inhibitors on HT29 human colon cancer cell lines.
Colonic Neoplasms
Induction of micronuclei by a new non-peptidic mimetic farnesyltransferase inhibitor RPR-115135: role of gene mutations.
Colonic Neoplasms
Liver metastasis models of colon cancer for evaluation of drug efficacy using NOD/Shi-scid IL2Rgammanull (NOG) mice.
Colonic Neoplasms
Nonpeptidomimetic farnesyltransferase inhibitor RPR-115135 increases cytotoxicity of 5-fluorouracil: role of p53.
Colonic Neoplasms
RPR-115135, a farnesyltransferase inhibitor, increases 5-FU- cytotoxicity in ten human colon cancer cell lines: role of p53.
Colonic Neoplasms
RPR-115135, a new non peptidomimetic farnesyltransferase inhibitor, induces G0/G1 arrest only in serum starved cells.
Colorectal Neoplasms
Increased farnesyltransferase activity in human colorectal cancer: relationship with clinicopathological features and K-ras mutation.
Colorectal Neoplasms
Inhibition of the mitogen-activated protein kinase pathway results in the down-regulation of P-glycoprotein.
Colorectal Neoplasms
Oncogenic K-Ras signals through epidermal growth factor receptor and wild-type H-Ras to promote radiation survival in pancreatic and colorectal carcinoma cells.
Coronary Artery Disease
Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions.
Craniosynostoses
Additional squamosal suture synostosis and segmented intracranial volume in patients with non-syndromic sagittal synostosis.
Dehydration
CRISPR/Cas9-targeted mutagenesis of OsERA1 confers enhanced responses to abscisic acid and drought stress and increased primary root growth under nonstressed conditions in rice.
Diphtheria
Update in childhood acute myeloid leukemia: recent developments in the molecular basis of disease and novel therapies.
Disorders of Excessive Somnolence
Relationship between overweight, obesity and sleep disorders in adolescents from selected cities of Upper Silesia, Poland.
Dyslipidemias
Design of Novel Potent Antihyperlipidemic Agents with Antioxidant/Anti-inflammatory Properties: Exploiting Phenothiazine's Strong Antioxidant Activity.
Dyslipidemias
Squalene synthase inhibition: a novel target for the management of dyslipidemia.
Endotoxemia
Farnesyltransferase inhibitor improved survival following endotoxin challenge in mice.
Erythema
Exclusion of CTSB and FDFT1 as positional and functional candidate genes for keratolytic winter erythema (KWE).
Exanthema
L-NAME has opposite effects on the productions of S-adenosylhomocysteine and S-adenosylmethionine in V12-H-Ras and M-CR3B-Ras pheochromocytoma cells.
Glioblastoma
?v?3 Integrin and Fibroblast growth factor receptor 1 (FGFR1): Prognostic factors in a phase I-II clinical trial associating continuous administration of Tipifarnib with radiotherapy for patients with newly diagnosed glioblastoma.
Glioblastoma
HDJ-2 as a target for radiosensitization of glioblastoma multiforme cells by the farnesyltransferase inhibitor R115777 and the role of the p53/p21 pathway.
Glioblastoma
Inhibition of cell growth in human glioblastoma cell lines by farnesyltransferase inhibitor SCH66336.
Glioblastoma
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells.
Glioblastoma
The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.
Glioma
Farnesyltransferase Inhibitor Manumycin Targets IL1?-Ras-HIF-1? Axis in Tumor Cells of Diverse Origin.
Glioma
Farnesyltransferase inhibitor, R115777, reverses the resistance of human glioma cell lines to ionizing radiation.
Glioma
Inhibition of Ras and related guanosine triphosphate-dependent proteins as a therapeutic strategy for blocking malignant glioma growth: II--preclinical studies in a nude mouse model.
Glioma
Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas.
Glioma
Manumycin inhibits STAT3, telomerase activity and growth of glioma cells by elevating intracellular reactive oxygen species generation.
Glioma
Phase 1/1b study of lonafarnib and temozolomide in patients with recurrent or temozolomide refractory glioblastoma.
Glioma
Phase I trial of tipifarnib in children with newly diagnosed intrinsic diffuse brainstem glioma.
Glioma
Phase I trial of tipifarnib in patients with recurrent malignant glioma taking enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.
Glioma
Phase II trial of tipifarnib and radiation in children with newly diagnosed diffuse intrinsic pontine gliomas.
Glioma
Phase II trial of tipifarnib in patients with recurrent malignant glioma either receiving or not receiving enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.
Glioma
The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.
Glomerulonephritis
Functional polymorphisms in inbred rat strains and their allele frequencies in commercially available outbred stocks.
Head and Neck Neoplasms
A Phase I trial of the farnesyltransferase inhibitor L-778,123 and radiotherapy for locally advanced lung and head and neck cancer.
Heart Diseases
Chemical Genetics Reveals a Role of Squalene Synthase in TGF? Signaling and Cardiomyogenesis.
Hematologic Neoplasms
Clinical development of farnesyltransferase inhibitors in leukemias and myelodysplastic syndrome.
Hematologic Neoplasms
Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.
Hematologic Neoplasms
Development of farnesyltransferase inhibitors for clinical cancer therapy: focus on hematologic malignancies.
Hematologic Neoplasms
Development of the farnesyltransferase inhibitor tipifarnib for therapy of hematologic malignancies.
Hematologic Neoplasms
Farnesyltransferase inhibition in hematologic malignancies: the clinical experience with tipifarnib.
Hematologic Neoplasms
Farnesyltransferase inhibitors in hematologic malignancies: new horizons in therapy.
Hematologic Neoplasms
Farnesyltransferase inhibitors: novel compounds in development for the treatment of myeloid malignancies.
Hematologic Neoplasms
Future clinical implications for farnesyltransferase inhibitors in hematologic malignancies.
Hematologic Neoplasms
In Vitro Apoptotic Effects of Farnesyltransferase blockade in Acute Myeloid Leukemia Cells.
Hematologic Neoplasms
Tipifarnib and tanespimycin show synergic proapoptotic activity in U937 cells.
Hepatitis C
Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation.
Hepatitis C
Targeting Cellular Squalene Synthase, an Enzyme Essential for Cholesterol Biosynthesis, Is a Potential Antiviral Strategy against Hepatitis C Virus.
Hepatitis C, Chronic
Role of FDFT1 polymorphism for fibrosis progression in patients with chronic hepatitis C.
Hepatitis, Autoimmune
The farnesyltransferase inhibitor tipifarnib protects against autoimmune hepatitis induced by Concanavalin A.
Hyperalgesia
Differential Effects of Subcutaneous Electrical Stimulation (SQS) and Transcutaneous Electrical Nerve Stimulation (TENS) in Rodent Models of Chronic Neuropathic or Inflammatory Pain.
Hypercholesterolemia
Antiproliferative and ultrastructural effects of BPQ-OH, a specific inhibitor of squalene synthase, on Leishmania amazonensis.
Hypercholesterolemia
Increased cholesterol biosynthesis and hypercholesterolemia in mice overexpressing squalene synthase in the liver.
Hypercholesterolemia
Isolation and structural determination of squalene synthase inhibitor from Prunus mume fruit.
Hypercholesterolemia
Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia.
Hypercholesterolemia
Lead nitrate-induced development of hypercholesterolemia in rats: sterol-independent gene regulation of hepatic enzymes responsible for cholesterol homeostasis.
Hypercholesterolemia
Pharmacologic inhibition of squalene synthase and other downstream enzymes of the cholesterol synthesis pathway: a new therapeutic approach to treatment of hypercholesterolemia.
Hypercholesterolemia
Squalene synthase: a critical enzyme in the cholesterol biosynthesis pathway.
Hyperinsulinism
Effect of insulin on farnesyltransferase gene transcription and mRNA stability.
