Ontology highlight
ABSTRACT:
SUBMITTER: Jin Y
PROVIDER: S-EPMC5046141 | biostudies-literature | 2016 Oct
REPOSITORIES: biostudies-literature
Jin Yifeng Y Han Younho Y Khadka Daulat Bikram DB Zhao Chao C Lee Kwang Youl KY Cho Won-Jea WJ
Scientific reports 20161003
Conformational change in helix 12 can alter ligand-induced PPARγ activity; based on this reason, isoquinolinoquinazolinones, structural homologs of berberine, were designed and synthesized as PPARγ antagonists. Computational docking and mutational study indicated that isoquinolinoquinazolinones form hydrogen bonds with the Cys285 and Arg288 residues of PPARγ. Furthermore, SPR results demonstrated strong binding affinity of isoquinolinoquinazolinones towards PPARγ. Additionally, biological assays ...[more]