A structural mechanism for directing inverse agonism of PPARγ
R. Brust, J. Shang, J. Fuhrmann, J. Bass, A. Cano, Z. Heidari, I. Chrisman, A.-L. Blayo, P. Griffin, T. Kamenecka, T. Hughes, D. Kojetin
The paper shows how a phenyl-to-pyridyl substitution in PPARγ ligands converts an antagonist to an inverse agonist through a water-mediated hydrogen bond network involving Arg288.
bioRxiv · Jan 17, 2018Biochemistry