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

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Title: Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069.
Authors: Orsi DL; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Pook E; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Bräuer N; Nuvisan ICB GmbH, 13353 Berlin, Germany., Friberg A; Nuvisan ICB GmbH, 13353 Berlin, Germany., Lienau P; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Lemke CT; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Stellfeld T; Nuvisan ICB GmbH, 13353 Berlin, Germany., Brüggemeier U; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Pütter V; Nuvisan ICB GmbH, 13353 Berlin, Germany., Meyer H; Nuvisan ICB GmbH, 13353 Berlin, Germany., Baco M; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Tang S; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Cherniack AD; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States., Westlake L; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Bender SA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Kocak M; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Strathdee CA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States., Meyerson M; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.; Center for Cancer Genomics, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.; Department of Genetics and Medicine, Harvard Medical School, Boston, Massachusetts 02115, United States., Eis K; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Goldstein JT; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2022 Nov 10; Vol. 65 (21), pp. 14843-14863. Date of Electronic Publication: 2022 Oct 21.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
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  Data: Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069.
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  Data: <searchLink fieldCode="AU" term="%22Orsi+DL%22">Orsi DL</searchLink>; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Pook+E%22">Pook E</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Bräuer+N%22">Bräuer N</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Friberg+A%22">Friberg A</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Lienau+P%22">Lienau P</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Lemke+CT%22">Lemke CT</searchLink>; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Stellfeld+T%22">Stellfeld T</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Brüggemeier+U%22">Brüggemeier U</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Pütter+V%22">Pütter V</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Meyer+H%22">Meyer H</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Baco+M%22">Baco M</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Tang+S%22">Tang S</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Cherniack+AD%22">Cherniack AD</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.<br /><searchLink fieldCode="AU" term="%22Westlake+L%22">Westlake L</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Bender+SA%22">Bender SA</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Kocak+M%22">Kocak M</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Strathdee+CA%22">Strathdee CA</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Meyerson+M%22">Meyerson M</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.; Center for Cancer Genomics, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States.; Department of Genetics and Medicine, Harvard Medical School, Boston, Massachusetts 02115, United States.<br /><searchLink fieldCode="AU" term="%22Eis+K%22">Eis K</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Goldstein+JT%22">Goldstein JT</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, Massachusetts 02142, United States.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2022 Nov 10; Vol. 65 (21), pp. 14843-14863. <i>Date of Electronic Publication: </i>2022 Oct 21.
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