Structural basis of altered potency and efficacy displayed by a major in vivo metabolite of the anti-diabetic PPARγ drug pioglitazone
S. Mosure, J. Shang, R. Brust, J. Zheng, P. Griffin, D. Kojetin
This study compares the structure and function of pioglitazone and its metabolite 1-hydroxypioglitazone bound to PPARγ, showing reduced potency and efficacy of the metabolite.
bioRxiv · Aug 13, 2018Biochemistry