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余志义 教授

余志义,博士,国精产品满18岁教授,药物化学及分子药理学专业博士生导师。2018年获得山东大学“齐鲁青年学者”称号。

Tel:+86-13605416337

Email:zhiyi_yu@sdu.edu.cn

通讯地址:山东省济南市文化西路44号,国精产品满18岁

研究领域

1. 钾离子通道变构调节剂的发现、优化及其转化应用研究

2. 以半胱氨酸环受体(Cys-loop receptors)为靶点的新型神经系统类药物的设计、合成及其药理活性研究

3. 药物与靶标蛋白相互作用的动力学常数(如:residence time,kon,koff等)测定及其药理学机制研究

4. 基于分子探针、蛋白质组学以及计算机模拟技术的药物靶点(target deconvolution)及其活性结合位点(binding site identification)的鉴定

工作及学习经历

2019.06 -至今, 国精产品满18岁,药物化学系,教授、博士生导师

2015.10 - 2019.06,美国哈佛大学医学院, 神经生物系, 博士后研究员

2011.09 - 2015.10,荷兰莱顿大学药物研究中心, 药物化学及分子药理学专业, 博士

2008.09 - 2011.06,四川大学华西药学院, 药物化学专业, 硕士

2004.09 - 2008.06,四川大学华西药学院, 药学专业, 学士

承担课题

1. 山东大学“齐鲁青年学者”科研启动基金

2. 国家自然科学基金青年科学基金项目 hERG钾离子通道变构调节剂的发现、优化及药理活性研究 2020.01-2022.12

代表性学术论文(限10篇)

1. Z. Yu, D.C. Chiara, P.Y. Savechenkov, K.S. Bruzik KS, J.B. Cohen, A photoreactive analog of allopregnanolone enables identification of steroid-binding sites in a nicotinic acetylcholine receptor,Journal of Biological Chemistry, 294(19): 7892-7903 (2019)

2. M. McGrath,Z. Yu, S.S. Jayakar, C. Ma, M. Tolia, X. Zhou, K.W. Miller, J.B. Cohen, D.E. Raines, Etomidate and etomidate analog binding and positive modulation of γ-aminobutyric acid type A receptors: Evidence for a state-dependent cutoff effect,Anesthesiology129(5):959-969 (2018)

3. L. Sala,Z. Yu, D. Ward-van Oostwaard, J.P. van Veldhoven, A. Moretti, K.-L. Laugwitz, C.L. Mummery, A.P. IJzerman, M. Bellin, A new hERG allosteric modulator rescues genetic and drug-induced long-QT syndrome phenotypes in cardiomyocytes from isogenic pairs of patient induced pluripotent stem cells,EMBO Molecular Medicine8(9):1065-1081 (2016)

4. Z. Yu, J.B. Cohen, Enantiomeric barbiturates bind distinctinter-andintra-subunit binding sites in a nicotinic acetylcholine receptor (nAChR),Journal of Biological Chemistry292(42):17258-17271 (2017)

5. Z. Yu, J. Liu, J.P. van Veldhoven, A.P. IJzerman, M.J. Schalij, D.A. Pijnappels, L.H. Heitman, A.A. de Vries, Allosteric modulation of Kv11.1(hERG) channels protects against drug-induced ventricular arrhythmias,Circulation: Arrhythmia and Electrophysiology9(4):e003439 (2016)

6. Z. Yu, J.P. van Veldhoven, J. Louvel, I.M. ’t Hart, M.B. Rook, M.A. van der Heyden, L.H. Heitman, A.P. IJzerman, Structure-affinity relationships (SARs) and structure-kinetics relationships (SKRs) of Kv11.1 blockers,Journal of Medicinal Chemistry58(15):5916-5929 (2015)

7. Z. Yu, J.P. van Veldhoven, I. ME't Hart, A.H. Kopf, L.H. Heitman, A.P. IJzerman, Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel,European Journal of Medicinal Chemistry106:50-59 (2015)

8. Z. Yu, A.P. IJzerman, L.H. Heitman, Kv11.1(hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv11.1(hERG) inhibitors,British Journal of Pharmacology172(3):940-955 (2015)

9. Z. Yu, E. Klaasse, L.H. Heitman, A.P. IJzerman, Allosteric modulators of the hERG K+channel: Radioligand binding assays reveal allosteric characteristics of dofetilide analogs,Toxicology and Applied Pharmacology274(1):78-86 (2014)

10.Z. Yu, G. Shi, Q. Sun, H. Jin, Y. Teng, K. Tao, G. Zhou, W. Liu, F. Wen, T. Hou, Design, synthesis andin vitroantibacterial/antifungal evaluation of novel 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl) quinoline-3-carboxylic acid derivatives,European Journal of Medicinal Chemistry44(11):4726-4733 (2009)

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