Hyperinsulinism
Fetal hyperinsulinemia increases farnesylation of p21 Ras in fetal tissues.
Hyperinsulinism
Insulin potentiates platelet-derived growth factor action in vascular smooth muscle cells.
Hyperlactatemia
Burn-induced muscle metabolic derangements and mitochondrial dysfunction are associated with activation of HIF-1? and mTORC1: Role of protein farnesylation.
Hyperlipidemias
Characteristics of the squalene synthase inhibitors produced by a Streptomyces species isolated from soils.
Hyperlipidemias
Cholesterol diet-induced hyperlipidemia influences gene expression pattern of rat hearts: a DNA microarray study.
Hyperlipidemias
Design of Novel Potent Antihyperlipidemic Agents with Antioxidant/Anti-inflammatory Properties: Exploiting Phenothiazine's Strong Antioxidant Activity.
Hyperlipidemias
Discovery of Potential Inhibitors of Squalene Synthase from Traditional Chinese Medicine Based on Virtual Screening and In Vitro Evaluation of Lipid-Lowering Effect.
Hyperlipidemias
Docking study of novel antihyperlipidemic thieno[2,3-d]pyrimidine; LM-1554, with some molecular targets related to hyperlipidemia - an investigation into its mechanism of action.
Hyperlipidemias
Drug evaluation: TAK-475--an oral inhibitor of squalene synthase for hyperlipidemia.
Hyperlipidemias
Evaluation of potential inhibitors of squalene synthase based on virtual screening and in vitro studies.
Hyperlipoproteinemia Type II
Lipid-lowering effects of TAK-475, a squalene synthase inhibitor, in animal models of familial hypercholesterolemia.
Hyperpigmentation
Automated in vivo screen in zebrafish identifies Clotrimazole as targeting a metabolic vulnerability in a melanoma model.
Hypersensitivity
Differential Effects of Subcutaneous Electrical Stimulation (SQS) and Transcutaneous Electrical Nerve Stimulation (TENS) in Rodent Models of Chronic Neuropathic or Inflammatory Pain.
Hypersensitivity
Hypersensitivity of abscisic acid-induced cytosolic calcium increases in the Arabidopsis farnesyltransferase mutant era1-2.
Hypersensitivity
Role of farnesyltransferase in ABA regulation of guard cell anion channels and plant water loss.
Hypersensitivity
Squalene is lipotoxic to yeast cells defective in lipid droplet biogenesis.
Hypertension, Pulmonary
Effect of limonene and sobrerol on monocrotaline-induced lung alterations and pulmonary hypertension.
Hypertension, Pulmonary
Tipifarnib prevents development of hypoxia-induced pulmonary hypertension.
Hypertrophy, Right Ventricular
Effect of limonene and sobrerol on monocrotaline-induced lung alterations and pulmonary hypertension.
Infections
Endotoxin, tumor necrosis factor, and interleukin-1 decrease hepatic squalene synthase activity, protein, and mRNA levels in Syrian hamsters.
Infections
Expression, purification, and characterization of the human squalene synthase: use of yeast and baculoviral systems.
Infections
Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation.
Infections
Quantitative Proteomic Analysis of Simian Primary Hepatocytes Reveals Candidate Molecular Markers for Permissiveness to Relapsing Malaria Plasmodium Cynomolgi.
Infections
The farnesyltransferase ?-subunit RAM1 regulates localization of RAS proteins and appressorium-mediated infection in Magnaporthe oryzae.
Insulin Resistance
Burn-induced muscle metabolic derangements and mitochondrial dysfunction are associated with activation of HIF-1? and mTORC1: Role of protein farnesylation.
Insulin Resistance
Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle.
Insulin Resistance
The Association Between Hepatic Fat Content and Liver Injury in Obese Children and Adolescents: Effects of ethnicity, insulin resistance, and common gene variants.
Kidney Failure, Chronic
Farnesyltransferase inhibitor R115777 protects against vascular disease in uremic mice.
Laminopathies
LMNA-associated cardiocutaneous progeria: an inherited autosomal dominant premature aging syndrome with late onset.
Leishmaniasis
Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
Leukemia
A phase I clinical-pharmacodynamic study of the farnesyltransferase inhibitor tipifarnib in combination with the proteasome inhibitor bortezomib in advanced acute leukemias.
Leukemia
Advancing the treatment of hematologic malignancies through the development of targeted interventions.
Leukemia
Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial.
Leukemia
Clinical development of farnesyltransferase inhibitors in leukemias and myelodysplastic syndrome.
Leukemia
Clinical improvement by farnesyltransferase inhibition in NK large granular lymphocyte leukemia associated with imbalanced NK receptor signaling.
Leukemia
Combination of tipifarnib and rapamycin synergistically inhibits the growth of leukemia cells and overcomes resistance to tipifarnib via alteration of cellular signaling pathways.
Leukemia
Complete remission following clofarabine treatment in refractory juvenile myelomonocytic leukemia.
Leukemia
Enhancement of manumycin A-induced apoptosis by methoxyamine in myeloid leukemia cells.
Leukemia
Farnesyltransferase inhibitors and myeloid malignancies: phase I evidence of Zarnestra activity in high-risk leukemias.
Leukemia
Farnesyltransferase inhibitors interact synergistically with the Chk1 inhibitor UCN-01 to induce apoptosis in human leukemia cells through interruption of both Akt and MEK/ERK pathways and activation of SEK1/JNK.
Leukemia
Inhibition of juvenile myelomonocytic leukemia cell growth in vitro by farnesyltransferase inhibitors.
Leukemia
Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1? and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.
Leukemia
Relative importance of apoptosis and cell cycle blockage in the synergistic effect of combined R115777 and imatinib treatment in BCR/ABL-positive cell lines.
Leukemia
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Leukemia, Large Granular Lymphocytic
Clinical improvement by farnesyltransferase inhibition in NK large granular lymphocyte leukemia associated with imbalanced NK receptor signaling.
Leukemia, Large Granular Lymphocytic
Tipifarnib-mediated suppression of T-bet-dependent signaling pathways.
Leukemia, Lymphocytic, Chronic, B-Cell
Farnesyltransferase inhibitor BMS-214662 induces apoptosis in B-cell chronic lymphocytic leukemia cells.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Chronic myeloid leukemia: current therapies and the potential role of farnesyltransferase inhibitors.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Cloning and characterization of a human BCR/ABL-positive cell line, K562/RR, resistant to the farnesyltransferase inhibition by tipifarnib.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Involvement of nitric oxide in farnesyltransferase inhibitor-mediated apoptosis in chronic myeloid leukemia cells.
Leukemia, Myeloid
Combination of tipifarnib and rapamycin synergistically inhibits the growth of leukemia cells and overcomes resistance to tipifarnib via alteration of cellular signaling pathways.
Leukemia, Myeloid
In vitro and in vivo effects of a farnesyltransferase inhibitor on Nf1-deficient hematopoietic cells.
Leukemia, Myeloid
Synergistic cytotoxic effects in myeloid leukemia cells upon cotreatment with farnesyltransferase and geranylgeranyl transferase-I inhibitors.
Leukemia, Myeloid, Acute
A 2-gene classifier for predicting response to the farnesyltransferase inhibitor tipifarnib in acute myeloid leukemia.
Leukemia, Myeloid, Acute
A phase 1-2 study of a farnesyltransferase inhibitor, tipifarnib, combined with idarubicin and cytarabine for patients with newly diagnosed acute myeloid leukemia and high-risk myelodysplastic syndrome.
Leukemia, Myeloid, Acute
A phase 2 study of the farnesyltransferase inhibitor tipifarnib in poor-risk and elderly patients with previously untreated acute myelogenous leukemia.
