Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer

Author:

Zhang Yan123,Wu Xishan123,Xue Xiaoqian14,Li Chenchang1,Wang Junjian5,Wang Rui1,Zhang Cheng16,Wang Chao123,Shi Yudan123,Zou Lingjiao123,Li Qiu123,Huang Zenghong,Hao Xiaojuan7ORCID,Loomes Kerry8,Wu Donghai9,Chen Hong-Wu,Xu Jinxin9,Xu Yong13ORCID

Affiliation:

1. Guangdong Provincial Key Laboratory of Biocomputing, Joint School of Life Sciences, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences; Guangzhou Medical University, Guangzhou 510530, China

2. University of Chinese Academy of Sciences, No. 19 Yuquan Road, Beijing 100049, China

3. Guangzhou Regenerative Medicine and Health Guangdong Laboratory (GRMH-GDL), Guangzhou 510530, China

4. School of Life Science, Huizhou University, Huizhou 516007, China

5. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China

6. School of Pharmaceutical Sciences, Jilin University, No.1266 Fujin Road, Chaoyang District, Changchun, Jilin 130021, China

7. Manufacturing, Commonwealth Scientific and Industrial Research Organization (CSIRO), Clayton, Vic 3168, Australia

8. School of Biological Sciences & Maurice Wilkins Centre, University of Auckland, Auckland 1010, New Zealand

9. Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China

Funder

National Natural Science Foundation of China

Chinese Academy of Sciences

U.S. Department of Defense

Ministry of Science and Technology of the People's Republic of China

Prostate Cancer Foundation

National Cancer Institute

Guangdong Provincial Key Laboratory of Biocomputing

Guangzhou Regenerative Medicine and Health Guangdong Laboratory

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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