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Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer.
Aicher, Thomas D; Van Huis, Chad A; Hurd, Alexander R; Skalitzky, Donald J; Taylor, Clarke B; Beleh, Omar M; Glick, Gary; Toogood, Peter L; Yang, Bing; Zheng, Tao; Huo, Changxin; Gao, Jie; Qiao, Chenxi; Tian, Xiaolong; Zhang, Junping; Demock, Kellie; Hao, Ling-Yang; Lesch, Charles A; Morgan, Rodney W; Moisan, Jacques; Wang, Yahong; Scatina, JoAnn; Paulos, Chrystal M; Zou, Weiping; Carter, Laura L; Hu, Xiao.
Afiliación
  • Aicher TD; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Van Huis CA; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Hurd AR; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Skalitzky DJ; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Taylor CB; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Beleh OM; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Glick G; Chief Scientific Officer, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Toogood PL; Department of Chemistry, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Yang B; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Zheng T; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Huo C; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Gao J; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Qiao C; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Tian X; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Zhang J; Department of Chemistry, Pharmaron Beijing, Co. Ltd., Beijing 100176, P. R. China.
  • Demock K; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Hao LY; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Lesch CA; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Morgan RW; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Moisan J; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Wang Y; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Scatina J; Department of Preclinical Development, Lycera Corp., 620 Germantown Pike, Plymouth Meeting, Pennsylvania 19462, United States.
  • Paulos CM; Hollings Cancer Center, Medical University of South Carolina, 173 Ashley Avenue, MSC 509, Room 203, Charleston, South Carolina 29425, United States.
  • Zou W; School of Medicine, Department of Surgery, University of Michigan, 2101 Taubman Center, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, United States.
  • Carter LL; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
  • Hu X; Department of Biology, Lycera Corp., 1350 Highland Drive, Suite A, Ann Arbor, Michigan 48108, United States.
J Med Chem ; 64(18): 13410-13428, 2021 09 23.
Article en En | MEDLINE | ID: mdl-34499493
ABSTRACT
Retinoic acid receptor-related orphan receptor γ (RORc, RORγ, or NR1F3) is the nuclear receptor master transcription factor that drives the function and development of IL-17-producing T helper cells (Th17), cytotoxic T cells (Tc17), and subsets of innate lymphoid cells. Activation of RORγ+ T cells in the tumor microenvironment is hypothesized to render immune infiltrates more effective at countering tumor growth. To test this hypothesis, a family of benzoxazines was optimized to provide LYC-55716 (37c), a potent, selective, and orally bioavailable small-molecule RORγ agonist. LYC-55716 decreases tumor growth and enhances survival in preclinical tumor models and was nominated as a clinical development candidate for evaluation in patients with solid tumors.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Propionatos / Benzoxazinas / Miembro 3 del Grupo F de la Subfamilia 1 de Receptores Nucleares / Neoplasias / Antineoplásicos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Propionatos / Benzoxazinas / Miembro 3 del Grupo F de la Subfamilia 1 de Receptores Nucleares / Neoplasias / Antineoplásicos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Estados Unidos