Leukemia, Myeloid, Acute
A phase 2 study of the oral farnesyltransferase inhibitor tipifarnib in patients with refractory or relapsed acute myeloid leukemia.
Leukemia, Myeloid, Acute
Active oral regimen for elderly adults with newly diagnosed acute myelogenous leukemia: a preclinical and phase 1 trial of the farnesyltransferase inhibitor tipifarnib (R115777, Zarnestra) combined with etoposide.
Leukemia, Myeloid, Acute
Combining simvastatin with the farnesyltransferase inhibitor tipifarnib results in an enhanced cytotoxic effect in a subset of primary CD34+ acute myeloid leukemia samples.
Leukemia, Myeloid, Acute
Farnesyltransferase inhibitor therapy in acute myelogenous leukemia.
Leukemia, Myeloid, Acute
Farnesyltransferase inhibitor tipifarnib inhibits Rheb prenylation and stabilizes Bax in acute myelogenous leukemia cells.
Leukemia, Myeloid, Acute
Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.
Leukemia, Myeloid, Acute
Four different regimens of farnesyltransferase inhibitor tipifarnib in older, untreated acute myeloid leukemia patients: North American Intergroup Phase II study SWOG S0432.
Leukemia, Myeloid, Acute
Identification of molecular predictors of response in a study of tipifarnib treatment in relapsed and refractory acute myelogenous leukemia.
Leukemia, Myeloid, Acute
In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia.
Leukemia, Myeloid, Acute
In Vitro Apoptotic Effects of Farnesyltransferase blockade in Acute Myeloid Leukemia Cells.
Leukemia, Myeloid, Acute
Role of farnesyltransferase inhibitors in hematologic malignancies.
Leukemia, Myeloid, Acute
Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib.
Leukemia, Myeloid, Acute
[Farnesyltransferase inhibitors: preliminary results in acute myeloid leukemia]
Leukemia, Myelomonocytic, Juvenile
Inhibition of juvenile myelomonocytic leukemia cell growth in vitro by farnesyltransferase inhibitors.
Lipodystrophy
Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice.
Liver Diseases
Association of polymorphisms in GCKR and TRIB1 with nonalcoholic fatty liver disease and metabolic syndrome traits.
Liver Diseases
Plasma cholesterol-lowering and transient liver dysfunction in mice lacking squalene synthase in the liver.
Liver Failure, Acute
Farnesyltransferase inhibitor, tipifarnib, prevents galactosamine/lipopolysaccharide-induced acute liver failure.
Liver Neoplasms
Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent.
Liver Neoplasms
Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines.
Lung Diseases
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Lung Injury
Effect of limonene and sobrerol on monocrotaline-induced lung alterations and pulmonary hypertension.
Lung Neoplasms
An overview of farnesyltransferase inhibitors and their role in lung cancer therapy.
Lung Neoplasms
Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines.
Lung Neoplasms
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Lung Neoplasms
Effects of insulin-like growth factor binding protein-3 and farnesyltransferase inhibitor SCH66336 on Akt expression and apoptosis in non-small-cell lung cancer cells.
Lung Neoplasms
Farnesyltransferase inhibitors are potent lung cancer chemopreventive agents in A/J mice with a dominant-negative p53 and/or heterozygous deletion of Ink4a/Arf.
Lung Neoplasms
Hypoxia-inducible factor 1alpha and antiangiogenic activity of farnesyltransferase inhibitor SCH66336 in human aerodigestive tract cancer.
Lung Neoplasms
In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines.
Lung Neoplasms
Ras homologue enriched in brain is a critical target of farnesyltransferase inhibitors in non-small cell lung cancer cells.
Lung Neoplasms
Relationship of SNP rs2645429 in Farnesyl-Diphosphate Farnesyltransferase 1 Gene Promoter with Susceptibility to Lung Cancer.
Lung Neoplasms
Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis.
Lung Neoplasms
Squalene synthase promotes the invasion of lung cancer cells via the osteopontin/ERK pathway.
Lung Neoplasms
The farnesyltransferase inhibitor Lonafarnib induces growth arrest or apoptosis of human lung cancer cells without downregulation of Akt.
Lung Neoplasms
The farnesyltransferase inhibitor R115777 up-regulates the expression of death receptor 5 and enhances TRAIL-induced apoptosis in human lung cancer cells.
Lung Neoplasms
The farnesyltransferase inhibitor, FTI-2153, blocks bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells.
Lung Neoplasms
The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status.
Lymphoma
Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.
Lymphoma
Farnesyltransferase inhibitor tipifarnib inhibits Rheb prenylation and stabilizes Bax in acute myelogenous leukemia cells.
Lymphoma
Multi-institutional phase II of the farnesyltransferase inhibitor tipifarnib (R115777) in patients with relapsed and refractory lymphomas.
Lymphoma
Phase II trial and prediction of response of single agent tipifarnib in patients with relapsed/refractory mantle cell lymphoma: a Groupe d'Etude des Lymphomes de l'Adulte trial.
Lymphoma, B-Cell
Phase II trial and prediction of response of single agent tipifarnib in patients with relapsed/refractory mantle cell lymphoma: a Groupe d'Etude des Lymphomes de l'Adulte trial.
Lymphoma, Mantle-Cell
Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.
Lymphoma, Mantle-Cell
Phase II trial and prediction of response of single agent tipifarnib in patients with relapsed/refractory mantle cell lymphoma: a Groupe d'Etude des Lymphomes de l'Adulte trial.
Lymphoma, T-Cell
Roles of GTP and Rho GTPases in pancreatic islet beta cell function and dysfunction.
Malaria
2-Oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability.
Malaria
Development of benzophenone-based farnesyltransferase inhibitors as novel antimalarials.
Malaria
Effect of Farnesyltransferase Inhibitor R115777 on Mitochondria of Plasmodium falciparum.
Malaria
Farnesyltransferase inhibitors inhibit the growth of malaria parasites in vitro and in vivo.
Malaria
Molecular dynamic simulations and structure-based pharmacophore development for farnesyltransferase inhibitors discovery.
Malaria
Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.
Malaria
Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites.
Malaria
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.
Malaria
The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents.
Melanoma
Activated N-ras contributes to the chemoresistance of human melanoma in severe combined immunodeficiency (SCID) mice by blocking apoptosis.
Melanoma
Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines.
Melanoma
Phase II study of the farnesyltransferase inhibitor R115777 in advanced melanoma (CALGB 500104).
Melanoma
Sasanquasaponin ??? from Schima crenata Korth induces autophagy through Akt/mTOR/p70S6K pathway and promotes apoptosis in human melanoma A375 cells.
Mesothelioma
Farnesyltransferase inhibitors and human malignant pleural mesothelioma: a first-step comparative translational study.
Mesothelioma, Malignant
Farnesyltransferase inhibitors and human malignant pleural mesothelioma: a first-step comparative translational study.
Metabolic Syndrome
Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice.
Metabolism, Inborn Errors
Genetic disorders of cholesterol biosynthesis in mice and humans.
Mevalonate Kinase Deficiency
Anti-inflammatory and cytoprotective effects of a squalene synthase inhibitor, TAK-475 active metabolite-I, in immune cells simulating mevalonate kinase deficiency (MKD)-like condition.
Mevalonate Kinase Deficiency
Genetic disorders of cholesterol biosynthesis in mice and humans.
Multiple Myeloma
Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells.
Multiple Myeloma
Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.
Multiple Myeloma
Farnesyltransferase inhibitors and rapamycin in the treatment of multiple myeloma.
Multiple Myeloma
Farnesyltransferase inhibitors and their role in the treatment of multiple myeloma.
Multiple Myeloma
The farnesyltransferase inhibitor L744832 potentiates UCN-01-induced apoptosis in human multiple myeloma cells.
