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Search term: drug development

Results 1 - 100 of 1025 > >>
EC Number
Application
Commentary
aldehyde reductase
drug development
the enzyme is a target for inhibitor design, enzyme inhibition has considerable potential for the treatment of diabetes, without increased risk of hypoglycemia
aldehyde reductase
drug development
homochiral 3-hydroxy-4-substituted beta-lactams serve as precursors to the corresponding alpah-hydroxy-beta-amino acids, the enzyme might be useful insynthesis of these key components of many biologically and therapeutically important compounds
aldehyde reductase
drug development
the enzyme may be a potential drug target or vaccine candidate for schistosomes
aldehyde reductase
drug development
development of reductase inhibitors as drugs counteracting the onset of diabetic complications
histidinol dehydrogenase
drug development
histidinol dehydrogenase is a suitable target for not only for Geotrichum candidum but also for related species, wherby compounds identified can serve as a valuable lead for development of novel non-classical antifungal therapy, notably against strain like Candida rapidly becoming resistant to conventional therapy
shikimate dehydrogenase
drug development
the enzyme can be a target for rational design of specific inhibitors, aiming at the development of antitubercular drugs
L-lactate dehydrogenase
drug development
a selective lactate dehydrogenase inhibitor targeting the L-malate dehydrogenase function of Plasmodium falciparum and its corresponding tricarboxylic acid cycle provides an attractive therapeutic opportunity, in contrast to LDH targeting due to the functional similarity between human and parasite LDHs
L-lactate dehydrogenase
drug development
parasite LDH is a target for antimalarial compounds owing to structural and functional differences from the human isozymes
L-lactate dehydrogenase
drug development
LDH is a potential drug target and candidate antigen for immunodiagnosis (LDH can be recognized in serum from swine or patient infected with Taenia asiatica) and vaccine for taeniasis and viscero-cysticercosis caused by Taenia asiatica
L-lactate dehydrogenase
drug development
Sa-LDH-1 can become a potential drug target for antibiotics against Staphylococcus aureus
L-lactate dehydrogenase
drug development
the parasite enzyme is a potential target for antimalarial drugs
L-lactate dehydrogenase
drug development
LDH is critically implicated in tumor growth and therefore considered to be an important target protein for antitumor metal complexes
hydroxymethylglutaryl-CoA reductase (NADPH)
drug development
inhibitors of HMG-CoA reductase for reducing low density lipoprotein cholesterol in the treatment of hypercholesterolemia
hydroxymethylglutaryl-CoA reductase (NADPH)
drug development
a yeast expression system can serve to study the influence of selected mutations in human HMG-CoA reductase on the sensitivity of the enzyme to commonly prescribed statins, thus this model system is suitable for the development and selection of lipid-lowering drugs as well as for the examination of DNA sequence variations in the context of statin therapy
hydroxymethylglutaryl-CoA reductase (NADPH)
drug development
overexpression of HMGR appears promising for obtaining a constant high production of artemisinin, an effective drug against malaria for which no resistant strains of Plasmodium falciparum have been reported
malate dehydrogenase
drug development
mitochondrial malate dehydrogenase is a biological target for antiproliferative activity
11beta-hydroxysteroid dehydrogenase (NAD+)
drug development
the enzyme is a target for inhibitor design and development; the enzyme is a target for inhibitor design and development
glucose-6-phosphate dehydrogenase (NADP+)
drug development
the enzyme is a target for anti-parasite drug development
glucose-6-phosphate dehydrogenase (NADP+)
drug development
Trypanosoma brucei G6PDH is a valid drug target for human steroids. Inhibition of G6PDH by dehydroepiandrosterone derivatives may lead to the development of a new class of anti-trypanosomatid compounds
3alpha-hydroxysteroid 3-dehydrogenase (Si-specific)
drug development
the enzyme is a target for treatment of chronic pain in neuropathic diseases, overview
17beta-estradiol 17-dehydrogenase
drug development
several 17beta-HSD isozymes are targets for drug development with importance in cancer, metabolic diseases, neurodegeneration and possibly immunity
ketol-acid reductoisomerase (NADP+)
drug development
the enzyme is a target for herbicide drug development, computer-aided drug design
ketol-acid reductoisomerase (NADP+)
drug development
the enzyme is a promising target for the design of herbicides
3-oxoacyl-[acyl-carrier-protein] reductase
drug development
the enzyme has no isoforms and thus is a good target for inhibitor design
3-oxoacyl-[acyl-carrier-protein] reductase
drug development
