High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate.
Article Details
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Zolli-Juran M, Cechetto JD, Hartlen R, Daigle DM, Brown ED
High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate.
Bioorg Med Chem Lett. 2003 Aug 4;13(15):2493-6.
- PubMed ID
- 12852950 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Trimethoprim Dihydrofolate reductase IC 50 (nM) 18 N/A N/A Details Trimethoprim Dihydrofolate reductase IC 50 (nM) 37 N/A N/A Details Trimethoprim Dihydrofolate reductase Ki (nM) 3.8 N/A N/A Details