Shifting the PPARγ conformational ensemble towards a transcriptionally repressive state improves covalent inhibitor efficacy
Liudmyla Arifova, Brian S. MacTavish, Zane T. Laughlin, Mithun Nag Karadi Giridhar, Jinsai Shang, Mei Li, Xiaoyu Yu, Di Zhu, Theodore M. Kamenecka, Douglas J. Kojetin
The paper investigates how covalent inhibitors of PPARγ shift its conformational state, affecting ligand binding and inhibitor efficacy.
eLife · Jan 21, 2026Peer-reviewedBiochemistry