Muscular Diseases
Protective effects of a squalene synthase inhibitor, lapaquistat acetate (TAK-475), on statin-induced myotoxicity in guinea pigs.
Mycoses
Synthetic arylquinuclidine derivatives exhibit antifungal activity against Candida albicans, Candida tropicalis and Candida parapsilopsis.
Mycoses
Virus-induced gene silencing of Withania somnifera squalene synthase negatively regulates sterol and defence-related genes resulting in reduced withanolides and biotic stress tolerance.
Myelodysplastic Syndromes
A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome.
Myelodysplastic Syndromes
A phase 1-2 study of a farnesyltransferase inhibitor, tipifarnib, combined with idarubicin and cytarabine for patients with newly diagnosed acute myeloid leukemia and high-risk myelodysplastic syndrome.
Myelodysplastic Syndromes
Advancing the treatment of hematologic malignancies through the development of targeted interventions.
Myelodysplastic Syndromes
Clinical development of farnesyltransferase inhibitors in leukemias and myelodysplastic syndrome.
Myelodysplastic Syndromes
Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting.
Myelodysplastic Syndromes
Farnesyltransferase inhibitors and their potential role in therapy for myelodysplastic syndromes and acute myeloid leukaemia.
Myelodysplastic Syndromes
Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.
Myelodysplastic Syndromes
Farnesyltransferase inhibitors in myelodysplastic syndrome.
Myelodysplastic Syndromes
In vitro effects of the farnesyltransferase inhibitor tipifarnib on myelodysplastic syndrome progenitors.
Myelodysplastic Syndromes
Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib.
Myocardial Infarction
Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions.
Myocardial Infarction
Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.
Myocardial Infarction
[Evaluation of ventricular arrhythmias late after coronary artery bypass graft surgery--relation to clinical variables]
Myotoxicity
Discovery of Potential Inhibitors of Squalene Synthase from Traditional Chinese Medicine Based on Virtual Screening and In Vitro Evaluation of Lipid-Lowering Effect.
Myotoxicity
Inhibition of cholesterol synthesis by squalene synthase inhibitors does not induce myotoxicity in vitro.
Myotoxicity
Protective effects of a squalene synthase inhibitor, lapaquistat acetate (TAK-475), on statin-induced myotoxicity in guinea pigs.
Myotoxicity
Statins induce apoptosis in rat and human myotube cultures by inhibiting protein geranylgeranylation but not ubiquinone.
Neoplasm Metastasis
Feasibility of CT scan-guided Tru-Cut serial liver biopsies to evaluate pharmacodynamic endpoints in patients with liver metastasis treated with experimental drugs.
Neoplasm Metastasis
Liver metastasis models of colon cancer for evaluation of drug efficacy using NOD/Shi-scid IL2Rgammanull (NOG) mice.
Neoplasm Metastasis
Selective inhibition of cancer cell invasion by a geranylgeranyltransferase-I inhibitor.
Neoplasm Metastasis
Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis.
Neoplasm Metastasis
Squalene synthase promotes the invasion of lung cancer cells via the osteopontin/ERK pathway.
Neoplasms
(--)-Xanthatin selectively induces GADD45? and stimulates caspase-independent cell death in human breast cancer MDA-MB-231 cells.
Neoplasms
20(S)-Rg3 upregulates FDFT1 via reducing miR-4425 to inhibit ovarian cancer progression.
Neoplasms
3D-QSAR with the aid of pharmacophore search and docking-based alignments for farnesyltransferase inhibitors.
Neoplasms
8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells.
Neoplasms
A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.
Neoplasms
A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
Neoplasms
A novel amplicon at 8p22-23 results in overexpression of cathepsin B in esophageal adenocarcinoma.
Neoplasms
A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors.
Neoplasms
A phase I study of the farnesyltransferase inhibitor Tipifarnib in combination with the epidermal growth factor tyrosine kinase inhibitor Erlotinib in patients with advanced solid tumors.
Neoplasms
A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.
Neoplasms
Absence of the CAAX endoprotease Rce1: effects on cell growth and transformation.
Neoplasms
Activity of SCH 66336, a tricyclic farnesyltransferase inhibitor, against human tumor colony-forming units.
Neoplasms
Advances in the development of farnesyltransferase inhibitors: substrate recognition by protein farnesyltransferase.
Neoplasms
Advancing the treatment of hematologic malignancies through the development of targeted interventions.
Neoplasms
An overview on natural farnesyltransferase inhibitors for efficient cancer therapy.
Neoplasms
Anticancer Activity of BIM-46174, a New Inhibitor of the Heterotrimeric G{alpha}/G{beta}{gamma} Protein Complex.
Neoplasms
Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.
Neoplasms
Antitumor effects of low-dose tipifarnib on the mTOR signaling pathway and reactive oxygen species production in HIF-1?-expressing gastric cancer cells.
Neoplasms
Apoptotic and cytostatic farnesyltransferase inhibitors have distinct pharmacology and efficacy profiles in tumor models.
Neoplasms
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Neoplasms
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Neoplasms
Assessment of the bioactive conformation of the farnesyltransferase protein binding recognition motif by computational methods.
Neoplasms
Atorvastatin inhibits pancreatic carcinogenesis and increases survival in LSL-Kras(G12D) -LSL-Trp53(R172H) -Pdx1-Cre mice.
Neoplasms
BMS-214662 potently induces apoptosis of chronic myeloid leukemia stem and progenitor cells and synergizes with tyrosine kinase inhibitors.
Neoplasms
Both farnesylated and geranylgeranylated RhoB inhibit malignant transformation and suppress human tumor growth in nude mice.
Neoplasms
Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts.
Neoplasms
c-myc down-regulation induces apoptosis in human cancer cell lines exposed to RPR-115135 (C31H29NO4), a non-peptidomimetic farnesyltransferase inhibitor.
Neoplasms
Cdk inhibitors, roscovitine and olomoucine, synergize with farnesyltransferase inhibitor (FTI) to induce efficient apoptosis of human cancer cell lines.
Neoplasms
Characterization of farnesyl diphosphate farnesyl transferase 1 (FDFT1) expression in cancer.
Neoplasms
Chemoprevention of benzo(a)pyrene-induced lung tumors in mice by the farnesyltransferase inhibitor R115777.
Neoplasms
Chemopreventive effect of perillyl alcohol on 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induced tumorigenesis in (C3H/HeJ X A/J)F1 mouse lung.
Neoplasms
Clinical and pharmacologic study of the farnesyltransferase inhibitor tipifarnib in cancer patients with normal or mildly or moderately impaired hepatic function.
Neoplasms
Combined effect of protein kinase B inhibitor or extracellular signal-regulated kinase inhibitor against farnesyltransferase inhibition-induced apoptosis in SiHa cells.
Neoplasms
Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines.
Neoplasms
Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.
Neoplasms
Comparison of Multiparametric MRI Scoring Systems and the Impact on Cancer Detection in Patients Undergoing MR US Fusion Guided Prostate Biopsies.
Neoplasms
Computer-aided drug design and ADMET predictions for identification and evaluation of novel potential farnesyltransferase inhibitors in cancer therapy.
Neoplasms
Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.
Neoplasms
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Neoplasms
Design, Synthesis, and Evaluation of Novel Modular Bisubstrate Analogue Inhibitors of Farnesyltransferase.
Neoplasms
Development of farnesyltransferase inhibitors for clinical cancer therapy: focus on hematologic malignancies.
Neoplasms
Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone.
Neoplasms
Effect of novel CAAX peptidomimetic farnesyltransferase inhibitor on angiogenesis in vitro and in vivo.
Neoplasms
Effects of statins and farnesyltransferase inhibitors on the development and progression of cancer.
Neoplasms
Efficacy of the farnesyltransferase inhibitor R115777 in a rat mammary tumor model: role of Ha-ras mutations and use of microarray analysis in identifying potential targets.
