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Selective thyroid hormone receptor ß agonists with oxadiazolone acid isosteres.
Kirschberg, Thorsten A; Jones, Christopher T; Xu, Yingzi; Fenaux, Martijn; Halcomb, Randall L; Wang, Yujin; Klucher, Kevin.
Afiliación
  • Kirschberg TA; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA. Electronic address: tkirschberg@ternspharma.com.
  • Jones CT; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
  • Xu Y; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
  • Fenaux M; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
  • Halcomb RL; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
  • Wang Y; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
  • Klucher K; Terns Pharmaceuticals Inc., 1065 E. Hillsdale Blvd., Suite 100, Foster City, CA 94404, USA.
Bioorg Med Chem Lett ; 30(21): 127465, 2020 11 01.
Article en En | MEDLINE | ID: mdl-32768645
ABSTRACT
Use of the oxadiazolone acid isostere in triiodothyronine analogs yielded potent and selective agonists for the thyroid hormone receptor ß. Selected examples showed good in-vivo efficacy in a rat hypercholesterolemic model. One compound was further profiled in a diet-induced mouse model of nonalcoholic steatohepatitis (NASH) and showed robust target engagement and significant histological improvements in both liver steatosis and fibrosis.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxadiazoles / Receptores beta de Hormona Tiroidea Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxadiazoles / Receptores beta de Hormona Tiroidea Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article