Drug design from the cryptic inhibitor envelope

oleh: Chul-Jin Lee, Xiaofei Liang, Qinglin Wu, Javaria Najeeb, Jinshi Zhao, Ramesh Gopalaswamy, Marie Titecat, Florent Sebbane, Nadine Lemaitre, Eric J. Toone, Pei Zhou

Format: Article
Diterbitkan: Nature Portfolio 2016-02-01

Deskripsi

The conformational dynamics of a compound has a large effect on ligand/receptor binding. Here, the authors employ NMR spectroscopy to study ligand binding to the enzyme LpxC, discovering an inhibitor envelope that was not identifiable by crystallography and subsequently developing a highly potent inhibitor.