潘峥婴 - 北京大学 - 化学生物学与生物技术学院

个人简介

教育背景及工作经历 2009- 博士生导师，特聘研究员北京大学深圳研究生院深圳 2008-2009 研究科学家OPTI Medical Systems, IDEXX 实验室, Roswell 2006-2007 高级科学家, AtheroGenics, Alpharetta 2002-2006 高级科学家, Celera Genomics, South San Francisco 2000-2002 博士后斯坦福大学斯坦福 1994-1999 博士哥伦比亚大学纽约 1989-1994 学士北京大学北京奖项及荣誉 2013 生命科学与化学学者药明康德奖上海 2005 Celera DNA Award Celera Genomics, South San Francisco, CA 1994 优秀毕业生奖北京大学北京

研究领域

我们课题组致力于开拓新的方法用于研究人类化学生物学及推动药物的发现。我们结合尖端的药物化学和新兴化学蛋白质组学推进我们对疾病的认识和发现新的治疗药物。最初的成果包括：被誉为 “突破”的首创新药已批准在美国和欧盟上市，以及人类样品中活细胞成像和应用的小分子探针。 1. 肿瘤导向性的药物化学对于人类的多种类型的肿瘤疾病，大量生物数据证明，非正常的激酶活性在这些疾病中异常活跃。因此，我们的药物化学方向更关注于这类关键的药物靶标。我们正在开发多种结合形式靶向激酶催化结构域与和实施针对激酶的其他结构域新的化合物。 2. 激酶组学 -研究信号的转导精密工具细胞的活性很大程度受生物及化学信号的影响。激酶是信号转导通路的主要的调控因素。我们的主要目标是能够直接在人类活细胞的内源性环境中检测激酶的活性。我们正在开发新型活性/亲和力的探针激酶和方法来捕获这些酶的生理底物，了解细胞环路中时间和空间的控制因素。 3. 发展合成方法学众多科研基础中其中之一是有机合成。尽管这个领域已具有惊人的进步，但仍然有很大的需求取发现新的方法来提供方便的临床相关的生物活性分子。

