简单介绍

          罗海彬 博士、教授、博士生导师,中山大学药学院副院长,国家重点研发计划首席科学家,广东省“珠江学者”特聘教授,国家自然科学基金优秀青年基金获得者,中国药学会-施维雅青年药物化学奖获得者SCI期刊Chem Biol Drug Des、药学学报(英文版)、药学研究编委。罗博士,1977年出生,1999年于厦门大学获学士学位; 2005年于香港浸会大学获博士学位;200612月中山大学"百人计划"引进为药学院副教授;201112月晋升为教授,2012年被聘为药学院院长助理,2014年被聘为药学院副院长,2015年获得国家自然科学基金优秀青年基金支持,2016年入选广东省“珠江学者”特聘教授罗博士主要从事药物化学和结构生物学等方面的研究。多年来从事抗老年性痴呆、肺动脉高压、糖尿病、哮喘等药物靶标结构生物学和发现研究,重点构建基于靶标磷酸二酯酶(PDE)的药物筛选体系,并进行相关的药物分子设计、有机合成和作用机制研究。

         2000年以来, CellJ Med ChemChem CommunOrg LettJ Chem Theory ComputBiochem PharmJ Chem Inf Model等国内外杂志发表100多篇论文。已主持五项国家级、七项省部级和两项市局级项目, 七项发明专利授权和两项PCT专利。

 

研究方向

药物化学和结构生物学

 

教育经历

  • 1995.09-1999.07    厦门大学化学系,学士    

  • 1999.09-2002.07    厦门大学化学系,硕士    

  • 2002.10-2005.12    香港浸会大学化学系,博士    

 

工作经历

  • 2005.12-2006.12    香港浸会大学化学系,博士后

  • 2006.11-2011.12    中山大学药学院,“百人计划”引进,副教授,药物化学    

  • 2008.07-2008.10    弗吉尼亚大学医学院,访问学者    

  • 2009.06-2009.09    弗吉尼亚大学医学院,访问学者    

  • 2011.12-迄今    中山大学药学院,教授    

  • 2012.06-2014.04    中山大学药学院,院长助理    

  • 2012.08-迄今    中山大学药学院,博导    

  • 2014.04-迄今    中山大学药学院,副院长    

社会/学术任职

  1. 中国化学会计算机化学专业委员会委员

  2. 广东省高性能计算协会常务理事

  3. 广东省药物化学专业委员会副主委兼秘书长

  4. SCI期刊Chem Biol Drug Des、药学学报(英文版)、药学研究编委

科研项目

  1. 国家重点研发计划高性能计算专项,基于E级计算的高性能生物医药软件系统的研制与应用,2017.07-2020.122.

  2. 国家自然科学基金优秀青年基金项目:药物设计与发现,2016.01-2018.123.

  3. 广东省“珠江学者”特聘教授项目,2016.10-2021.094.

  4. 国家自然科学基金面上项目:新型抗肺动脉高压PDE5高选择性抑制剂的结构优化和分子机制研究,2016.01-2019.125.

  5. 国家自然科学基金面上项目: 选择性识别磷酸二酯酶PDE9的嘧啶酮类衍生物:设计、合成与分子机制研究, 2013.01-2017.126.

  6. 广东省自然科学基金团队项目:基于靶标磷酸二酯酶结构的先导物筛选及其临床前研究,分题主持,2011.10-2016.097.

  7. 教育部博士点基金: 磷酸二酯酶PDE9高选择性抑制剂的设计和构效关系研究,2014.01-2016.12

     

论著专利

      2000年后,在Cell、J Med Chem、Chem Commun、Org Lett、J Chem Theory Comput、Biochem Pharm、J Chem Inf Model、J Chromatogr A、J Nat Prod、J Struct Biol等国内外杂志发表论文100多篇(*表示为论文通讯作者)。

 

 [1]        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 Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension. J. Med. Chem. 2017, DOI: 10.1021/acs.jmedchem.7b00523.

 [2]        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 natural PDE4 inhibitor from Selaginella pulvinata. Biochem. Pharmacol. 2017, 130, 51-59.

 [3]        Zhang, C.; Feng, L.J.; Huang, Y.; Wu, D.; Li, Z.; Zhou, Q.; Wu, Y. *; Luo, H.-B.* Discovery of Novel Phosphodiesterase-2A Inhibitors by Structure-Based Virtual Screening, Structural Optimization, and Bioassay. J. Chem. Inf. Model. 2017, 57, 355-364.

 [4]        Cai, Y. H. #; Guo, Y. #; Li, Z.; Wu, D.; Li, X.; Zhang, H.; Yang, J.; Lu, H.; Sun, Z.; Luo, H.-B.; Yin, S.*; Wu, Y*. Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4. Eur. J. Med. Chem. 2016, 114, 134-140.

