070303-有机化学

激酶非催化功能的小分子调控
激酶抑制剂的研发

2011-09--2016-07   中国科学院广州生物医药与健康研究院   博士
2007-09--2011-07   合肥工业大学   学士

   

2021-06~现在, 中国科学院上海有机化学研究所, 研究员
2016-08~2021-05,美国Moffitt Cancer Center & Research Institute, 博士后
2011-09~2016-07,中国科学院广州生物医药与健康研究院, 博士
2007-09~2011-07,合肥工业大学, 学士

2024-12-01-今,中国药学会药物化学专业委员会, 青年委员

   

（ 1 ） 一类新型CDK12/13共价抑制剂或其药物组合物和应用, 2024, 第 6 作者, 专利号: CN117658982A

   

（1） Discovery of HZS60 as a Novel Brain Penetrant NMDAR/TRPM4 Interaction Interface Inhibitor with Improved Activity and Pharmacokinetic Properties for the Treatment of Cerebral Ischemia, JOURNAL OF MEDICINAL CHEMISTRY, 2025, 第 20 作者
（2） Discovery of LLC355 as an Autophagy-Tethering Compound for the Degradation of Discoidin Domain Receptor 1, JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 15 作者  通讯作者
（3） Unlocking the Potential: Advancements and Future Horizons in ROR1-Targeted Cancer Therapies, 中国科学:生命科学(英文版), 2024, 第 4 作者
（4） Discovery of ZLC491 as a Potent, Selective, and Orally Bioavailable CDK12/13 PROTAC Degrader, JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 17 作者  通讯作者
（5） Discovery of 5-aminopyrido[2,3-d]pyrimidin-7(8H)-one derivatives as new hematopoietic progenitor kinase 1 (HPK1) inhibitors, European Journal of Medicinal Chemistry, 2024, 第 9 作者
（6） Discovery of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 9 作者  通讯作者
（7） Structure-Based Design of "Head-to-Tail" Macrocyclic PROTACs, JACS AU, 2024, 第 11 作者
（8） Mechanisms of Acquired Resistance to HER2-Positive Breast Cancer Therapies Induced by HER3: A Comprehensive Review, European Journal of Pharmacology, 2024, 第 9 作者
（9） Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader, JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 14 作者  通讯作者
（10） NSD2 is a requisite subunit of the AR/FOXA1 neo-enhanceosome in promoting prostate tumorigenesis, NATURE GENETICS, 2024, 第 32 作者
（11） The role of SLC12A family of cation-chloride cotransporters and drug discovery methodologies, JOURNAL OF PHARMACEUTICAL ANALYSIS, 2023, 第 12 作者
（12） Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 第 6 作者
（13） Discovery of a First-in-Class Degrader for the Lipid Kinase PIKfyve, JOURNAL OF MEDICINAL CHEMISTRY, 2023, 第 13 作者  通讯作者
（14） Discovery of AXL Degraders with Improved Potencies in Triple- Negative Breast Cancer (TNBC) Cells, JOURNAL OF MEDICINAL CHEMISTRY, 2023, 第 10 作者
（15） A small-molecule drug inhibits autophagy gene expression through the central regulator TFEB., Proc Natl Acad Sci U S A, 2023, 第 13 作者
（16） A novel photocaged B-Raf V600E inhibitor toward precise melanoma treatment, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2022, 第 7 作者  通讯作者
（17） New ZW4864 Derivatives as Small-Molecule Inhibitors for the beta-Catenin/BCL9 Protein-Protein Interaction, ACS MEDICINAL CHEMISTRY LETTERS, 2022, 第 1 作者
（18） A novel photocaged B-RafV600E inhibitor toward precise melanoma treatment, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2022, 第 7 作者  通讯作者
（19） Targeting the Non-Catalytic Functions: a New Paradigm for Kinase Drug Discovery?, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 1 作者  通讯作者
（20） 1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 10 作者  通讯作者
（21） Discovery of Hexahydrofuro3,2-bfurans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 16 作者  通讯作者
