· 海南大学
研究生教育
    罗海彬
    2023年07月22日 10:02

罗海彬博士、海南大学二级教授、药学院院长,目前为国家重大人才工程获得者(2021年)、政府特殊津贴专家(2023)、 海南省B类人才(2021年)、广东医学-(2018年)、国家重点研发计划首席科学家(2017年)、广东省珠江学者(2016 年)、国家-(2015年)。2021年11月荣获国际超算“戈登贝尔”提名奖(药学界首次入围该奖,戈登贝尔奖是国际上高性能 计算应用领域的最高学术奖项),2019年荣获中国化学会青年计算化学家奖和2014年荣获中国药学会施维雅青年药物化学奖。20 20年11月荣获民革中央的“抗击新冠肺炎疫情新冠肺炎疫情先进个人”称号和广东民革省委会的“抗击新冠肺炎疫情先进个人”称号。1999年7月本科 毕业于厦门大学,2002年7月硕士毕业于厦门大学、2005年10月博士毕业于香港浸会大学,2006年12月-2020年12月工作于中山大学药 学院,先后担任副教授、教授和副院长。2021年1月起任海南大学药学院首任院长,筹建海南大学新药筛选与评价平台。多年来 主要从事新药研发工作(包括药物设计、有机合成、药物筛选和靶标验证等),已创制新冠肺炎治疗药物双嘧达莫和2个临床前 候选药物(已实现了成果转化)。

E-Mail:hbluo@hainanu.edu.cn,20817504@qq.com

1.教育背景

1995.09 - 2002.07

厦门大学化学系,学士、硕士

2002.10 - 2005.12

香港浸会大学化学系,博士


2.教学情况

主讲计算机辅助药物设计

3.科研情况

面向突发重大公共疫情和国家/军队的重大需求,聚焦于药物设计新方法、肺部炎症性疾病、皮肤类疾病新药研发,构建了基于自由能微扰的药/靶结合强度预测等核心算法,实现部分方法的新突破及国产化,成功应用于新冠肺炎、缺氧性肺动脉高压和肺纤维化等肺部炎症性疾病新药研发。创制了新冠肺炎治疗药物双嘧达莫、两个靶向磷酸二酯酶PDE临床前候选新药1607和LW33(两个均实现成果转化)、十个PDEs成药性候选分子。在Cell、Nat Sci Rev、PNAS、Acta Pharm Sin B、J Med Chem等国内外权威期刊发表150多篇论文;申请专利30多项;获批1项国家重点研发计划和6项国自然基金,科研经费超过3000万。

4.研究领域

药物设计新方法、PDE靶向药物

5.社会兼职

中国化学会计算机化学专业委员会委员

广东药学会药物化学专业委员会副主委兼秘书长

6.代表性项目

  • 国家自然科学基金面上项目:新型磷酸二酯酶PDE1选择性抑制剂的发现、成药性优化和抗肺纤维化作用研究,2021.01-2024.12

  • 国家自然科学基金面上项目:特异性识别磷酸二酯酶PDE8的黄嘌呤类衍生物:设计、抗血管性痴呆活性及作用机制研究,2019.01-2022.12

  • 国家重点研发计划:基于E 级高性能计算生物医药应用软件系统研制及应用 2017.07-2020.12

  • 国自然优秀青年基金,药物设计与发现,2016.01-2018.12

  • 广东省“珠江学者”特聘教授项目,2016.10-2021.09

  • 广州市科技机会科学研究重点项目,抗肺动脉高压首创药物2058对磷酸二酯酶PDE5变构位点的调节机制、结构优化和成药性研究,2019.04-2022.03,

7.代表性成果

2000年后,在Cell、Natl Sci Rev、PNAS、ACS Nano、ACS Catalysis、Acta Pharm Sin B、J Med Chem等国内外杂志发表论文150多篇(*表示为通讯作者)。

1)Discovery of novelphosphodiesterase-1 inhibitorsfor curing vascular dementia: Suppression of neuroinflammation by blocking NF-κB transcription regulation and activating cAMP/CREB axis. Zhou Q, Le M, Yang Y, Wang W, Huang Y, Wang Q, Tian Y, Jiang M, Rao Y,*Luo, H.-B*., Wu Y.*Acta Pharm. Sin. B.2023, 13(3): 1180-1191.

2)Structure-based discovery of orally efficient inhibitors via unique interactions with H-pocket ofPDE8for the treatment of vascular dementia. Wu XN, Zhou Q, Huang YD, Xie X, Li Z, Wu Y*,Luo, H.-B*.Acta Pharm. Sin. B.2022,12(7):3103-3112.

