Areas of Focus
- Drug Chemistry
- Computer-Aided Drug Design
- Structural Biology
- Nuclear Receptor Drugs
- Epigenetics
Work Experience
- 2011-09 to Present - Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences - Researcher
- 2006-06 to 2011-08 - Van Andel Research Institute, USA - Postdoctoral Researcher
- 2004-08 to 2006-05 - Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences - Postdoctoral Researcher
Academic Background & Achievements
- 2001-09 to 2004-07 PhD: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Publications
- Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity, Corresponding Author, 2024
- Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia, Corresponding Author, 2024
- Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo4,5-cquinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation, Corresponding Author, 2024
- 1,3-disubstituted-1,2,4-triazin-6-ones with potent activity against androgen receptor-dependent prostate cancer cells, Corresponding Author, 2024
- Discovery of a potent and selective CBP bromodomain inhibitor (Y08262) for treating acute myeloid leukemia, Corresponding Author, 2024
- Discovery and pharmacological characterization of 1,2,3,4-tetrahydroquinoline derivatives as RORγ inverse agonists against prostate cancer, Corresponding Author, 2024
- Advances in Anti-prostate Cancer-Related Nuclear Receptors and Small Molecule Drugs, Corresponding Author, 2023
- Rational design, synthesis and biological evaluation of benzodisoxazole derivatives as potent BET bivalent inhibitors for potential treatment of prostate cancer, Corresponding Author, 2023
- Discovery of a Highly Selective and H435R-Sensitive ThyroidHormone Receptor?Agonist, Corresponding Author, 2022
- Structural insights revealed by the cocrystal structure of CCS1477 in complex with CBP bromodomain, Corresponding Author, 2022
- Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer, Corresponding Author, 2022
- Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders, 7th Author, 2022
- Structure-Based Discovery and Optimization of Furo3,2-cpyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors, Corresponding Author, 2022
- Design, synthesis and anticancer evaluation of 3-methyl-1H-indazole derivatives as novel selective bromodomain-containing protein 4 inhibitors, Corresponding Author, 2022
- Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors, Corresponding Author, 2022
- Design,synthesis and pharmacological characterization of N-(3-ethylbenzodisoxazol-5-yl)sulfonamide derivatives as BRD4 inhibitors against acute myeloid leukemia, Corresponding Author, 2022
- Design, synthesis, and anticancer evaluation of ammosamide B with pyrroloquinoline derivatives as novel BRD4 inhibitors, Corresponding Author, 2022
- Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist, Corresponding Author, 2021
- The natural compound rutaecarpine promotes white adipocyte browning through activation of the AMPK-PRDM16 axis, 10th Author, 2021
- Pyrido2, 3-dpyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors, 11th Author, 2021
- Y06014 is a selective BET inhibitor for the treatment of prostate cancer, Corresponding Author, 2021
- e-Graphene: A Computational Platform for the Prediction of Graphene-Based Drug Delivery System by Quantum Genetic Algorithm and Cascade Protocol, 5th Author, 2021
- Design and Optimization of 3 '-(Imidazo1,2-alphapyrazin-3-yl)-1,1 '-biphenyl-3-carboxamides as Selective DDR1 Inhibitors, 8th Author, 2020
- Quantitative Prediction of Hemolytic Toxicity for Small Molecules and Their Potential Hemolytic Fragments by Machine Learning and Recursive Fragmentation Methods, 5th Author, 2020
- In Silico Prediction of Hemolytic Toxicity on the Human Erythrocytes for Small Molecules by Machine-Learning and Genetic Algorithm, 6th Author, 2020
- Discovery and optimization of novel N-benzyl-3,6-dimethylbenzodisoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities, Corresponding Author, 2020
- e-Sweet: A Machine-Learning Based Platform for the Prediction of Sweetener and Its Relative Sweetness, 4th Author, 2019
- Prediction of Hemolytic Toxicity for Saponins by Machine-Learning Methods, 5th Author, 2019
- Identification of New Small Molecule Inducers of Estrogen-related Receptor alpha (ERR alpha) Degradation, 9th Author, 2019
- Y08197 is a novel and selective CBP/EP300 bromodomain inhibitor for the treatment of prostate cancer, Corresponding Author, 2019
- Computational Prediction of a New ADMET Endpoint for Small Molecules: Anticommensal Effect on Human Gut Microbiota, 5th Author, 2019
- Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable ROR gamma Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer, Corresponding Author, 2019
- Discovery of the First Low Nanomolar Liver Receptor Homolog-1 (LRH-1) Agonist, Corresponding Author, 2019
- Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer, Corresponding Author, 2018
- Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer, Corresponding Author, 2018
- Cell- and Tissue-Based Proteome Profiling and Dual Imaging of Apoptosis Markers with Probes Derived from Venetoclax and Idasanutlin, 8th Author, 2018
- e-Bitter: Bitterant Prediction by the Consensus Voting From the Machine-Learning Methods, 6th Author, 2018
- The natural compound, formononetin, extracted from Astragalus membranaceus increases adipocyte thermogenesis by modulating PPAR gamma activity, 16th Author, 2018
- Structure-Based Discovery and Optimization of Benzo&ITd&ITisoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC), Corresponding Author, 2018
- Y08060: A Selective BET Inhibitor for Treatment ofProstate Cancer, Corresponding Author, 2018
- Design, synthesis, and structure-activity relationship study of 2-oxo-3,4-dihydropyrimido4,5-dpyrimidines as new colony stimulating factor 1 receptor (csf1r) kinase inhibitors, 9th Author, 2018
- The first pediatric case of glucagon receptor defect due to biallelic mutations in GCGR is identified by newborn screening of elevated arginine, 8th Author, 2018
- A structure-guided optimization of pyrido2,3-dpyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties, 7th Author, 2017
- Proposed Hydrogen-Bonding Index of Donor or Acceptor Reflecting Its Intrinsic Contribution to Hydrogen-Bonding Strength, 7th Author, 2017
- 2-Aminopyrimidine Derivatives as New SelectiveFibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors, 7th Author, 2017
- Structural basis for functional selectivity and ligand recognition revealed by crystal structures of human secreted phospholipase A2 group IIE., 5th Author, 2017
- Visualization and Quantification of Browning Using a Ucp1-2A-Luciferase Knock-in Mouse Model., 8th Author, 2017
Awards
- Prostate Cancer Foundation, 2017 PCF Challenge Award
- Guangdong Provincial Science and Technology Award, Second Prize, Provincial Level, 2018
