2.1.1.45: thymidylate synthase
This is an abbreviated version!
For detailed information about thymidylate synthase, go to the full flat file.
Word Map on EC 2.1.1.45
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2.1.1.45
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5-fluorouracil
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thymidine
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colorectal
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dihydrofolate
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antifolate
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methotrexate
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dihydropyrimidine
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pyrimidine
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fluoropyrimidine
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phosphorylase
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ribonucleotide
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leucovorin
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pemetrexed
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resect
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fdump
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uracil
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mthfr
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casey
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schedule
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polyglutamates
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non-small
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cisplatin
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folylpolyglutamate
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deoxyuridine
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oxaliplatin
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5-fluoro-2'-deoxyuridine
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antimetabolite
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orotate
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irinotecan
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capecitabine
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5-fu-based
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ccrf-cem
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folate-dependent
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gemcitabine
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folinic
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formyltransferase
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quinazoline
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glycinamide
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dttp
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polyglutamylation
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2'-deoxyuridine
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tegafur
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medicine
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methotrexate-resistant
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deoxycytidylate
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cross-complementing
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drug development
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transformylase
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5-fu-induced
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dutpase
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aminopterin
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deoxythymidine
- 2.1.1.45
- 5-fluorouracil
- thymidine
- colorectal
- dihydrofolate
- antifolate
- methotrexate
- dihydropyrimidine
- pyrimidine
-
fluoropyrimidine
- phosphorylase
- ribonucleotide
- leucovorin
- pemetrexed
-
resect
- fdump
- uracil
- mthfr
-
casey
-
schedule
- polyglutamates
-
non-small
- cisplatin
- folylpolyglutamate
- deoxyuridine
- oxaliplatin
- 5-fluoro-2'-deoxyuridine
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antimetabolite
- orotate
- irinotecan
- capecitabine
-
5-fu-based
-
ccrf-cem
-
folate-dependent
- gemcitabine
-
folinic
-
formyltransferase
- quinazoline
- glycinamide
- dttp
-
polyglutamylation
- 2'-deoxyuridine
-
tegafur
- medicine
-
methotrexate-resistant
- deoxycytidylate
-
cross-complementing
- drug development
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transformylase
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5-fu-induced
- dutpase
- aminopterin
- deoxythymidine
Reaction
Synonyms
BgDHFR-TS, bifunctional TS-DHFR, DFR-TS, DHFR-TS, DHFR–TS, dihydrofolate reductase-thymidylate synthase, dTMP synthase, HTS, human TS, LBRM_06_0830, methylenetetrahydrofolate:dUMP C-methyltransferase, More, Thy1, ThyA, thymidylate synthase, thymidylate synthase A, thymidylate synthase-dihydrofolate reductase, thymidylate synthetase, ThyX, TMP synthetase, TMPS, TS, TS-DHFR, TSase, TYMS, Y110A7A.4
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Application
Application on EC 2.1.1.45 - thymidylate synthase
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drug development
medicine
the enzyme is a target for drug development in the treatement of Human African trypanosomiasis (HAT), an infectious disease caused by two distinct subspecies of the protozoan parasite Trypanosoma brucei subsp. gambiense and Trypanosoma brucei subsp. rhodesiense
drug development
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the enzyme is a target for drug development in the treatement of Human African trypanosomiasis (HAT), an infectious disease caused by two distinct subspecies of the protozoan parasite Trypanosoma brucei subsp. gambiense and Trypanosoma brucei subsp. rhodesiense
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medicine
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important drug target, fungus causes opportunistic pneumonia infections in immune-compromised patients and is among the leading causes of death of AIDS patients, inhibitors selective for fungal TS over human TS will be greatly beneficial in combating this disease
medicine
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enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs
medicine
