| Literature DB >> 31577901 |
Yuting Feng1, Jaeok Park1,2, Shi-Guang Li1, Rebecca Boutin1, Peter Viereck1, Matthew A Schilling2, Albert M Berghuis2, Youla S Tsantrizos1,2.
Abstract
Thienopyrimidine-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS), characterized by a chiral α-aminophosphonic acid moiety, were synthesized as enantiomerically enriched pairs, and their binding mode was investigated by X-ray crystallography. A general consensus in the binding orientation of all (R)- and (S)-enantiomers was revealed. This finding is a prerequisite for establishing a reliable structure-activity relationship (SAR) model.Entities:
Mesh：
Substances：
Year: 2019 PMID： 31577901 DOI： 10.1021/acs.jmedchem.9b01104
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446