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STRUCTURES OF APO AND COMPLEXED ESCHERICHIA-COLI GLYCINAMIDE RIBONUCLEOTIDE TRANSFORMYLASE
被引:111
|作者:
ALMASSY, RJ
JANSON, CA
KAN, CC
HOSTOMSKA, Z
机构:
[1] Agouron Pharmaceuticals, San Diego, CA 92121
来源:
关键词:
D O I:
10.1073/pnas.89.13.6114
中图分类号:
O [数理科学和化学];
P [天文学、地球科学];
Q [生物科学];
N [自然科学总论];
学科分类号:
07 ;
0710 ;
09 ;
摘要:
The three-dimensional structure of phosphoribosylglycinamide formyltransferase (10-formyltetrahydrofolate:5'-phosphoribosylglycinamide formyltransferase, EC 2.1.2.2) has been solved both as an apoenzyme at 2.8-angstrom resolution and as a ternary complex with the substrate glycinamide ribonucleotide and a folate inhibitor at 2.5-angstrom 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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页码:6114 / 6118
页数:5
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