FabG is the antibacteria target of maple leaf extracts and tannic acid, and both reversible and irreversible inhibitions of FabG are important for the antibacterial effect
3-oxoacyl-[acyl-carrier-protein] reductase
drug development
galangal extract inhibits FabG, thereby displaying antibacterial ability
11beta-hydroxysteroid dehydrogenase
drug development
isozyme 11beta-HSD1 is a target in treatment of metabolic diseases such as diabetes mellitus type 2 or obesity
11beta-hydroxysteroid dehydrogenase
drug development
11beta-HSD1 will significantly contribute to the biotransformation of oracin in humans. The microsomal carbonyl reductase has a great potential to significantly impair the chemotherapy with the anticancer drug oracin
carbonyl reductase (NADPH)
drug development
CBR1 inhibition can improve the therapeutic response to doxorubicin and reduce its side effects
carbonyl reductase (NADPH)
drug development
the cardioprotectant 7-monohydroxyethylrutoside inhibits CBR1 activity. CBR1 V88I genotype status and the type of anthracycline substrate dictate the inhibition of CBR1 activity. Inhibition of CBR1 activity shall be considered during the development of novel cardioprotectants against anthracycline-related cardiotoxicity
IMP dehydrogenase
drug development
the enzyme is a target in enzyme-pattern-targeted chemotherapy in acuet leukemia, AML, treatment
IMP dehydrogenase
drug development
the enzyme is a target in parasite treatment and elimination
IMP dehydrogenase
drug development
the enzyme is a potential therapeutic target, and the NAD+ site may be an exploitable target for the design of antimicrobial drugs
IMP dehydrogenase
drug development
the enzyme is a target for drug development in treatment of structural schizophrenia
IMP dehydrogenase
drug development
the IMPDH-1 is an antiangiogenic drug target
IMP dehydrogenase
drug development
the enzyme is a target for therapeutic drugs
IMP dehydrogenase
drug development
IMPDH2 is the major target for cancer chemotherapy
IMP dehydrogenase
drug development
at therapeutic concentrations in organ transplant patients, the effect of mycophenolic acid-acyl-glucuronide on IMPDHII activity is minimal compared to mycophenolic acid, and the quantification of mycophenolic acid metabolites for mycophenolate therapeutic drug monitoring and dose adjustment will be of no benefit
IMP dehydrogenase
drug development
1,2,3-triazole IMPDH inhibitors provide new tools for elucidating the role of IMPDH in Cryptosporidium parvum and may serve as potential therapeutics for treating cryptosporidiosis
IMP dehydrogenase
drug development
type I IMPDH is identified as an antiangiogenic drug target. Inhibition may cause endothelial cell cycle arrest
IMP dehydrogenase
drug development
differences between the human and Mycobacterium tuberculosis IMPDHs in the region of binding of nucleotide inhibitors on the inosine 5'-phosphate binding site. These and other differences, may be exploited for the design of new inhibitors with selectivity against Mycobacterium tuberculosis IMPDH
IMP dehydrogenase
drug development
Roche total mycophenolic acid assay (a new inosine monophosphate dehydrogenase inhibition assay) is a promising alternative for mycophenolic acid quantification where chromatographic methods are not available
3alpha-hydroxysteroid 3-dehydrogenase (Re-specific)
drug development
the enzyme is a target for treatment of chronic pain in neuropathic diseases, overview
3alpha-hydroxysteroid 3-dehydrogenase (Re-specific)
drug development
2'-hydroxyflavanone may be useful for clinical therapy of malignancies where AKR1C3 is overexpressed like in prostate and breast cancer
tetrahydroxynaphthalene reductase
drug development
the enzyme represents a target for the development of fungicides and antimicotics
tetrahydroxynaphthalene reductase
drug development
flavonoids inhibit 3HNR, which can thus be considered a potential target for flavonoid action. In addition to being a known target for different fungicides, 3HNR can also serve as an interesting and novel target for the development of antimycotics
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
the enzyme is a target for antibacterial agents and inhibitor design
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
the enzyme is a potential target for antimalarial drug development and chemotherapy
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
Escherichia coli Dxr represents a valuable model enzyme for the screening for new antimalarial compounds, since work with the Plasmodium falciparum Dxr is associated with considerably high effort due to the instability of this enzyme and the low yield of the available recombinant expression system, no major differences in the IC50 between Escherichia coli Dxr and Plasmodium falciparum Dxr
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
1-deoxy-D-xylulose-5-phosphate reductoisomerase in the nonmevalonate isoprene biosynthesis pathway is a target for developing antimalarial drugs
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
