Ontology highlight
ABSTRACT:
SUBMITTER: Mizukoshi Y
PROVIDER: S-EPMC7527212 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Mizukoshi Yumiko Y Takeuchi Koh K Tokunaga Yuji Y Matsuo Hitomi H Imai Misaki M Fujisaki Miwa M Kamoshida Hajime H Takizawa Takeshi T Hanzawa Hiroyuki H Shimada Ichio I
Science advances 20200930 40
Cryptic ligand binding sites, which are not evident in the unligated structures, are beneficial in tackling with difficult but attractive drug targets, such as protein-protein interactions (PPIs). However, cryptic sites have thus far not been rationally pursued in the early stages of drug development. Here, we demonstrated by nuclear magnetic resonance that the cryptic site in Bcl-xL exists in a conformational equilibrium between the open and closed conformations under the unligated condition. W ...[more]