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Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor
Institution:1. Department of Diabetes and Metabolic Diseases Research, Beckman Research Institute, City of Hope National Medical Center, Duarte, CA 91010, USA;2. Department of Chemical Biology & Therapeutics, St. Jude Children’s Research Hospital, Memphis, TN 38105, USA;1. Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India;2. Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM, Jammu Campus, Jammu 180001, India;1. Hiroshima International University, Faculty of Clinical Nutrition, 5-1-1, Hirokoshingai, Kure, Hiroshima 737-0112, Japan;2. Hiroshima International University, Faculty of Pharmaceutical Sciences, 5-1-1, Hirokoshingai, Kure, Hiroshima 737-0112, Japan;3. National Institute of Health Sciences, Kamiyoga 1-18-1, Setagaya-ku, Tokyo 158-8501, Japan;4. Computer-aided Molecular Modeling Research Center, Kansai (CAMM-Kansai), 3-32-302, Tsuto-Otsuka, Nishinomiya 663-8241, Japan;3. From the School of Life Sciences, University of Science and Technology of China, Hefei 230026, China,;4. the State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China,;5. the Guangdong Provincial Key Laboratory of Biocomputing, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China, and;6. Guangzhou Henovcom Biosciences Inc., Guangzhou 510530, China
Abstract:
Keywords:HTS"}  {"#name":"keyword"  "$":{"id":"k0010"}  "$$":[{"#name":"text"  "_":"high-throughput screen  FXR"}  {"#name":"keyword"  "$":{"id":"k0020"}  "$$":[{"#name":"text"  "_":"farnesoid X receptor  NRs"}  {"#name":"keyword"  "$":{"id":"k0030"}  "$$":[{"#name":"text"  "_":"nuclear receptors  Cyp7A1"}  {"#name":"keyword"  "$":{"id":"k0040"}  "$$":[{"#name":"text"  "_":"cytochrome 7A1  BAs"}  {"#name":"keyword"  "$":{"id":"k0050"}  "$$":[{"#name":"text"  "_":"bile acids  BSEP"}  {"#name":"keyword"  "$":{"id":"k0060"}  "$$":[{"#name":"text"  "_":"bile salt export pump  SAR"}  {"#name":"keyword"  "$":{"id":"k0070"}  "$$":[{"#name":"text"  "_":"structure–activity relationship  LBD"}  {"#name":"keyword"  "$":{"id":"k0080"}  "$$":[{"#name":"text"  "_":"ligand-binding domain
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