Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069

[Image: see text] The ligand-activated nuclear receptor peroxisome-proliferator-activated receptor-γ (PPARG or PPARγ) represents a potential target for a new generation of cancer therapeutics, especially in muscle-invasive luminal bladder cancer where PPARγ is a critical lineage driver. Here we disc...

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Detalles Bibliográficos
Autores principales: Orsi, Douglas L., Pook, Elisabeth, Bräuer, Nico, Friberg, Anders, Lienau, Philip, Lemke, Christopher T., Stellfeld, Timo, Brüggemeier, Ulf, Pütter, Vera, Meyer, Hanna, Baco, Maria, Tang, Stephanie, Cherniack, Andrew D., Westlake, Lindsay, Bender, Samantha A., Kocak, Mustafa, Strathdee, Craig A., Meyerson, Matthew, Eis, Knut, Goldstein, Jonathan T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9662185/
https://www.ncbi.nlm.nih.gov/pubmed/36270630
http://dx.doi.org/10.1021/acs.jmedchem.2c01379

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