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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.

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Title: Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Authors: Orsi DL; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Ferrara SJ; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Siegel S; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Friberg A; Nuvisan ICB GmbH, 13353 Berlin, Germany., Bouché L; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Pook E; Research and Development, Pharmaceuticals, Bayer AG, 42113 Wuppertal, Germany., Lienau P; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Bluck JP; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Lemke CT; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Akcay G; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA., Stellfeld T; Nuvisan ICB GmbH, 13353 Berlin, Germany., Meyer H; Nuvisan ICB GmbH, 13353 Berlin, Germany., Pütter V; Nuvisan ICB GmbH, 13353 Berlin, Germany., Holton SJ; Nuvisan ICB GmbH, 13353 Berlin, Germany., Korr D; Nuvisan ICB GmbH, 13353 Berlin, Germany., Jerchel-Furau I; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA., Pantelidou C; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA., Strathdee CA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Meyerson M; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Center for Cancer Genomics, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Genetics and Medicine, Harvard Medical School, Boston, MA 02115, USA., Eis K; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Goldstein JT; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA. Electronic address: jgold@broadinstitute.org.
Source: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2023 Jan 15; Vol. 78, pp. 117130. Date of Electronic Publication: 2022 Dec 13.
Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
Journal Info: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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  Data: Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
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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, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Ferrara+SJ%22">Ferrara SJ</searchLink>; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Siegel+S%22">Siegel S</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 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="%22Bouché+L%22">Bouché L</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Pook+E%22">Pook E</searchLink>; Research and Development, Pharmaceuticals, Bayer AG, 42113 Wuppertal, 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="%22Bluck+JP%22">Bluck JP</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, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Akcay+G%22">Akcay G</searchLink>; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Stellfeld+T%22">Stellfeld T</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="%22Pütter+V%22">Pütter V</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Holton+SJ%22">Holton SJ</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Korr+D%22">Korr D</searchLink>; Nuvisan ICB GmbH, 13353 Berlin, Germany.<br /><searchLink fieldCode="AU" term="%22Jerchel-Furau+I%22">Jerchel-Furau I</searchLink>; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Pantelidou+C%22">Pantelidou C</searchLink>; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Strathdee+CA%22">Strathdee CA</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Meyerson+M%22">Meyerson M</searchLink>; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Center for Cancer Genomics, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Genetics and Medicine, Harvard Medical School, Boston, MA 02115, USA.<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, MA 02142, USA. Electronic address: jgold@broadinstitute.org.
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  Data: <searchLink fieldCode="JN" term="%229413298%22">Bioorganic & medicinal chemistry</searchLink> [Bioorg Med Chem] 2023 Jan 15; Vol. 78, pp. 117130. <i>Date of Electronic Publication: </i>2022 Dec 13.
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