3)Structural Modifications of Nimodipine Lead to NovelPDE1 Inhibitorswith Anti-pulmonary Fibrosis Effects. Huang MX, Tian YJ, Han C, Liu RD, Xie X, Yuan Y, Yang YY, Li Z, Chen J*,Luo, H.-B*., Wu Y.*J. Med. Chem.2022, 65(12):8444-8455.

4)Wu D, Zheng X, Liu R, Li Z, Jiang Z, Zhou Q, Huang Y, Wu XN, Zhang C, Huang YY*,Luo, H.-B*. Free energy perturbation (FEP)-guided scaffold hopping.Acta Pharm. Sin. B.2022,12(3):1351-1362.

5)Xie G, Wu XN, Ling Y, Rui Y, Wu D, Zhou J, Li J, Lin S, Peng Q, Li Z, Wang H*,Luo, H.-B*. A novel inhibitor of N 6-methyladenosine demethylase FTO induces mRNA methylation and shows anti-cancer activities.Acta Pharm. Sin. B.202212(2):853-866.

6)Li, Z.; Li, H.; Yu, K.*;Luo, H.-B*. Perspective of drug design with high-performance computing.Natl. Sci. Rev.2021, 8(12), nwab105.

7)Huang YY, Deng J, Tian YJ, Liang J, Xie X, Huang Y, Zhu J, Zhu Z, Zhou Q, He X,*Luo H.-B.*Mangostanin Derivatives as Novel and Orally ActivePhosphodiesterase 4 Inhibitorsfor the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.J. Med. Chem.2021, 64(18):13736-13751.

8)Wu Y, Wang Q, Jiang MY, Huang YY, Zhu Z, Han C, Tian YJ, Zhang B,Luo, H.-B*.Discovery of PotentPhosphodiesterase-9 Inhibitorsfor the Treatment of Hepatic Fibrosis.J. Med. Chem.2021, 64(13):9537-9549.

9)Guo L, Wei RX, Sun R, Yang Q, Li GJ, Wang LY*,Luo H-B*,Feng M*. "Cytokine-microfactories" recruit DCs and deliver tumor antigens via gap junctions for immunotherapy.J. Control. Release.2021, 337:417-430.

10)Li, Z.; Li X.; Huang, Y.Y.; Wu, Y.; Liu, R.; Zhou, L.; Lin, Y.; Wu, D.; Zhang, L.; Liu, H.; Xu, X.; Yu, K.; Zhang, Y.; Cui. J*.; Zhan, C.G*.; Wang, X*.;Luo, H.-B*. Identify potent SARS-CoV-2 main protease inhibitors via accelerated free energy perturbation-based virtual screening of existing drugs.Proc. Natl. Acad. Sci. U S A.2020,117(44): 27381-27387.高被引论文。

11)Wu, Y.; Li, Z.; Zhao, Y.S.; Huang, Y.Y.; Jiang, M.Y.;Luo, H.-B*.Therapeutic targets and potential agents for the treatment of COVID-19.Med. Res. Rev.2021, 41(3):1775-1797.

12)Sun J, Xiao Z, Haider A, Gebhard C, Xu H,Luo H-B, Zhang HT, Josephson L, Wang L, Liang SH. Advances in Cyclic NucleotidePhosphodiesterase-Targeted PET Imaging and Drug Discovery.J. Med. Chem.2021, 64(11): 7083-7109.

13)Gao Y, Huang J, Zhou Q, Liu R, Zhang S, Zhang C, Huang YY, Li Z, Huang L, Wu D, Wu Y, Xiao L, Guo L*,Luo H-B.*Discovery of Highly Specific Catalytic-Site-Targeting Fluorescent Probes for Detecting LysosomalPDE10Ain Living Cells.ACS Chem. Biol.2021, 16(5):857-863.

14)Yang Y, Zhang S, Zhou Q, Zhang C, Gao Y, Wang H, Li Z, Wu D, Wu Y, Huang YY*, Guo L*,Luo H-B.* Discovery of highly selective and orally available benzimidazole-basedphosphodiesterase 10 inhibitorswith improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension.Acta Pharm. Sin. B.2020,10(12):2339-2347.

15)Huang, Y.; Wu, X.N.; Zhou, Q.; Wu. Y.; Zheng. D, Li, Z.; Guo, L.;Luo, H.-B*.Rational Design of 2-Chloroadenine Derivatives as Highly SelectivePhosphodiesterase 8A Inhibitors.J. Med. Chem.2020,63(24): 15852-15863.

16)Zhang T, Lai Z, Yuan S, Huang YY, Dong G, Sheng C*, Ke H*, Luo H.-B.* Discovery of Evodiamine Derivatives as Highly SelectivePDE5 InhibitorsTargeting a Unique Allosteric Pocket.J. Med. Chem.2020, 63(17):9828-9837.