because the enzyme is absent in humans, DXR is a target for drug discovery
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
the enzyme is a target for the design of antimalarial drugs
1-deoxy-D-xylulose-5-phosphate reductoisomerase
drug development
the enzyme is an excellent drug target in a number of pathogenic organisms
(S)-2-hydroxy-acid oxidase
drug development
in humans the enzyme is a potential drug target for treatment of primary hyperoxaluria, a genetic disorder where overproduction of oxalate results in the formation of kidney stones
(S)-2-hydroxy-acid oxidase
drug development
isozyme Hao2 is a target for drug development in high blood pressure
aspartate-semialdehyde dehydrogenase
drug development
ASADH is a target for the development of novel antibiotics, especially for Gram-negative bacteria that require diaminopimelate for cell-wall biosynthesis
long-chain acyl-[acyl-carrier-protein] reductase
drug development
since the giant CpFAS1 and polyketide synthase CpPKS1 are structurally and functionally different from human Type I FAS, these parasite megasynthases may serve as novel drug targets, also because CpFAS1 and CpPKS1 utilize R domains to release final products
dihydropyrimidine dehydrogenase (NADP+)
drug development
the enzyme is an adjunct target in cancer therapy since it rapidly breaks down the anti-cancer drug 5-fluorouracil and related compounds
fumarate reductase (NADH)
drug development
lack of NADH-fumarate reductase in mammalian cells provides an interesting target against Chagas disease
enoyl-[acyl-carrier-protein] reductase (NADH)
drug development
InhA is an attractive target for the development of drugs against tuberculosis
enoyl-[acyl-carrier-protein] reductase (NADH)
drug development
the bacterial enoyl-ACP reductase is a target for antibacterial drug development
enoyl-[acyl-carrier-protein] reductase (NADPH, Si-specific)
drug development
the bacterial enoyl-ACP reductase is a target for antibacterial drug development
protoporphyrinogen oxidase
drug development
protoporphyrinogen oxidase is one of the most important action targets of commercial herbicides
dihydroorotate dehydrogenase (quinone)
drug development
DHODH represents a potential target for anti-malarial therapy
D-aspartate oxidase
drug development
a DDO inhibitor that augments brain D-Asp levels can be a potent antipsychotic drug for the treatment of NMDA receptor-related disease
L-amino-acid oxidase
drug development
purified LAAO-I exhibits antiprotozoal activities which are demonstrated to be hydrogen-peroxide mediated. Exposure of promastigotes of Leishmania sp. results in dose-dependent parasite killing. LAAOs are interesting multifunctional enzymes, not only for a better understanding of the ophidian envenomation mechanism, but also due to their biotechnological potential as model for therapeutic agents
L-amino-acid oxidase
drug development
ACTX-6 demonstrates cytotoxicity in vitro and can inhibit tumor growth in vivo. It can markedly increase accumulation of sub-G1 phase, which suggests that this enzyme can induce apoptosis. ACTX-6 is a potential substance to develop into an antitumor drug
D-amino-acid oxidase
drug development
the enzyme is a drug target in schizophrenia
D-amino-acid oxidase
drug development
the enzyme is a potential therapeutic target for schizophrenia treatment
D-amino-acid oxidase
drug development
the enzyme is a target in schizophrenia treatment
monoamine oxidase
drug development
MAO-A is a target for a series of therapeutically valuable drugs. Thus, selective MAO-A inhibitors are used as antidepressants; MAO-B is a target for a series of therapeutically valuable drugs. Thus, selective MAO-B inhibitors are used in the treatment of Parkinson’s disease
monoamine oxidase
drug development
dual-target-directed drugs, compounds that inhibit MAO-B and antagonize A2A receptors, may have value in the management of Parkinson's disease, overview
monoamine oxidase
drug development
indole and benzofuran derivatives are promising reversible MAO-B inhibitors with a possible role in the treatment of neurodegenerative diseases such as Parkinson’s disease
dihydrofolate reductase
drug development
enzyme is identical to enzyme from Bacillus cereus. Use of enzyme from Bacillus cereus as antimicrobial target for Bacillus anthracis, homology modelling of inhibitors and growth inhibition assays
dihydrofolate reductase
drug development
enzyme is identical to enzyme from Bacillus anthracis. Use of enzyme as antimicrobial target for Bacillus anthracis, homology modelling of inhibitors and growth inhibition assays
dihydrofolate reductase
drug development
comparison of Danio rerio and human enzyme to evaluate the suitability of the fish enzyme as an assay system for antifolate drug discovery. Structural and kinetic proterties of both enzymes are similar and susceptibilities to known inhibitors are also comparable
dihydrofolate reductase
drug development
