2011.09 – now Guangzhou Institutes of Biomedicine and Health, CAS /Principle Investigator
2006.06 – 2011.08 Van Andel Research Institute, Michigan, USA/Postdoctoral fellow
2004.08 – 2006.05 Shanghai Institute of Organic Chemistry, CAS/Postdoctoral fellow
2001.09 – 2004.07 Shanghai Institute of Materia Medica, CAS/Ph.D
Dr. Xu mainly focuses on the clinical-need-oriented basic research on medicinal chemistry with the aim of identifying and validating drug targets and lead compounds. By combining computational biology, computer-aided drug design, medicinal chemistry, and structural biology, significant achievements have been achieved in the field of lead compounds discovery and target validation for hormone receptors and related epigenetic receptors.
For the first time, he identified and validated RORγ as novel therapeutic target for lethal castration resistant prostate cancer. For lead development, a series of potent compounds with drug like properties was identified for RORγ (AR driver), BRD4 (AR coregulator). Dr. Xu has published over 60 SCI indexed papers in Nature, Science, Nature Medicine, Nat Struct Mol Biol, J Med Chem and others with cumulative impact factors exceeding 400. Some research works were highlighted in Nature, Nat Rev Urol and other journals. Dr. Xu was awarded the "2016 Movember-PCF Challenge Award" by Prostate Cancer Foundation.
1. Zhang M, Zhang Y,……, Wu D, Ding K, Xu Y*. Structure-Based Discovery and Optimization of Benzo[d]isoxazole Derivatives as Potent and Selective BET Inhibitors as Potential Treatment for Castration-Resistant Prostate Cancer (CRPC). J. Med. Chem. 2018 Apr;61(7):3037-3058
2. Wang J, Zou, JX,……, Evans R.M, Xu Y*, Chen, H.W*.ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer. Nat Med, 2016 May;22(5): 488-496. (Highlighted by Nature, Nature Review Urology)
3. Xue X, Zhang Y, Liu Z,……, Xu Y*. Discovery of benzo[cd]indol-2(1H)-ones as potent and specific BET bromodomain inhibitors: structure-based virtual screening, optimization, and biological evaluation. J Med Chem.2016 Feb; 59, 1565-1579
4. Cao M, Liu X,……, Zhu JK.*, Xu HE*, Xu Y*. An ABA-mimicking ligand that reduces water loss and promotes drought resistance in plants. Cell Res. 2013 Aug;23(8): 1043-1054. (Highlighted by Nature Review Genetics)
5. Melcher K#, Xu Y#, Ng LM, Zhou XE. ,……, Zhu JK, Xu, HE*. Identification and mechanism of ABA receptor antagonism. Nat Struct Mol Biol.2010 Sep;17(9):1102 -1108