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High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate.

Abstract：

:This communication describes the high-throughput screen of a diverse library of 50,000 small molecules against Escherichia coli dihydrofolate reductase to detect inhibitors. Sixty-two compounds were identified as having significant inhibitory activity against the enzyme. Secondary screening of these revealed twelve molecules that were competitive with dihydrofolate, nine of which have not been previously characterized as inhibitors of dihydrofolate reductase. These novel molecules ranged in potency (K(i)) from 26 nM to 11 microM and may represent fresh starting points for new small molecule therapeutics directed against dihydrofolate reductase.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zolli-Juran M,Cechetto JD,Hartlen R,Daigle DM,Brown ED

doi

10.1016/s0960-894x(03)00480-3

subject

Has Abstract

pub_date

2003-08-04 00:00:00

pages

2493-6

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960894X03004803

journal_volume

13

pub_type

杂志文章

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