Dihydrofolate reductase

Description:

Description
  • Accession: P00374
  • Swissprot: DYR_HUMAN
  • Organism: Homo sapiens
  • Gene: DHFR
  • Target class: Enzyme

Drug Relations:

edatrexate
Bioactivity details MOA
methotrexate
An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA. Bioactivity details MOA
pemetrexed
Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication. In vitro studies show that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT. Bioactivity details MOA
pralatrexate
Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase. It is also a competitive inhibitor for polyglutamylation by the enzyme folylpolyglutamyl synthetase. This inhibition results in the depletion of thymidine and other biological molecules the synthesis of which depends on single carbon transfer. Bioactivity details MOA
aminopterin
A folic acid derivative used as a rodenticide that has been shown to be teratogenic. Bioactivity details MOA
cycloguanil
was MH 1975-92 (see under TRIAZINES 1975-90); use CYCLOGUANIL EMBONATE was see CYCLOGUANIL PAMOATE 1975-92; TRIAZINES to search CYCLOGUANIL PAMOATE 1975-92; metabolite of chloroguanide Bioactivity details MOA
gentamicin
A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS. Bioactivity details MOA
iclaprim
has antiviral activity Bioactivity details MOA
leucovorin
The active metabolite of FOLIC ACID. Leucovorin is used principally as an antidote to FOLIC ACID ANTAGONISTS. Bioactivity details MOA
pyrimethamine
One of the FOLIC ACID ANTAGONISTS that is used as an antimalarial or with a sulfonamide to treat toxoplasmosis. Bioactivity details MOA
raltitrexed
Bioactivity details MOA
sulfacetamide
An anti-infective agent that is used topically to treat skin infections and orally for urinary tract infections. Bioactivity details MOA
trimethoprim
A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported. Bioactivity details MOA
trimetrexate
A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect. Bioactivity details MOA