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Article

Dihydrofolate reductase mutant with exceptional resistance to methotrexate but not to trimetrexate.

Journal of medicinal chemistry - 3 Jul 2003

Pineda Pamela, Kanter Aaron, McIvor R Scott, Benkovic Stephen J, Rosowsky Andre, Wagner Carston R

Abstract excerpt

Two double (F31A/F34A, I60A/L67G) and one quadruple (F31A/F34A/I60A/L67G) mutant murine dihydrofolate reductases were constructed and evaluated for their ability to impart antifolate resistance. Both I60A/L67G and F31A/F34A/I60A/L67G were found to be unstable and devoid of catalytic activity. The K(i) values for F31A/F34A, methotrexate (MTX), bis-MTX, and PT-523 were found to be 10100-, 4410-, and 617-fold higher...

Topics

Antineoplastic Agents
Drug Resistance, Neoplasm
Folic Acid Antagonists
Kinetics
Methotrexate
Mutation
Recombinant Proteins
Tetrahydrofolate Dehydrogenase
Trimetrexate

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Source

Identifiers

PMID: 12825924
DOI: 10.1021/jm034057i

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