17)Wu Y, Tian YJ, Le ML, Zhang SR, Zhang C, Huang MX, Jiang MY, Zhang B,Luo H-B.*Discovery of Novel Selective and Orally BioavailablePhosphodiesterase-1 Inhibitorsfor the Efficient Treatment of Idiopathic Pulmonary Fibrosis.J. Med. Chem.2020, 63(14): 7867-7879.

18)Jinhao Liang, Yi-You Huang, Qian Zhou, Yuqi Gao, Zhe Li, Deyan Wu, Si Yu, Lei Guo, Zhen Chen, Ling Huang, Steven H Liang, Xixin He*, Ruibo Wu*,Hai-Bin Luo.*Discovery and optimization of α-mangostin derivatives as novelPDE4 inhibitorsfor the treatment of vascular dementia,J. Med. Chem.2020, 63, 3370-3380

19)Xiaoyan Liu; Zhe Li; Shuai Liu; Jing Sun; Zhanghua Chen; Min Jiang; Qingling Zhang; Yinghua Wei; Xin Wang; Yi-You Huang; Yinyi Shi; Yanhui Xu; Huifang Xian; Fan Bai; Changxing Ou; Bei Xiong; Andrew M Lew; Jun Cui; Rongli Fang; Hui Huang; Jincun Zhao*; Xuechuan Hong*; Yuxia Zhang*; Fuling Zhou*;Hai-Bin Luo.*Potential therapeutic effects of dipyridamole to the severely ill , patients with COVID-19(12家机构参加本研究)Acta Pharm. Sin. B2020,10(7):1205-1215.高被引论文。

20)Ma, Y.; Ye, Z.; Zhang, C.; Wang, X.; Li, H.W.; Wong, M.S.;Luo, H.-B.*; Xiao, L.* Deep Red Blinking Fluorophore for Nanoscopic Imaging and Inhibition of β-Amyloid Peptide Fibrillation.ACS Nano.2020,14(9):11341-11351.

21)Li Z.; Zhao, Y.; Huifang Zhou, H.;Luo, H-B*.; Zhan, C.G.* Catalytic Roles of Coenzyme Pyridoxal-5′-phosphate (PLP) in PLP-Dependent Enzymes: Reaction Pathway for Methionine-γ-Lyase-Catalyzed l-Methionine Depletion.ACS Catalysis2020,10, 2198-2210.

22)Fan Zhang, Tianyue An, Xiaowen Tang, Jiachen Zi*,Hai-Bin Luo*,Ruibo Wu*. Enzyme Promiscuity versus Fidelity in Two Sesquiterpene Cyclases (TEAS versus ATAS).ACS Catalysis2020,10, 1470-1484.

23)Li, Z.; Huang, Y.; Wu, Y.; Chen, J.; Wu, D.; Zhan, C.G.*; Luo, H.-B*. Absolute Binding Free Energy Calculation and Design of a Subnanomolar Inhibitor ofPhosphodiesterase-10.J. Med. Chem.2019, 62, 2099-2111.

24)Wu, Y.; Zhou, Q.; Zhang,T.; Li, Z.; Chen, Y.P.; Zhang, P.; Yu, Y.F.; Geng, H.; Tian, Y.J.; Zhang, C.; Wang, Y.; Chen, J.W.*; Chen, Y. *;Luo, H.-B.*Discovery of Potent, Selective, and Orally Bioavailable Inhibitors againstPhosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.J. Med. Chem.2019,62, 4218-4224.

25)Huang, Y.Y.; Yu, Y.; Zhang, C.; Chen, Y.; Zhou, Q.; Li, Z.; Zhou, S.; Li, Z.; Guo, L.; Wu, D.*; Wu, Y.*;Luo, H-B*.Validation ofPhosphodiesterase-10as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.J. Med. Chem.2019, 62, 3707-3721.

26)Senling Feng; Huifang Zhou; Deyan Wu; Dechong Zheng; Biao Qu; Ruiming; Liu; Chen Zhang; Zhe Li; Ying Xie;*Hai-Bin Luo.*Nobiletin and its derivatives overcome multidrug resistance (MDR) in cancer: total synthesis and discovery of potent MDR reversal agents.Acta Pharm. Sin. B.2020, 10,327-343.

27)Wu, D.W.; Huang Y.; Chen, Y.; Huang, Y.; Geng, H.; Zhang, T.; Zhang, C.; Li, Z.; Guo, L.; Chen, J. W.;Luo, L.-B.*Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Highly Potent, Selective, and Orally BioavailablePDE5Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.J. Med. Chem.,2018, 61, 8468-8473.

