Document Report Card

ID: ALA1671844

Journal: ACS Med Chem Lett

Title: Structure guided development of potent reversibly binding penicillin binding protein inhibitors.

Authors: Woon EC, Zervosen A, Sauvage E, Simmons KJ, Zivec M, Inglis SR, Fishwick CW, Gobec S, Charlier P, Luxen A, Schofield CJ.

Abstract: Following from the evaluation of different types of electrophiles, combined modeling and crystallographic analyses are used to generate potent boronic acid based inhibitors of a penicillin binding protein. The results suggest that a structurally informed approach to penicillin binding protein inhibition will be useful for the development of both improved reversibly binding inhibitors, including boronic acids, and acylating inhibitors, such as β-lactams.

CiteXplore: 24900305

DOI: 10.1021/ml100260x