|
A dihydrofolate reductase inhibitor (DHFR inhibitor) is a molecule that inhibits the function of dihydrofolate reductase, and is a type of antifolate. Since folate is needed by rapidly dividing cells to make thymine, this effect may be used to therapeutic advantage. For example, methotrexate is used as cancer chemotherapy because it can prevent neoplastic cells from dividing. Bacteria also need DHFR to grow and multiply and hence inhibitors selective for bacterial vs. host DHFR have found application as antibacterial agents. Classes of small-molecules employed as inhibitors of dihydrofolate reductase include diaminoquinazoline & diaminopyrroloquinazoline, diaminopyrimidine, diaminopteridine and diaminotriazines. The examples provided below are specific molecules belonging to one of the above mentioned classes. A variety of drugs act as inhibitors of dihydrofolate reductase: * the antibiotic trimethoprim and its derivatives brodimoprim, tetroxoprim, and iclaprim. * the antimalarial drugs pyrimethamine and proguanil. * the experimental new antimalarial drug JPC-2056, which may also be more effective and better tolerated than current treatments against toxoplasmosis.〔 〕 * the chemotherapeutic agents methotrexate and pemetrexed. Methotrexate acts on this enzyme binding to it some 1000 times more tightly than folate itself. ==References== 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Dihydrofolate reductase inhibitor」の詳細全文を読む スポンサード リンク
|