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Author response: Shifting the PPARγ conformational ensemble toward a transcriptionally repressive state improves covalent inhibitor efficacy

Year: 2026

Type: peer-review

Abstract: Covalent PPARγ inhibitors that better stabilize a repressive conformation are more effective inhibitors, but structural plasticity still allows ligand cobinding by enabling a shift back to an active conformation.

DOI: 10.7554/elife.106697.3.sa3

Authors: Liudmyla Arifova, Brian S MacTavish, Zane Laughlin, Mithun Nag Karadi Girdhar, Jinsai Shang, Min-Hsuan Li, Xiaoyu Yu, Di Zhu, Thedore M Kamenecka, Douglas J Kojetin

Institutions: Vanderbilt University, The Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, Guangzhou Regenerative Medicine and Health Guangdong Laboratory

Topic: Peroxisome Proliferator-Activated Receptors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

OpenAlex ID: W7125237174

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