Neoplasms
Endotoxin, tumor necrosis factor, and interleukin-1 decrease hepatic squalene synthase activity, protein, and mRNA levels in Syrian hamsters.
Neoplasms
Enhancement of interleukin-12 gene-based tumor immunotherapy by the reduced secretion of p40 subunit and the combination with farnesyltransferase inhibitor.
Neoplasms
Enhancement of tumor response by farnesyltransferase inhibitor in C3H/HeJ hepatocarcinoma.
Neoplasms
Enlarging the scope of cell-penetrating prenylated peptides to include farnesylated 'CAAX' box sequences and diverse cell types.
Neoplasms
Expression of the farnesyltransferase beta-subunit gene in human ovarian carcinoma: correlation to K-ras mutation.
Neoplasms
Farnesyltransferase and geranylgeranyltransferase I inhibitors and cancer therapy: lessons from mechanism and bench-to-bedside translational studies.
Neoplasms
Farnesyltransferase and geranylgeranyltransferase I inhibitors in cancer therapy: important mechanistic and bench to bedside issues.
Neoplasms
Farnesyltransferase and geranylgeranyltransferase I inhibitors upregulate RhoB expression by HDAC1 dissociation, HAT association and histone acetylation of the RhoB promoter.
Neoplasms
Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling.
Neoplasms
Farnesyltransferase inhibition in hematologic malignancies: the clinical experience with tipifarnib.
Neoplasms
Farnesyltransferase inhibitor effects on prostate tumor micro-environment and radiation survival.
Neoplasms
Farnesyltransferase inhibitor FTI-277 inhibits PD-L1 expression on septic spleen lymphocytes and promotes spleen lymphocyte activation.
Neoplasms
Farnesyltransferase Inhibitor Manumycin Targets IL1?-Ras-HIF-1? Axis in Tumor Cells of Diverse Origin.
Neoplasms
Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells.
Neoplasms
Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.
Neoplasms
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Neoplasms
Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent.
Neoplasms
Farnesyltransferase inhibitor-induced regression of mammary tumors in TGF alpha and TGF alpha/neu transgenic mice correlates with inhibition of map kinase and p70s6 kinase phosphorylation.
Neoplasms
Farnesyltransferase inhibitors and human malignant pleural mesothelioma: a first-step comparative translational study.
Neoplasms
Farnesyltransferase inhibitors and myeloid malignancies: phase I evidence of Zarnestra activity in high-risk leukemias.
Neoplasms
Farnesyltransferase inhibitors induce cytochrome c release and caspase 3 activation preferentially in transformed cells.
Neoplasms
Farnesyltransferase inhibitors induce DNA damage via reactive oxygen species in human cancer cells.
Neoplasms
Farnesyltransferase inhibitors induce dramatic morphological changes of KNRK cells that are blocked by microtubule interfering agents.
Neoplasms
Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS.
Neoplasms
Farnesyltransferase inhibitors reverse Ras-mediated inhibition of Fas gene expression.
Neoplasms
Farnesyltransferase inhibitors target multiple endothelial cell functions in angiogenesis.
Neoplasms
Farnesyltransferase Inhibitors: A Comprehensive Review Based on Quantitative Structural Analysis.
Neoplasms
Farnesyltransferase inhibitors: antineoplastic properties, mechanisms of action, and clinical prospects.
Neoplasms
Farnesyltransferase inhibitors: novel compounds in development for the treatment of myeloid malignancies.
Neoplasms
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic.
Neoplasms
Fasting inhibits aerobic glycolysis and proliferation in colorectal cancer via the Fdft1-mediated AKT/mTOR/HIF1? pathway suppression.
Neoplasms
Geranylgeranylated RhoB mediates suppression of human tumor cell growth by farnesyltransferase inhibitors.
Neoplasms
Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.
Neoplasms
GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.
Neoplasms
Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines.
Neoplasms
Have molecular hybrids delivered effective anti-cancer treatments and what should future drug discovery focus on?
Neoplasms
High affinity for farnesyltransferase and alternative prenylation contribute individually to K-Ras4B resistance to farnesyltransferase inhibitors.
Neoplasms
Hypoxia-inducible factor 1alpha and antiangiogenic activity of farnesyltransferase inhibitor SCH66336 in human aerodigestive tract cancer.
Neoplasms
Identification of novel peptide substrates for protein farnesyltransferase reveals two substrate classes with distinct sequence selectivities.
Neoplasms
Implications of farnesyltransferase and its inhibitors as a promising strategy for cancer therapy.
Neoplasms
In vitro and in vivo effects of a farnesyltransferase inhibitor on Nf1-deficient hematopoietic cells.
Neoplasms
Increased farnesyltransferase activity in human colorectal cancer: relationship with clinicopathological features and K-ras mutation.
Neoplasms
Indolizine-phenothiazine hybrids as the first dual inhibitors of tubulin polymerization and farnesyltransferase with synergistic antitumor activity.
Neoplasms
Induction of N-myc in neuroblastoma by autocrine IGF-II depends on farnesylated Ras. Application of farnesyltransferase inhibitors.
Neoplasms
Inhibition of farnesyltransferase increases TGFbeta type II receptor expression and enhances the responsiveness of human cancer cells to TGFbeta.
Neoplasms
Inhibition of farnesyltransferase reduces angiogenesis by interrupting endothelial cell migration.
Neoplasms
Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue.
Neoplasms
Inhibition of human tumor cell growth in vitro and in vivo by a specific inhibitor of human farnesyltransferase: BIM-46068.
Neoplasms
Inhibition of human tumor cell growth in vivo by an orally bioavailable inhibitor of human farnesyltransferase, BIM-46228.
Neoplasms
Inhibition of Ras and related guanosine triphosphate-dependent proteins as a therapeutic strategy for blocking malignant glioma growth: II--preclinical studies in a nude mouse model.
Neoplasms
Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines.
Neoplasms
Inhibition of the Ras/Raf/MEK/ERK and RET Kinase Pathways with the Combination of the Multikinase Inhibitor Sorafenib and the Farnesyltransferase Inhibitor Tipifarnib in Medullary and Differentiated Thyroid Malignancies.
Neoplasms
Lipid synthesis and processing proteins ABHD5, PGRMC1 and squalene synthase can serve as novel immunohistochemical markers for sebaceous neoplasms and differentiate sebaceous carcinoma from sebaceoma and basal cell carcinoma with clear cell features.
Neoplasms
Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas.
Neoplasms
Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1? and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.
Neoplasms
MicroRNA induction by copy number gain is associated with poor outcome in squamous cell carcinoma of the lung.
Neoplasms
Molecular dynamic simulations and structure-based pharmacophore development for farnesyltransferase inhibitors discovery.
Neoplasms
Molecular Pathways: Targeting the Dependence of Mutant RAS Cancers on the DNA Damage Response.
Neoplasms
New applications of squalene synthase inhibitors: Membrane cholesterol as a therapeutic target.
Neoplasms
Pancreatic cancer cell radiation survival and prenyltransferase inhibition: the role of K-Ras.
Neoplasms
Phase I and pharmacokinetic study of the farnesyltransferase inhibitor R115777 in combination with irinotecan in patients with advanced cancer.
Neoplasms
Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.
Neoplasms
Phase I and pharmacological study of the farnesyltransferase inhibitor tipifarnib (Zarnestra, R115777) in combination with gemcitabine and cisplatin in patients with advanced solid tumours.
Neoplasms
Phase I and pharmacological study of the oral farnesyltransferase inhibitor SCH 66336 given once daily to patients with advanced solid tumours.
Neoplasms
Phase I clinical trial of the farnesyltransferase inhibitor BMS-214662 administered as a weekly 24 h continuous intravenous infusion in patients with advanced solid tumors.
