| Literature DB >> 16734442 |
Erika A Taylor Ringia1, Peter C Tyler, Gary B Evans, Richard H Furneaux, Andrew S Murkin, Vern L Schramm.
Abstract
Transition state analogues of PNP, the Immucillins and DADMe-Immucillins, were designed to match transition state features of bovine and human PNPs, respectively. The inhibitors with or without the hydroxyl and hydroxymethyl groups of the substrate demonstrate that inhibitor geometry mimicking that of the transition state confers binding affinity discrimination. This finding is remarkable since crystallographic analysis indicates complete conservation of active site residues and contacts to ligands in human and bovine PNPs.Entities:
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Year: 2006 PMID： 16734442 PMCID： PMC2518100 DOI： 10.1021/ja061403n
Source DB: PubMed Journal: J Am Chem Soc ISSN： 0002-7863 Impact factor: 15.419