dihydrofolate reductase inhibitors

dihydrofolate reductase inhibitors

Drugs that block the action of DIHYDROFOLATE REDUCTASE. Some of the drugs that inhibit this enzyme can, as in the case of METHOTREXATE, be used as anticancer drugs. Some of them have little effect on the human enzyme but a strong effect on the dihydrofolate reductases of bacterial and other parasites. Trimetrexate (Neutrexin) is a case in point; it is active against Pneumocystis carinii .
References in periodicals archive ?
Hartman et al., "Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening," Journal of Medicinal Chemistry, vol.
One group (dihydrofolate reductase inhibitors) prevents folate from being converted into its active metabolites and includes trimethoprim (antibiotic), sulfasalazine (for ulcerative colitis) and methotrexate (chemotherapeutic).
Evolution of the bacterial dihydrofolate reductase inhibitors. J Antimicrob Chemother 1995;36:887-90.
One group of such agents is dihydrofolate reductase inhibitors, which block the conversion of folate to its more active metabolites.
Methods: We assessed exposure to folic acid antagonists that act as dihydrofolate reductase inhibitors and to certain antiepileptic drugs in 3,870 infants with cardiovascular defects, 1,962 infants with oral clefts, and 1,100 infants with urinary tract defects, and also in 8,387 control infants with malformations, the risk of which is not reduced after vitamin supplementation.