Neoplasms
Phase I clinical trial of the farnesyltransferase inhibitor BMS-214662 given as a 1-hour intravenous infusion in patients with advanced solid tumors.
Neoplasms
Phase I pharmacokinetic and pharmacodynamic study of weekly 1-hour and 24-hour infusion BMS-214662, a farnesyltransferase inhibitor, in patients with advanced solid tumors.
Neoplasms
Phase I study of the farnesyltransferase inhibitor BMS-214662 given weekly in patients with solid tumors.
Neoplasms
Phase I study of the farnesyltransferase inhibitor lonafarnib with paclitaxel in solid tumors.
Neoplasms
Phase I study of the farnesyltransferase inhibitor lonafarnib with weekly paclitaxel in patients with solid tumors.
Neoplasms
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Neoplasms
Phase I trial of a combination of the multikinase inhibitor sorafenib and the farnesyltransferase inhibitor tipifarnib in advanced malignancies.
Neoplasms
Phase II trial of the farnesyltransferase inhibitor tipifarnib plus fulvestrant in hormone receptor-positive metastatic breast cancer: New York Cancer Consortium Trial P6205.
Neoplasms
Post-translational modifications and regulation of the RAS superfamily of GTPases as anticancer targets.
Neoplasms
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
Neoplasms
Potentiated antitumor effects of a combination therapy with a farnesyltransferase inhibitor L-744,832 and butyrate in vitro.
Neoplasms
Potentiation of nitric oxide-induced apoptosis of MDA-MB-468 cells by farnesyltransferase inhibitor: implications in breast cancer.
Neoplasms
Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors.
Neoplasms
Protein farnesylation in mammalian cells: effects of farnesyltransferase inhibitors on cancer cells.
Neoplasms
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Neoplasms
Quantitative Gene Expression of ERG9 in Model Saccharomyces cerevisiae: Chamomile Extract For Human Cancer Treatment.
Neoplasms
R115777 (Zarnestra)/Zoledronic acid (Zometa) cooperation on inhibition of prostate cancer proliferation is paralleled by Erk/Akt inactivation and reduced Bcl-2 and bad phosphorylation.
Neoplasms
Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion.
Neoplasms
Ras farnesyltransferase inhibitors suppress the phenotype resulting from an activated ras mutation in Caenorhabditis elegans.
Neoplasms
ras protein p21 processing enzyme farnesyltransferase in chemical carcinogen-induced murine skin tumors.
Neoplasms
Reactive oxygen species-dependent destruction of MEK and Akt in Manumycin stimulated death of lymphoid tumor and myeloma cell lines.
Neoplasms
Recent advances in understanding the antineoplastic mechanisms of farnesyltransferase inhibitors.
Neoplasms
RhoB, not RhoA, represses the transcription of the transforming growth factor beta type II receptor by a mechanism involving activator protein 1.
Neoplasms
Role of squalene synthase in prostate cancer risk and the biological aggressiveness of human prostate cancer.
Neoplasms
Roles of Farnesyl-Diphosphate Farnesyltransferase 1 in Tumour and Tumour Microenvironments.
Neoplasms
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Neoplasms
Selective drug combination vulnerabilities in STAT3- and TP53-mutant malignant NK cells.
Neoplasms
Selective inhibition of cancer cell invasion by a geranylgeranyltransferase-I inhibitor.
Neoplasms
Sequential simulation (SqS) of clinical pathways: a tool for public and patient engagement in point-of-care diagnostics.
Neoplasms
Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis.
Neoplasms
Squalene synthase, a determinant of Raft-associated cholesterol and modulator of cancer cell proliferation.
Neoplasms
Successful molecular dynamics simulation of the zinc-bound farnesyltransferase using the cationic dummy atom approach.
Neoplasms
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.
Neoplasms
Synthesis, biodistribution and effects of farnesyltransferase inhibitor therapy on tumour uptake in mice of 99mTc labelled epidermal growth factor.
Neoplasms
Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors.
Neoplasms
Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.
Neoplasms
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Neoplasms
Targeting the Ras signaling pathway: a rational, mechanism-based treatment for hematologic malignancies?
Neoplasms
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Neoplasms
The discovery of a novel compound with potent antitumor activity: virtual screening, synthesis, biological evaluation and preliminary mechanism study.
Neoplasms
The farnesyl transferase inhibitor RPR-130401 does not alter radiation susceptibility in human tumor cells with a K-Ras mutation in spite of large changes in ploidy and lamin B distribution.
Neoplasms
The farnesyl transferase inhibitor, FTI-277, inhibits growth and induces apoptosis in drug-resistant myeloma tumor cells.
Neoplasms
The farnesyltransferase inhibitor L744,832 reduces hypoxia in tumors expressing activated H-ras.
Neoplasms
The Farnesyltransferase Inhibitor LB42708 Suppresses VEGF-induced Angiogenesis by Inhibiting Ras-dependent MAPK and PI3K/Akt Signal Pathways.
Neoplasms
The farnesyltransferase inhibitor lonafarnib induces CCAAT/enhancer-binding protein homologous protein-dependent expression of death receptor 5, leading to induction of apoptosis in human cancer cells.
Neoplasms
The farnesyltransferase inhibitor R115777 up-regulates the expression of death receptor 5 and enhances TRAIL-induced apoptosis in human lung cancer cells.
Neoplasms
The farnesyltransferase inhibitor, FPT inhibitor III upregulates Bax and Bcl-xs expression and induces apoptosis in human ovarian cancer cells.
Neoplasms
The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner.
Neoplasms
The noncoding RNAs SNORD50A and SNORD50B bind K-Ras and are recurrently deleted in human cancer.
Neoplasms
The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents.
Neoplasms
Ubiquitin specific peptidase 32 acts as an oncogene in epithelial ovarian cancer by deubiquitylating farnesyl-diphosphate farnesyltransferase 1.
Neoplasms
Ultrasounds-mediated 10-seconds synthesis of chalcones as potential farnesyltransferase inhibitors.
Neoplasms
Use of synthetic isoprenoids to target protein prenylation and Rho GTPases in breast cancer invasion.
Neoplasms
Virtual lead identification of farnesyltransferase inhibitors based on ligand and structure-based pharmacophore techniques.
Neoplasms
[Inhibitors of farnesyltransferase: a new approach for development of potential cancer drugs]
Neuralgia
Differential Effects of Subcutaneous Electrical Stimulation (SQS) and Transcutaneous Electrical Nerve Stimulation (TENS) in Rodent Models of Chronic Neuropathic or Inflammatory Pain.
Neuroblastoma
24S-hydroxycholesterol effects on lipid metabolism genes are modeled in traumatic brain injury.
Neuroblastoma
Farnesyltransferase inhibitor attenuates methamphetamine toxicity-induced Ras proteins activation and cell death in neuroblastoma SH-SY5Y cells.
Neuroblastoma
Farnesyltransferase inhibitor FTI-277 prevents autocrine growth stimulation of neuroblastoma by BDNF.
Neuroblastoma
Induction of N-myc in neuroblastoma by autocrine IGF-II depends on farnesylated Ras. Application of farnesyltransferase inhibitors.
Neurofibroma, Plexiform
Phase 2 randomized, flexible crossover, double-blinded, placebo-controlled trial of the farnesyltransferase inhibitor tipifarnib in children and young adults with neurofibromatosis type 1 and progressive plexiform neurofibromas.
Neurofibroma, Plexiform
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Neurofibromatoses
Farnesyltransferase inhibitors block the neurofibromatosis type I (NF1) malignant phenotype.
Neurofibromatoses
Phase 2 randomized, flexible crossover, double-blinded, placebo-controlled trial of the farnesyltransferase inhibitor tipifarnib in children and young adults with neurofibromatosis type 1 and progressive plexiform neurofibromas.