（22） Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 13 作者  通讯作者
（23） Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 4 作者
（24） New ZW4864 Derivatives as Small-Molecule Inhibitors for the ��-Catenin/BCL9 Protein-Protein Interaction, ACS Med. Chem. Lett., 2022, 第 1 作者
（25） Direct targeting of ��-catenin in the Wnt signaling pathway: Current progress and perspectives, MEDICINAL RESEARCH REVIEWS, 2021, 第 1 作者
（26） Autophagy inhibition by targeting PIKfyve potentiates response to immune checkpoint blockade in prostate cancer, NATURE CANCER, 2021, 第 24 作者
（27） Direct targeting of beta-catenin in the Wnt signaling pathway: Current progress and perspectives, MEDICINAL RESEARCH REVIEWS, 2021, 第 1 作者
（28） Discovery of an Orally Bioavailable Small-Molecule Inhibitor for the beta-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction, JOURNAL OF MEDICINAL CHEMISTRY, 2021, 第 1 作者
（29） Preclinical Evaluation of [225Ac]Ac-DOTA-TATE for Treatment of Lung Neuroendocrine Neoplasms, European Journal of Nuclear Medicine and Molecular Imaging, 2021, 第 1 作者
（30） Discovery of 2-(3-(3-Carbamoylpiperidin-1-yl)phenoxy)acetic Acid Derivatives as Novel Small-Molecule Inhibitors of the beta-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction, JOURNAL OF MEDICINAL CHEMISTRY, 2021, 第 1 作者
（31） Small-Molecule CSF1R Inhibitors as Anticancer Agents, CURRENT MEDICINAL CHEMISTRY, 2020, 第 2 作者
（32） GZD2202, a novel TrkB inhibitor, suppresses BDNF-mediated proliferation and metastasis in neuroblastoma models, JOURNAL OF DRUG TARGETING, 2019, 第 7 作者
（33） Optimization of Peptidomimetics as Selective Inhibitors for the beta-Catenin/T-Cell Factor Protein-Protein Interaction, JOURNAL OF MEDICINAL CHEMISTRY, 2019, 第 1 作者
（34） Design, Synthesis, and Biological Evaluation of 3-(Imidazo1,2- a pyrazin-3-ylethynyl)-4-isopropyl- N -(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 1 作者
（35） Structure-Based Optimization of Small-Molecule Inhibitors for the beta-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 2 作者
（36） Design, Synthesis, and Biological Evaluation of 3-(Imidazo1,2-apyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 1 作者
（37） 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, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 6 作者
（38） Inhibition of discoidin domain receptor 1 reduces collagen-mediated tumorigenicity in pancreatic ductal adenocarcinoma, MOLECULAR CANCER THERAPEUTICS, 2017, 第 5 作者
（39） Tetrahydroisoquinoline-7-carboxamide Derivatives asNew Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors, ACS MEDICINAL CHEMISTRY LETTERS, 2017, 第 1 作者
（40） Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma, NATURE MEDICINE, 2016, 第 11 作者
（41） Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 第 1 作者
（42） Small-Molecule BET Inhibitors in Clinical and Preclinical Development and Their Therapeutic Potential, CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2015, 第 2 作者

   

（ 1 ） CDK12/13 抑制剂和降解剂的发现及其在前列腺癌中的潜在治疗作用研究, 负责人, 国家任务, 2023-12--2026-11
（ 2 ） 新型HPK1小分子抑制剂的设计、合成和抗肿瘤活性研究, 负责人, 国家任务, 2023-01--2025-12
（ 3 ） 国家引才计划-院匹配, 负责人, 中国科学院计划, 2023-01--2025-12
（ 4 ） 国家引才计划, 负责人, 国家任务, 2023-01--2025-12
（ 5 ） 可克服EGFR三代抑制剂osimertinib耐药的非小细胞肺癌的 治疗药物研究, 负责人, 地方任务, 2022-09--2025-08