Multiple folate enzyme inhibition: mechanism of a novel pyrrolopyrimidine-based antifolate LY231514 (MTA)

Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays

1983 • 52,849 citations

LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes.

1997 • 560 citations

Polyglutamation of methotrexate. Is methotrexate a prodrug?

1985 • 460 citations

ICI D1694, a quinazoline antifolate thymidylate synthase inhibitor that is a potent inhibitor of L1210 tumor cell growth in vitro and in vivo: a new agent for clinical study.

1991 • 360 citations

Enhanced inhibition of thymidylate synthase by methotrexate polyglutamates.

1985 • 330 citations

Folylpolyglutamate Synthesis and Role in the Regulation of One-Carbon Metabolism

1989 • 320 citations

Inhibition of phosphoribosylaminoimidazolecarboxamide transformylase by methotrexate and dihydrofolic acid polyglutamates.

1985 • 312 citations

A rapid and sensitive high pressure liquid chromatography assay for deoxyribonucleoside triphosphates in cell extracts

1979 • 272 citations

A dideazatetrahydrofolate analog lacking a chiral center at C-6: N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5yl)ethyl[benzoyl]-L-glutamic acid is an inhibitor of thymidylate synthase

1992 • 254 citations

A new folate antimetabolite, 5,10-dideaza-5,6,7,8-tetrahydrofolate is a potent inhibitor of de novo purine synthesis

1989 • 234 citations

Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin

1985 • 150 citations

Evidence for the cytotoxic activity of polyglutamate derivatives of methotrexate.

1980 • 147 citations

Production and characterization of monoclonal antibodies that localize human thymidylate synthase in the cytoplasm of human cells and tissue.

1991 • 123 citations

Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase.

1993 • 112 citations

The Human purH Gene Product, 5-Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase/IMP Cyclohydrolase

1996 • 91 citations

Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications

1991 • 78 citations

Evaluation of ascorbic acid in protecting labile folic acid derivatives.

1983 • 75 citations

Mammalian folylpoly-.gamma.-glutamate synthetase. 1. Purification and general properties of the hog liver enzyme

1987 • 69 citations

Mammalian folylpoly-.gamma.-glutamate synthetase. 4. In vitro and in vivo metabolism of folates and analogues and regulation of folate homeostasis

1987 • 68 citations

Substrate specificity of mammalian folylpolyglutamate synthetase for 5,10-dideazatetrahydrofolate analogs.

1995 • 67 citations

Mammalian folyl polyglutamate synthetase: partial purification and properties of the mouse liver enzyme

1984 • 63 citations

A novel class of monoglutamated antifolates exhibits tight-binding inhibition of human glycinamide ribonucleotide formyltransferase and potent activity against solid tumors.

1994 • 60 citations

Phase I trial and clinical pharmacological evaluation of 10-ethyl-10-deazaaminopterin in adult patients with advanced cancer.

1988 • 56 citations

Resistance to Tomudex (ZD1694): Multifactorial in human breast and colon carcinoma cell lines

1996 • 52 citations

Activity of the new antifolate N10-propargyl-5,8-dideazafolate and its polyglutamates against human dihydrofolate reductase, human thymidylate synthetase, and KB cells containing different levels of dihydrofolate reductase.

1985 • 36 citations

Measurement of folylpolyglutamate synthetase activity in head and neck squamous carcinoma cell lines and clinical samples using a new rapid separation procedure.

1992 • 29 citations

Quinazoline antifolates inhibiting thymidylate synthase: synthesis of four oligo(L-.gamma.-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition

1989 • 26 citations

ICI D1694, An Inhibitor of Thymidylate Synthase for Clinical Study

1991 • 25 citations

Influence of exogenous ras and p53 on P-glycoprotein function in immortalized rodent fibroblasts.

1995 • 18 citations

Phase II trials of trimetrexate in advanced adult soft tissue sarcoma

1991 • 16 citations

5,10-Dideazatetrahydrofolic acid reduces toxicity and deoxyadenosine triphosphate pool expansion in cultured L1210 cells treated with inhibitors of thymidylate synthase

1995 • 15 citations

34 Phase II study of LY231514 in patients with advanced non-small cell lung cancer (NSCLC)

1997 • 14 citations

Single step LC method for determination of folypolyglutamate synthetase activity and separation of polyglutamates

1993 • 10 citations