Neurofibromatoses
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Neurofibromatosis 1
Farnesyltransferase inhibitors block the neurofibromatosis type I (NF1) malignant phenotype.
Neurofibromatosis 1
Phase 2 randomized, flexible crossover, double-blinded, placebo-controlled trial of the farnesyltransferase inhibitor tipifarnib in children and young adults with neurofibromatosis type 1 and progressive plexiform neurofibromas.
Neurofibromatosis 1
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Non-alcoholic Fatty Liver Disease
Association of polymorphisms in GCKR and TRIB1 with nonalcoholic fatty liver disease and metabolic syndrome traits.
Non-alcoholic Fatty Liver Disease
Association Study of Seven GWAS-Identified Common Variants with Nonalcoholic Fatty Liver Disease in Chinese Children.
Non-alcoholic Fatty Liver Disease
Bavachinin inhibits cholesterol synthesis enzyme FDFT1 expression via AKT/mTOR/SREBP-2 pathway.
Non-alcoholic Fatty Liver Disease
The Epidemiology, Risk Profiling and Diagnostic Challenges of Nonalcoholic Fatty Liver Disease.
Obesity
Relationship between overweight, obesity and sleep disorders in adolescents from selected cities of Upper Silesia, Poland.
Obesity
Studies of CTNNBL1 and FDFT1 variants and measures of obesity: analyses of quantitative traits and case-control studies in 18,014 Danes.
Obesity, Morbid
Studies of CTNNBL1 and FDFT1 variants and measures of obesity: analyses of quantitative traits and case-control studies in 18,014 Danes.
Osteoporosis, Postmenopausal
Association between FDFT1 gene polymorphism and postmenopausal osteoporosis.
Osteosarcoma
Driven to Death: Inhibition of Farnesylation Increases Ras Activity in Osteosarcoma and Promotes Growth Arrest and Cell Death.
Ovarian Neoplasms
20(S)-Rg3 upregulates FDFT1 via reducing miR-4425 to inhibit ovarian cancer progression.
Ovarian Neoplasms
Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.
Ovarian Neoplasms
Involvement of caspase family proteases in FPT inhibitor III-induced apoptosis in human ovarian cancer cells.
Ovarian Neoplasms
Randomized phase II trial of carboplatin and paclitaxel with or without lonafarnib in first-line treatment of epithelial ovarian cancer stage IIB-IV.
Ovarian Neoplasms
The farnesyltransferase inhibitor, FPT inhibitor III upregulates Bax and Bcl-xs expression and induces apoptosis in human ovarian cancer cells.
Overweight
Relationship between overweight, obesity and sleep disorders in adolescents from selected cities of Upper Silesia, Poland.
Overweight
Studies of CTNNBL1 and FDFT1 variants and measures of obesity: analyses of quantitative traits and case-control studies in 18,014 Danes.
Pancreatic Neoplasms
A phase I trial of the dual farnesyltransferase and geranylgeranyltransferase inhibitor L-778,123 and radiotherapy for locally advanced pancreatic cancer.
Pancreatic Neoplasms
Farnesyltransferase inhibitor (L-744,832) restores TGF-beta type II receptor expression and enhances radiation sensitivity in K-ras mutant pancreatic cancer cell line MIA PaCa-2.
Pancreatic Neoplasms
Inhibition of growth and invasive activity of human pancreatic cancer cells by a farnesyltransferase inhibitor, manumycin.
Pancreatic Neoplasms
Nanoformulation of Geranylgeranyltransferase-I Inhibitors for Cancer Therapy: Liposomal Encapsulation and pH-Dependent Delivery to Cancer Cells.
Pancreatic Neoplasms
Phase III trial of gemcitabine plus tipifarnib compared with gemcitabine plus placebo in advanced pancreatic cancer.
Pancreatic Neoplasms
Requirement of c-jun N-terminal kinase for apoptotic cell death induced by farnesyltransferase inhibitor, farnesylamine, in human pancreatic cancer cells.
Pancreatic Neoplasms
[Oleylamine (long-chain fatty amine)-induced cell death through MAP kinase pathways in human pancreatic cancer cells]
Pancreatitis
Farnesyltransferase regulates neutrophil recruitment and tissue damage in acute pancreatitis.
Papilloma
ras protein p21 processing enzyme farnesyltransferase in chemical carcinogen-induced murine skin tumors.
Parasitic Diseases
Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
Pheochromocytoma
L-NAME has opposite effects on the productions of S-adenosylhomocysteine and S-adenosylmethionine in V12-H-Ras and M-CR3B-Ras pheochromocytoma cells.
Pneumonia
Streptococcal M1 protein triggers farnesyltransferase-dependent formation of CXC chemokines in alveolar macrophages and neutrophil infiltration in the lung.
Polycythemia Vera
Farnesyltransferase inhibitor tipifarnib (R115777) preferentially inhibits in vitro autonomous erythropoiesis of polycythemia vera patient cells.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Environment-mediated drug resistance in Bcr/Abl-positive acute lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Farnesyltransferase inhibitors: molecular evidence of therapeutic efficacy in acute lymphoblastic leukemia through cyclin d1 inhibition.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Increased resistance to a farnesyltransferase inhibitor by N-cadherin expression in Bcr/Abl-P190 lymphoblastic leukemia cells.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Resistance to farnesyltransferase inhibitors in Bcr/Abl-positive lymphoblastic leukemia by increased expression of a novel ABC transporter homolog ATP11a.
Primary Myelofibrosis
In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia.
Progeria
A farnesyltransferase inhibitor improves disease phenotypes in mice with a Hutchinson-Gilford progeria syndrome mutation.
Progeria
A farnesyltransferase inhibitor prevents both the onset and late progression of cardiovascular disease in a progeria mouse model.
Progeria
Baricitinib, a JAK-STAT Inhibitor, Reduces the Cellular Toxicity of the Farnesyltransferase Inhibitor Lonafarnib in Progeria Cells.
Progeria
Clinical trial of a farnesyltransferase inhibitor in children with Hutchinson-Gilford progeria syndrome.
Progeria
Defective lamin A-Rb signaling in Hutchinson-Gilford Progeria Syndrome and reversal by farnesyltransferase inhibition.
Progeria
Disruption of lamin B1 and lamin B2 processing and localization by farnesyltransferase inhibitors.
Progeria
Dysfunction of iPSC-derived endothelial cells in human Hutchinson-Gilford progeria syndrome.
Progeria
Farnesyltransferase inhibitor and rapamycin correct aberrant genome organisation and decrease DNA damage respectively, in Hutchinson-Gilford progeria syndrome fibroblasts.
Progeria
Farnesyltransferase inhibitor treatment restores chromosome territory positions and active chromosome dynamics in Hutchinson-Gilford Progeria syndrome cells.
Progeria
Incomplete processing of mutant lamin A in Hutchinson-Gilford progeria leads to nuclear abnormalities, which are reversed by farnesyltransferase inhibition.
Progeria
Increased mechanosensitivity and nuclear stiffness in Hutchinson-Gilford progeria cells: effects of farnesyltransferase inhibitors.
Progeria
Intermittent treatment with farnesyltransferase inhibitor and sulforaphane improves cellular homeostasis in Hutchinson-Gilford progeria fibroblasts.
Progeria
Molecular dynamic simulations and structure-based pharmacophore development for farnesyltransferase inhibitors discovery.
Progeria
Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.
Progeria
Treatment with a farnesyltransferase inhibitor improves survival in mice with a Hutchinson-Gilford progeria syndrome mutation.
Prostatic Diseases
Role of squalene synthase in prostate cancer risk and the biological aggressiveness of human prostate cancer.
Prostatic Neoplasms
Androgen-dependent alternative mRNA isoform expression in prostate cancer cells.