近期论文

查看导师新发文章（温馨提示：请注意重名现象，建议点开原文通过作者单位确认）

Fu, T.; Zuo, Y.; Xue, G.; Zhou, D.; Pan, Z., Discovery of 2,5-diaminopyrimidine derivatives as the first series of selective monomeric degraders of B-lymphoid tyrosine kinase. European Journal of Medicinal Chemistry 2023, 256, 115460. Liu, L.; Chen, R.; Xue, G.; Hao, C.; Weng, W.; Pan, Z., Development of a cell-permeable adenine-derived probe for capture of nucleotide-binding proteins in living cells. Chinese Chemical Letters 2023, 108455. Zhou, D.; Zuo, Y.; Pan, Z., Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with In Vivo Activity. Journal of Medicinal Chemistry 2023, 66 (7), 4979-4998. Hao, C.; Li, X.; Wang, Z.; Liu, L.; He, F.; Pan, Z., Optically activated MEK1/2 inhibitors (Opti-MEKi) as potential antimelanoma agents. European Journal of Medicinal Chemistry 2023, 251, 115236. Zhong, Z.; Shi, L.; Fu, T.; Huang, J.; Pan, Z., Discovery of Novel 7-Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma. Journal of Medicinal Chemistry 2022, 65 (10), 7278-7295. Chen, R.; Wang, Z.; Liu, L.; Pan, Z., Discovery of novel photocaged ERK1/2 inhibitors as light-controlled anticancer agents. Chem. Commun. 2022, 58 (31), 4901-4904. Fu, T.; Zuo, Y.; Zhong, Z.; Chen, X.; Pan, Z., Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK). European Journal of Medicinal Chemistry 2022, 229, 114051. Wang, X.; Xue, G.; Pan, Z.* “Design, synthesis and structure–activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK)” Eur. J. Med. Chem. 2020, 187, 111918. Xue, G.; Chen, J.; Liu,L.; Zhou, D.; Zuo, Y.; Fu, T.; Pan, Z.* “Protein degradation through covalent inhibitor-based PROTACs” Chem. Commun., 2020,56, 1521. Xue, G.; Wang, K.; Zhou, D.; Zhong, H.*; Pan, Z.* “Light-Induced Protein Degradation with Photocaged PROTACs” J. Am. Chem. Soc. 2019, 141, 18370. Tang, G.; Liu, L.; Wang, X.; Pan, Z.* “Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk)” Eur. J. Med. Chem. 2019, 173, 167. Shi, L.; Zhong, Z.; Li, X.; Zhou, Y.; Pan, Z.* “Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor” J. Med. Chem. 2019, 62, 1054. Yang, Z.; Liu, H.; Pan, B.; He, F.; Pan, Z.* “Design and synthesis of (aza)indolyl maleimide based covalent inhibitors of glycogen synthase kinase 3β” Org. & Biomol. Chem. 2018, 16, 4127. Chen, J.; Wang, X.; He, F.; Pan, Z.* “Development of a selective labelling probe for Bruton’s tyrosine kinase quantification in live cells” Bioconjugate Chem. 2018, 29, 1640. Wang, X.; Guo, T.; Chen, J.; Li, X.; Zhou, Y.; Pan, Z.* “Covalent and selective immobilization of GST fusion proteins with fluorophosphonate-based probes” Chem. Commun. 2018, 54, 4661 (Back Cover). Zuo, Y.; Pan, Z*. “Small-molecule inhibitors of Bruton’s tyrosine kinase” Top. in Med. Chem. 2017. (Book Chapter) Ping, L.; Ding, N.; Shi, Y.; Feng, L.; Li, J.; Liu, Y.; Lin, Y.; Shi, C.; Wang, X.; Pan, Z.*; Song, Y.*; Zhu, J.* “The Bruton's tyrosine kinase inhibitor ibrutinib exerts immunomodulatory effects through regulation of tumor-infiltrating macrophages” Oncotarget 2017, 8, 39218. Zuo, Y.; Shi, Y.; Li, X.; Teng, Y.; Pan, Z.* “A novel 2,5-diaminopyrimidine-based affinity probe for Bruton’s tyrosine kinase” Sci. Rep. 2015, 5, 16136. Ding, N.; Li, X.; Shi, Y.; Ping, L.; Wu, L.; Fu, K.; Feng, L.; Zheng, X.; Song; Y.*; Pan, Z.*; Zhu, J.* “Irreversible dual inhibitory mode: the novel Btk inhibitor PLS-123 demonstrates promising anti-tumor activity in human B-cell lymphoma” Oncotarget. 2015, 6, 15122. Zhang, Q.; Liu, H.; Pan, Z.* “A general approach for the development of fluorogenic probes suitable for no-wash imaging of kinases in live cells” Chem. Commun. 2014, 50, 15319. Liu, H.; Yang, Z.; Pan, Z.* “Synthesis of Highly Substituted Imidazolidine-2,4-dione (Hydantoin) through Tf2O-Mediated Dual Activation of Boc-Protected Dipeptidyl Compounds” Org. Lett. 2014, 16, 5902. Zhou, Y.; Guo, T.; Tang, G.; Wu, H.; Wong, N-K.; Pan, Z.* “Site-selective Protein Immobilization by Covalent Modification of GST Fusion Proteins” Bioconjugate Chem. 2014, 25, 1911 Li, X.; Zuo, Y.; Tang, G.; Wang, Y.; Zhou, Y.; Wang, X.; Guo, T.; Xia, M.; Ding, N.; Pan, Z.* “Discovery of a Series of 2,5-Diaminopyrimidine Covalent Irreversible Inhibitors of Bruton’s Tyrosine Kinase with in Vivo Antitumor Activity” J. Med. Chem. 2014, 57, 5112. Zhou, Y.; Guo, T.; Li, X.; Dong, Y.; Galatsis, P.; Johnson, D.S.; Pan Z.* “Discovery of selective 2,4-diaminopyrimidinebased photoaffinity probes for glyoxalase I” Med. Chem. Commun. 2014, 5, 352. (Invited) Zheng, J,; Lin, S.; Zhu, X.; Jiang, B.*; Yang, Z.*; Pan Z.* “Reductant-directed formation of PS-PAMAM-supported gold nanoparticles for use as highly active and recyclable catalysts for the aerobic oxidation of alcohols and the homocoupling of phenylboronic acids.” Chem. Commun. 2012, 48, 6235. Honigberg, L.A.; Smith, A.M.; Sirisawad, M.; Verner, E.; Loury, D.; Chang, B.; Li, S.; Pan, Z.; Thamm, D.H.; Miller, R.A.; Buggy, J.J. “The Bruton Tyrosine Kinase Inhibitor PCI-32765 Blocks B-cell Activation and Is Efficacious in Models of Autoimmune Disease and B-cell Malignancy” Proc. Natl. Acad. Sci. USA 2010, 107, 13075. Zou, H.; Zhou, L.; Li, Y.; Cui, Y.; Zhong, H.; Pan, Z.; Yang, Z.; Quan, J. “Benzo[e]isoindole-1,3-diones as Potential Inhibitors of Glycogen Synthase Kinase-3 (GSK-3). Synthesis, Kinase Inhibitory Activity, Zebrafish Phenotype, and Modeling of Binding Mode” J. Med. Chem. 2010, 53, 994. Pan, Z.* “Bruton’s Tyrosine Kinase as a Drug Discovery Target” Drug News & Perspectives (Invited) Drug News & Perspectives 2008, 21, 357. Pan, Z.*; Scheerens, H.; Li, S.-J.; Schultz, B. E.; Sprengeler, P. A.; Burrill, L. C.; Mendonca, R. V.; Sweeney, M. D.; Scott, K. C. K.; Grothaus, P. G.; Jeffery, D. A.; Spoerke, J. M.; Honigberg, L. A.; Young, P. R.; Dalrymple, S. A. and Palmer, J. T. “Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase” ChemMedChem 2007, 2, 58. Pan, Z.*; Jeffery, D. A.; Chehade, K.; Beltman, J.; Clark, J. M.; Grothaus, P. G.; Bogyo, M.* and Baruch, A* “Development of Activity-based Probes for Trypsin-family Serine Proteases” Bioorg. Med. Chem. Lett. 2006, 16, 2882. Hansen, K.K.; Sherman, P.M.; Cellars, L.; Andrade-Gordon, P.; Pan, Z.; Baruch, A.; Wallace, J.L.; Hollenberg, M.D. and Vergnolle, N. “A Major Role for Proteolytic Activity and Proteinase-activated Receptor-2 in the Pathogenesis of Infectious Colitis” Proc. Natl. Acad. Sci. USA 2005, 102, 8363. Trost, B.M.*; Pan, Z.; Zambrano, J. and Kujat, C. “Polymer-supported C2-Symmetric Ligands for Palladium-Catalyzed Asymmetric Allylic Alkylation Reactions” Angew. Chem. Int. Ed. 2002, 41, 4691.