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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...

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Identifiers

PMID: 12825924
DOI: 10.1021/jm034057i

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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