28)Wu, D.W.; Zhang, T.H.; Chen, Y.; Huang, Y.; Geng, H.; Yu, Y.; Zhang, C., Lai, Z.W.; Wu, Y.; Guo, X.; Chen, J. W.*;Luo, L.-B.*Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally BioavailablePhosphodiesterase 5Inhibitors for the Treatment of Pulmonary Arterial Hypertension.J. Med. Chem.2017, 60(15): 6622-6637.

29)Wu, Y.; Li, Z.; Huang, Y.-Y.; Wu, D.Y.;Luo, L.-B.*NovelPhosphodiesterase Inhibitorsfor Cognitive Improvement in Alzheimer's Disease.J. Med. Chem.2018, 61 (13), 5467–5483.

30)Wu, X.N.; Huang, Y.D.; Li, J.X.; Yu, Y.F.; Qian, Z.; Zhang, C.; Wu Y*.;Luo H.-B.*Structure-based design, synthesis, and biological evaluation of novel pyrimidinone derivatives asPDE9inhibitors.Acta Pharm. Sin. B2018, 8(4), 615-628.

31)Huang, Y.; Liu, X.; Wu, D.; Tang, G.; Lai, Z.; Zheng, X. *; Yin. S. *;Luo, H.-B. *The discovery, complex crystal structure, and recognition mechanism of a novel naturalPDE4inhibitor fromSelaginella pulvinata.Biochem. Pharmacol.2017,130, 51-59.

32)Zhang, C.; Feng, L.J.; Huang, Y.; Wu, D.; Li, Z.; Zhou, Q.;Wu, Y. *;Luo, H.-B.*Discovery of NovelPhosphodiesterase-2A Inhibitorsby Structure-Based Virtual Screening, Structural Optimization, and Bioassay.J. Chem. Inf. Model.2017, 57, 355-364.

33)Li, Z.; Wu, Y., Feng, L.J.; Wu, R.*;Luo, H.-B.*Ab InitioQM/MM Study Shows a Highly Dissociated SN2 Hydrolysis mechanism for the cGMP-specificphosphodiesterase-5.J. Chem. Theory Comput.2015,10, 5448-5457.

34)Shao, Y.X.; Huang, M.; Cui, W.; Feng, L.J.; Wu, Y.; Cai, Y.; Li, Z.; Zhu, X.; Liu, P.; Wan, Y.;* Ke, H.*;Luo, H.-B.*Discovery of aphosphodiesterase-9Ainhibitor as a potential hypoglycemic agent.J. Med. Chem.2014,57, 10304-130313.

35)Shang, N.N.; Shao, Y.X.; Cai, Y.H.; Guan, M.; Huang, M.; Cui, W.; He, L.; Yu, Y.J.; Huang, L.; Li, Z.; Bu, X. Z.*; Ke, H.*;Luo, H.-B.*Discovery of 3-(4-hydroxybenzyl)-1-(thiophen-2-yl)chromeno[2,3-c]pyrrol-9(2H)-one as aphosphodiesterase-5inhibitor and its complex crystal structure.Biochem. Pharmacol.2014,89: 86-98.

36)Huang, Y.Y.; Li, Z.; Cai, Y.H.; Feng, L.J.; Wu, Y.; Li, X.;Luo, H.-B.*The molecular basis for the selectivity of tadalafil towardphosphodiesterase 5 and 6: A modeling study.J. Chem. Inf. Model.2013,53, 3044-3053. PMID: 24180640.

37)Li, Z.; Cai, Y.H.; Cheng, Y.K.; Lu, X.; Shao, Y.X.; Li, X.; Liu, M.; Liu, P.;Luo, H.-B.*Identification of novelphosphodiesterase-4Dinhibitors prescreened by molecular dynamics-augmented modeling and validated by bioassay.J. Chem. Inf. Model.2013, 53, 972-981.PMID: 23517293.

38)Meng, F.; Hou, J.; Shao, Y. X.; Wu, P. Y.; Huang, M.; Zhu, X.; Cai, Y. H.; Li, Z.; Xu, J.; Liu, P. Q.;Luo, H.-B.*;Wan, Y.*; Ke, H*. Structure-based discovery of highly selectivephosphodiesterase-9Ainhibitors and implications for inhibitor design.J. Med. Chem.2012, 55(19): 8549-8558. PMID: 22985069.

8.荣誉奖励

  • 中国药学会施维雅青年药物化学奖(2014)

  • 中国化学会青年计算化学家奖(2019)

  • 国际超算“戈登贝尔”提名奖(2021)

  • 联系地址:海南大学药学院
  • 联系电话/传真:0898-66254967
  • E-mail:yxyyb@hainanu.edu.cn
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