Prostatic Neoplasms
Comparison of Multiparametric MRI Scoring Systems and the Impact on Cancer Detection in Patients Undergoing MR US Fusion Guided Prostate Biopsies.
Prostatic Neoplasms
Potent Farnesyltransferase Inhibitors with 1,4-Diazepane Scaffolds as Novel Destabilizing Microtubule Agents in Hormone-Resistant Prostate Cancer.
Prostatic Neoplasms
Role of squalene synthase in prostate cancer risk and the biological aggressiveness of human prostate cancer.
Prostatic Neoplasms
Squalene synthase, a determinant of Raft-associated cholesterol and modulator of cancer cell proliferation.
Pulmonary Disease, Chronic Obstructive
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Sepsis
Farnesyltransferase inhibitor FTI-277 inhibits PD-L1 expression on septic spleen lymphocytes and promotes spleen lymphocyte activation.
Sepsis
Farnesyltransferase inhibitor, FTI-277, reduces mortality of septic mice along with improved bacterial clearance.
Sexually Transmitted Diseases
Aromatase inhibitors: combinations with fulvestrant or signal transduction inhibitors as a strategy to overcome endocrine resistance.
Sleep Initiation and Maintenance Disorders
A New Single-Item Sleep Quality Scale: Results of Psychometric Evaluation in Patients With Chronic Primary Insomnia and Depression.
squalene synthase deficiency
Basis for abnormal desquamation and permeability barrier dysfunction in RXLI.
squalene synthase deficiency
Squalene Synthase Deficiency: Clinical, Biochemical, and Molecular Characterization of a Defect in Cholesterol Biosynthesis.
Squamous Cell Carcinoma of Head and Neck
A Farnesyltransferase Inhibitor Shows Efficacy in HRAS-Mutant HNSCC.
Squamous Cell Carcinoma of Head and Neck
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Stomach Neoplasms
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Streptococcal Infections
Streptococcal M1 protein triggers farnesyltransferase-dependent formation of CXC chemokines in alveolar macrophages and neutrophil infiltration in the lung.
Stroke
Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.
Synostosis
Additional squamosal suture synostosis and segmented intracranial volume in patients with non-syndromic sagittal synostosis.
Synovitis
Analysis of correlation and causes for discrepancy between quantitative and semi-quantitative Doppler scores in synovitis in rheumatoid arthritis.
Tauopathies
A farnesyltransferase inhibitor activates lysosomes and reduces tau pathology in mice with tauopathy.
Thyroid Carcinoma, Anaplastic
Angiogenesis inhibition in the in vivo antineoplastic effect of manumycin and paclitaxel against anaplastic thyroid carcinoma.
Thyroid Carcinoma, Anaplastic
Bcl-2-associated X protein is the main mediator of manumycin a-induced apoptosis in anaplastic thyroid cancer cells.
Thyroid Carcinoma, Anaplastic
Combining a matrix metalloproteinase inhibitor, a farnesyltransferase inhibitor, and a taxane improves survival in an anaplastic thyroid cancer model.
Thyroid Carcinoma, Anaplastic
Cytochrome c release is upstream to activation of caspase-9, caspase-8, and caspase-3 in the enhanced apoptosis of anaplastic thyroid cancer cells induced by manumycin and paclitaxel.
Thyroid Carcinoma, Anaplastic
Modulation of parathyroid hormone-related protein levels (PTHrP) in anaplastic thyroid cancer.
Thyroid Carcinoma, Anaplastic
p21 Waf-1 (Cip-1) enhances apoptosis induced by manumycin and paclitaxel in anaplastic thyroid cancer cells.
Thyroid Carcinoma, Anaplastic
Redox Control of Manumycin A-Induced Apoptosis in Anaplastic Thyroid Cancer Cells: Involvement of the Xenobiotic Apoptotic Pathway.
Triple Negative Breast Neoplasms
Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1? and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.
Uterine Cervical Neoplasms
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Vascular Diseases
Farnesyltransferase inhibitor R115777 protects against vascular disease in uremic mice.
Vitreoretinopathy, Proliferative
Role of inhibitors of isoprenylation in proliferation, phenotype and apoptosis of human retinal pigment epithelium.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
squalene synthase consists of both an N-terminal catalytic domain and a C-terminal domain which consists of a hinge region and a membrane spanning helix responsible for tethering the enzyme to the cytosolic face of the endoplasmic reticulum
brenda
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
metabolism
physiological function
the catalytic domain performs the head-to-head dimerization of two molecules of farnesyl diphosphate to form squalene, a 30 carbon isoprenoid oxidized by squalene monooxygenase (Erg1) and cyclized by lanosterol synthase
additional information
metabolism
squalene synthase catalyzes the first committed step in sterol biosynthesis, role of squalene synthase in the ergosterol biosynthetic pathway of budding yeast, overview
metabolism
squalene synthase catalyzes the first step of sterol/hopanoid biosynthesis in the organism
additional information
the hinge domain plays an essential functional role, such as assembly of ergosterol multi-enzymecomplexes in fungi
additional information
-
the hinge domain plays an essential functional role, such as assembly of ergosterol multi-enzymecomplexes in fungi
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). SQS1_YEAST
Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
767
0
86950
Swiss-Prot
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
squalene synthase consists of both an N-terminal catalytic domain and a C-terminal domain tethering the enzyme to the endoplasmic reticulum membrane
additional information
-
squalene synthase consists of both an N-terminal catalytic domain and a C-terminal domain tethering the enzyme to the endoplasmic reticulum membrane
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
construction of a mutant containing three synonymous mutations G1125A, T1128C, T1176C and one nonsynonymous mutation G856A, which corresponds to Gly286Ser exchange, by gene replacement. Various mutations clustered around the residues that are important for NADPH binding effectively convert SQS into a dehydrosqualene synthase, overview
additional information
-
construction of a mutant containing three synonymous mutations G1125A, T1128C, T1176C and one nonsynonymous mutation G856A, which corresponds to Gly286Ser exchange, by gene replacement. Various mutations clustered around the residues that are important for NADPH binding effectively convert SQS into a dehydrosqualene synthase, overview
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
gene erg9, recombinant expression in enzyme-deficient SQS-knockout Saccharomyces cerevisiae DELTAerg9 strain, the endogenous enzyme partially complements the knockout mutation, restoration of the complete complementation phenotype is mapped to a 26-amino acid hinge region linking the catalytic and membrane-spanning domains specific to fungal squalene synthases
gene ysqs, recombinant expression of wild-type and endgineered enzymes in Escherichia coli strain XL1-Blue, coexpression with gene crtN encoding DSQ desaturase from Staphylococcus aureus in Escherichia coli results in carotinoid production and accumulation of C30 carotenoid pigments, which does not happen with coexpression of gene crtI encoding Pantoea ananatis phytoene desaturase, carotenoid pigment analysis, overview
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Linscott, K.B.; Niehaus, T.D.; Zhuang, X.; Bell, S.A.; Chappell, J.
Mapping a kingdom-specific functional domain of squalene synthase
Biochim. Biophys. Acta
1861
1049-1057
2016
Arabidopsis thaliana, Homo sapiens (P37268), Saccharomyces cerevisiae (P53866), Saccharomyces cerevisiae, Botryococcus braunii (Q9SDW9)
brenda
Furubayashi, M.; Li, L.; Katabami, A.; Saito, K.; Umeno, D.
Directed evolution of squalene synthase for dehydrosqualene biosynthesis
FEBS Lett.
588
3375-3381
2014
Thermosynechococcus vestitus, Homo sapiens (P37268), Homo sapiens, Saccharomyces cerevisiae (P53866), Saccharomyces cerevisiae
brenda
EXTERNAL LINKS (specific for EC-Number 2.5.1.21)
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
About BRENDA
Social media
Help
Survey
Download
Contribution
Legal
Curated at
Member of