comparison of Danio rerio and human enzyme to evaluate the suitability of the fish enzyme as an assay system for antifolate drug discovery. Structural and kinetic proterties of both enzymes are similar and susceptibilites to known inhibitors are also comparable
dihydrofolate reductase
drug development
use of multiple protein structure technique for structure-based drug discovery. Construction of receptor-based pharmacophores using multiple X-ray crystallographic structures. Models incorporate a fair degree of protein flexibility and are highly selective for known inhibitors over drug-like non-inhibitors
dihydrofolate reductase
drug development
receptor-based pharmacophore models based on ensembles of protein conformations from molecular dynamics simulations of enzyme in complex with NADPH in both the closed and open conformation of the M20 loop. Optimal models identify enzyme inhibitors over druglike noninhibitors. Model performance improves with increased dynamic sampling
dihydrofolate reductase
drug development
modeling of 32 pyrimethamine derivatives into the active site of dihydrofolate reductase obtained from crystal structure 1J3K.pdb. Evaluation of predicted binding modes and key protein-ligand interactions
dihydrofolate reductase
drug development
expression of bifunctional dihydrofolate reductase-thymidylate synthase in plasmodium falciparum to assess interaction with antifolates
dihydrofolate reductase
drug development
modeling of 31 pyrimethamine derivatives into the active site of dihydrofolate reductase obtained from crystal structures 1J3I.pdb and 1J3K.pdb. Evaluation of predicted binding modes and key protein-ligand interactions
dihydrofolate reductase
drug development
the essential enzyme is a target for development of specific inhibitors for treatment of the causative agent in AIDS pneumonia
dihydrofolate reductase
drug development
the essential enzyme is a target for development of specific inhibitors for treatment of the biodefense organism Bacillus anthracis
dihydrofolate reductase
drug development
the enzyme is a target for inhibitor design, overview
dihydrofolate reductase
drug development
the essential enzyme is a target for development of specific inhibitors
dihydrofolate reductase
drug development
the enzyme is a target for antifolate drugs. The parasite develops resistance to several used antifolates via mutations in the active site, e.g. point mutations of residues Ala16, Ile51, Cys59, Ser108 and Ile164, overview
dihydrofolate reductase
drug development
the enzyme is a target for drug development since the organism causes the opportunistic infection Pneumocystis pneumonia, a major cause of mortality in acquired immunodeficiency syndrome, AIDS, patients
dihydrofolate reductase
drug development
the enzyme is a target for drug development since the organism causes the opportunistic infection toxoplasmosis, a major cause of mortality in acquired immunodeficiency syndrome, AIDS, patients
dihydrofolate reductase
drug development
the enzyme is a possible target for treatment of cryptosporidiosis caused by the organism
dihydrofolate reductase
drug development
DHFR is a valid drug target
dihydrofolate reductase
drug development
mtDHFR is an attractive target for the development of anti-tuberculosis drugs
pteridine reductase
drug development
target for antifolate chemotherapy against Leishmania
pteridine reductase
drug development
target for antiparasite drug development
cytochrome-b5 reductase
drug development
flavonoids, regarding b5 reductase inhibition, indicate a potential for significant flavonoid–drug and/or flavonoid–xenobiotic interactions which may have important therapeutic and toxicological outcomes for certain drugs and/or xenobiotics.
NAD(P)H dehydrogenase (quinone)
drug development
NAD(P)H:quinone oxidoreductase is a major detoxifying enzyme for 7,12-dimethylbenz[a]anthracene. Eugenol has a potent protective effect against 7,12-dimethylbenz[a]anthracene-induced genotoxicity, presumably through the suppression of the 7,12-dimethylbenz[a]anthracene activation and the induction of its detoxification through NAD(P)H:quinone oxidoreductase
NAD(P)H dehydrogenase (quinone)
drug development
design of novel lavendamycin analogues with enhanced, selective, and potent antitumor activity
NAD(P)H dehydrogenase (quinone)
drug development
ability of ketoconazole and itraconazole to induce NQO1 gene expression at the transcriptional level through an aryl hydrocarbon receptor-dependent mechanism
NAD(P)H dehydrogenase (quinone)
drug development
greater induction activities of the phase II enzyme quinone reductase associated with stilbenoids serve as a useful starting point for the design of improved chemopreventive agents
NAD(P)H dehydrogenase (quinone)
drug development
in vitro, almond skin polyphenols act as antioxidants and induce quinone reductase activity, but these actions are dependent upon their dose, method of extraction, and interaction with antioxidant vitamins
Results 1 - 100 of 1025 > >>