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Cell Chemical Biology|May 28, 2026
Covalent PPARγ inverse agonism by FX-909 reveals mechanistic insights into therapeutic targeting of PPARγ/RXRα-activated urothelial carcinomaJacob I Stuckey, Jennifer A Mertz, Jonathan E Wilson, et al.Nature Medicine|February 27, 2026
A small-molecule inverse agonist of PPARγ for advanced solid tumors: a phase 1 trialMatthew D Galsky, Charlene Mantia, Michaela Bowden, et al.Bioorganic & Medicinal Chemistry Letters|April 9, 2015
Development of methyl isoxazoleazepines as inhibitors of BETMichael C Hewitt, Yves Leblanc, Victor S Gehling, et al.Clinical Cancer Research : an Official Journal of the American Association for Cancer Research|May 13, 2016
Regulation of GLI Underlies a Role for BET Bromodomains in Pancreatic Cancer Growth and the Tumor MicroenvironmentYinshi Huang, Sabikun Nahar, Akifumi Nakagawa, et al.ACS Medicinal Chemistry Letters|March 18, 2016
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET BromodomainsAlexander M Taylor, Rishi G Vaswani, Victor S Gehling, et al.Cancer Research|June 4, 2024
Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant CancersPatricia J Keller, Elizabeth J Adams, Rentian Wu, et al.ACS Medicinal Chemistry Letters|June 6, 2014
Discovery, Design, and Optimization of Isoxazole Azepine BET InhibitorsVictor S Gehling, Michael C Hewitt, Rishi G Vaswani, et al.Journal of Medicinal Chemistry|January 28, 2016
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical TrialsBrian K Albrecht, Victor S Gehling, Michael C Hewitt, et al.The Journal of Biological Chemistry|April 9, 2016
Regulatory T Cell Modulation by CBP/EP300 Bromodomain InhibitionSrimoyee Ghosh, Alexander Taylor, Melissa Chin, et al.Pageof 2