Titlebook: Antifolate Drugs in Cancer Therapy; Ann L. Jackman Book 1999 Springer Science+Business Media New York 1999 biochemistry.cancer.cancer ther

蚊子

Tomudex,er drug that owes its cytotoxicity to inhibition of the enzyme thymidylate synthase (TS). TS catalyzes the reductive methylation of deoxyuridylate monophosphate (dUMP) to thymidylate (TMP), the rate-limiting step in the . synthesis of thymidine triphosphate (TTP), the only nucleotide specific for DN

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Preclinical Pharmacology Studies and the Clinical Development of a Novel Multitargeted Antifolate, agents for the management of neoplastic diseases. However, it was only in the last 10–15 yr, because of the rapid advances of medicinal chemistry, X-ray protein crystallography, molecular biology, pharmacology, and clinical medicine, that a significant number of new generation antifolates were brou

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GW1843,te moieties in vivo. However, unlike some other TS inhibitors and other antifolates, the TS inhibition constant and noncompetitive mode of inhibition is unaffected by polyglutamation. The compound is readily transported on the reduced folate carrier, and accumulates in cells. The main cellular metab

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Preclinical and Clinical Studies with the Novel Thymidylate Synthase Inhibitor Nolatrexed Dihydrochriority to evaluate drugs that may possess either greater efficacy or activity in tumors with intrinsic or acquired resistance to established treatment. Nolatrexed dihydrochloride (Thymitaq.) is a novel folate-based inhibitor of thymidylate synthase (TS). TS is the rate-limiting enzyme in the . bios

臆斷

ZD9331,nce DNA synthesis, has been achieved with a range of quinazoline analogs of folic acid, including CB3717 (.–.) and its non-nephrotoxic successor, Tomudex. (ZD1694, raltitrexed) (.–.). The latter compound has recently been introduced in a number of counties for the treatment of advanced colorectal ca

catagen

Preclinical and Clinical Evaluation of the Glycinamide Ribonucleotide Formyltransferase Inhibitors ycinamide ribonucleotide formyltransferase (GARFT), the first folate-dependent enzyme in this pathway, might have utility in the treatment of cancer. In 1987, clinical investigations were initiated with lometrexol (6R-dideazatetrahydrofolic acid, 6R-DDATHF), a novel “tight-binding” inhibitor of GARF

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Folates as Chemotherapeutic Modulators,in hematopoietic cells and intestinal mucosa, with lesser effects on kidney, liver, and the central nervous system (.). An accepted strategy to overcome these toxicities is the supplementation of folates as rescue agents (.–.). In this context, the use of high doses of methotrexate (MTX) with leucov

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