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Proc Natl Acad Sci U S A. 1992 Jul 1;89(13):6114-8.

Structures of apo and complexed Escherichia coli glycinamide ribonucleotide transformylase.

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  • 1Agouron Pharmaceuticals, San Diego, CA 92121.


The three-dimensional structure of phosphoribosylglycinamide formyltransferase (10-formyltetrahydrofolate:5'-phosphoribosylglycinamide formyltransferase, EC has been solved both as an apoenzyme at 2.8-A resolution and as a ternary complex with the substrate glycinamide ribonucleotide and a folate inhibitor at 2.5-A resolution. The structure is a modified doubly wound alpha/beta sheet with flexibility in the active site, including a disordered loop in the apo structure, which is ordered in the ternary complex structure. This enzyme is a target for anti-cancer therapy and now for structure-based drug design.

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