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enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs
medicine
Tequatrovirus T4
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enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs
medicine
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enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs
medicine
enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs
medicine
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human TS mutants have potential applications in gene therapy by protecting hematopoietic progenitors from TS inhibitor toxicity, drug-resistant variants can be used to decrease the myelosuppressive side effects of TS-directed anticancer agents or to select genetically modified cells in vivo, clincal trials introduce chemoprotecting genes into hematopoietic cells
medicine
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development of effective chemotherapy of the eosinophilic meningoencephalitis angiostrongylosis
medicine
drug development against cryptococcosis, a pulmonary subclinical infection, in immunocompromised individuals having diseases such as leukemia, lymphoma or AIDS the infection seminates to the central nervous system, the fourth most common opportunistic infection complicating AIDS
medicine
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development of antimalarial drugs, selective chemoptherapy directed at malarial TS, inhibitors of pyrimidine biosynthesis shall be considered for malaria chemotherapy
medicine
inhibition of human thymidylate synthase leads to apoptosis of rapidly dividing cells such as cancer cells, human thymidylate synthase is a target in the chemotherapy of colorectal cancer and some other neoplasms
medicine
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inhibition of thymidylate synthase and DHFR enzymes has found clinical utility as antitumor, antimicrobial and antiprotozoal agents
medicine
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inhibition of TS and DHFR enzymes has found clinical utility as antitumor, antimicrobial and antiprotozoal agent
medicine
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inhibition of TS and DHFR enzymes has found clinical utility as antitumor, antimicrobial and antiprotozoal agents
medicine
inhibition of TS and DHFR enzymes has found clinical utility as antitumor, antimicrobial and antiprotozoal agents
medicine
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inhibitors of thymidylate synthase are used in the treatment of advanced colorectal carcinoma
medicine
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Lovo 175X2 cells transfected with mutant tumor suppressor gene p53 are more resistant to 5-fluorouracil, nolatrexed, raltitrexed and pemetrexed in comparison with the wild-type p53 parental cells Lovo 92. Resistance is associated with an increase in thymidylate synthase protein expression and catalytic activity. Lovo li cells, characterized by functionally inactive p53, are 3-13fold more sensitive to nolatrexed, raltitrexed and pemetrexed, and have a lower thymidylate synthase mRNA, protein expression and catalytic activity than Lovo 92. Mutant p53 WiDr cells transfected with wt p53 are not significantly different from mutant p53 WiDr cells with respect to sensitivity to thymidylate synthase inhibitors or thymidylate synthase levels
medicine
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the combination of the oral fluorouracil S-1 and the epidermal growth factor receptor-tyrosine kinase inhibitor gefitinib in shows a synergistic antiproliferative effect in vitro in all non-small cell lung cancer cell lines tested. Gefitinib inhibits the expression of the transcription factor E2F-1, resulting in the down-regulation of thymidylate synthase at the mRNA and protein levels
medicine
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the use of the TS inhibitor RTX in the treatment of colorectal cancer has been approved in Europe, Canada, Australia and Japan
medicine
thymidylate synthase as a target for antitubercular drugs
medicine
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thymidylate synthase is an important target of several chemotherapeutic agents including 5-fluorouracil and raltitrexed
medicine
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treatment of patients with advanced colorectal carcinoma with liposomal inhibitor OSI-7904L, in combination with oxaliplatin. At the highest dose level of OSI-7904L 9 mg/m2, oxaliplatin 130 mg/m2, one of nine patients experienced dose-limiting toxicity of grade 3 oral mucositis with cycle 1 and five further patients required dose reductions. The toxicity profile of stomatitis, diarrhea, nausea, fatigue, sensory neuropathy and skin rash was consistent with that expected for a thymidylate synthase inhibitor/oxaliplatin combination regimen. High interpatient variability with no detectable interaction between OSI-7904L and oxaliplatin
medicine
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treatment with thymidylate synthase inhibitors BGC 945 and BGC 9331 results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels. BGC 9331 induces accumulation of [18F]-fluorothymidine in the intestine
medicine
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TYMS is the target enzyme of fluorouracil, an antimetabolite widely used in the treatment of colorectal, head-and-neck, breast cancers, pancreatic cancer and hepatocellular carcinoma
medicine
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octapeptide inhibitor LSCQLYQR and derivatives are expected to work in combination with more aggressive chemotherapeutic agents in cancer cells to improve the efficacy, fight platinum-induced drug resistance, and reduce the overall drug combination toxicities. The cellular half-life observed for the peptide suggests that more chemical changes should be performed for an acceptable in vivo pharmacokinetics
medicine
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drug development against cryptococcosis, a pulmonary subclinical infection, in immunocompromised individuals having diseases such as leukemia, lymphoma or AIDS the infection seminates to the central nervous system, the fourth most common opportunistic infection complicating AIDS
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