Ontology highlight
ABSTRACT:
SUBMITTER: Shang J
PROVIDER: S-EPMC6317912 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Shang Jinsai J Brust Richard R Mosure Sarah A SA Bass Jared J Munoz-Tello Paola P Lin Hua H Hughes Travis S TS Tang Miru M Ge Qingfeng Q Kamenekca Theodore M TM Kojetin Douglas J DJ
eLife 20181221
Crystal structures of peroxisome proliferator-activated receptor gamma (PPARγ) have revealed overlapping binding modes for synthetic and natural/endogenous ligands, indicating competition for the orthosteric pocket. Here we show that cobinding of a synthetic ligand to the orthosteric pocket can push natural and endogenous PPARγ ligands (fatty acids) out of the orthosteric pocket towards an alternate ligand-binding site near the functionally important omega (Ω)-loop. X-ray crystallography, NMR sp ...[more]