 [5]        Wu, Y.; * Cheng, J.; Wu, D.; Gu, Q.; Luo, Z.Y.; Luo, H.-B.* Palladium-catalyzed C–H bond carboxylation of acetanilides: an efficient usage of N,N-dimethyloxamic acid as the carboxylate source. Chem. Commun. 2016, 52, 1286-1289. PMID: 26616015

 [6]        Su, T.; Zhang, T.; Xie, S.; Yan, J.; Wu, Y.; Li, X.; Huang, L.*; Luo, H.-B. *. Discovery of novel PDE9 inhibitors capable of inhibiting Aβ aggregation as potential candidates for the treatment of Alzheimer's disease. Sci. Rep. 2016, 6:21826. PMID: 26911795

 [7]        Wu, Y.*; Sun, L.; Chen, Y.; Zhou, Q.; Huang, J.W.; Miao, H.; Luo, H.-B.* Palladium-Catalyzed Decarboxylative Acylation of N-Nitrosoanilines with α-Oxocarboxylic Acids. J. Org. Chem. 2016, 81(3):1244-1250. PMID: 26746881

 [8]        Li, Z.; Wu, Y., Feng, L.J.; Wu, R.*; Luo, H.-B.* Ab Initio QM/MM Study Shows a Highly Dissociated SN2 Hydrolysis mechanism for the cGMP-specific phosphodiesterase-5. J. Chem. Theory Comput. 2015, 10, 5448-5457.

 [9]        Huang, M.; Shao, Y.; Hou, J.; Cui, W.; Liang, B.; Huang, Y.; Li, Z.; Wu, Y.; Zhu, X.; Liu, P.; Wan, Y.*; Ke. H.*; Luo, H.-B.* Structural Asymmetry of Phosphodiesterase-9A and a Unique Pocket for Selective Binding of a Potent Enantiomeric Inhibitor. Mol. Pharmacol. 2015, 88(5):836-845. PMID: 26316540

[10]        Zhou, J.; Wu, R.*; Luo, H.-B.* Inhibition mechanism of SAHA in HDAC: a revisit. Phys. Chem. Chem. Phys. 2015, 17(44):29483-29488. PMID: 26497064

[11]        Li, Z.; Lu, X.; Feng, L.J.; Gu, Y.; Li, X.; Wu, Y.;* Luo, H.-B.* Molecular dynamics-based discovery of novel phosphodiesterase-9A inhibitors with non-pyrazolopyrimidinone scaffolds. Mol. Biosyst. 2015, 15, 115-125. PMID: 25328054.

[12]        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 a phosphodiesterase-9A inhibitor as a potential hypoglycemic agent. J. Med. Chem. 2014, 57, 10304-130313. PMID: 25432025.

[13]        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 a phosphodiesterase-5 inhibitor and its complex crystal structure. Biochem. Pharmacol.2014, 89: 86-98. PMID:24565909

[14]        Wu, Y.; Feng, L.J.; Lu, X.; Kwong, F.Y.*; Luo, H.-B.* Palladium-catalyzed oxidative C-H bond acylation of N-nitrosoanilines with toluene derivatives: a traceless approach to synthesize N-alkyl-2-aminobenzophenones. Chem. Commun. 2014, 50(97), 15352-15354. PMID: 25348462

[15]        Zhou, J., Xie, H.; Liu, Z.;Luo, H.-B.*; Wu, R.* Structure-Function Analysis of the Conserved Tyrosine and Diverse π-Stacking among Class I Histone Deacetylases: A QM (DFT)/MM MD Study. J. Chem. Inf. Model. 2014, 54(11), 3162-3171. PMID: 25360823

[16]        Liu, X.(#); Luo, H.-B.(#,并列第一作者); Huang, Y.Y.; Bao, J.M.; Tang, G.H.; Chen, Y.Y.; Wang, J.; Yin, S. Selaginpulvilins A-D, New phosphodiesterase-4 inhibitors with an unprecedented skeleton from Selaginella Pulvinata. Org. Lett. 2014, 162, 282-285. PMID: 24328835.

[17]        Cheng, Z.B.; Lu, X.; Bao, J. M.; Han, Q.; Tang, G.H.; Gan, L.S. *; Luo, H.-B.*; Yin, S.* (±)-Torreyunlignans A.D, Rare 8-9’ Linked Neolignan Enantiomers as Phosphodiesterase-9A Inhibitors from Torreya yunnanensis. J. Nat. Prod. 2014, 77, 2651−2657.

[18]        Cheng, Z.B.; Deng, Y.L.; Fan, C.Q.; Han, Q.H.; Lin, S.L.; Tang, G.H.; Luo, H.-B.*; Yin, S.* Prostaglandin Derivatives: Nonaromatic Phosphodiesterase-4 Inhibitors from the Soft Coral Sarcophyton ehrenbergi. J. Nat. Prod. 2014, 77, 1928–1936. PMID: 25075977

[19]        Lin, T.T.; Huang, Y.Y.; Tang, G.H.; Cheng, Z.B.; Liu, X.; Luo, H.-B.*; Yin, S.* Prenylated Coumarins: Natural Phosphodiesterase-4 Inhibitors from Toddalia asiatica. J. Nat. Prod. 2014, 77: 955-962. PMID:24597921

[20]        Liu, Y.N.; Huang, Y.Y.; Bao, J.M.; Cai, Y.H.; Guo, Y.Q.; Liu, S.N.; Luo, H.-B.*; Yin, S.* Natural phosphodiesterase-4 (PDE4) inhibitors from Crotalaria Ferruginea. Fitoterapi 2014, 94: 177-182. PMID:24594242

[21]        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 toward phosphodiesterase 5 and 6: A modeling study. J. Chem. Inf. Model. 2013, 53, 3044-3053. PMID: 24180640.

[22]        Li, Z.; Cai, Y.H.; Cheng, Y.K.; Lu, X.; Shao, Y.X.; Li, X.; Liu, M.; Liu, P.; Luo, H.-B.* Identification of novel phosphodiesterase-4D inhibitors prescreened by molecular dynamics-augmented modeling and validated by bioassay. J. Chem. Inf. Model. 2013,53, 972-981.PMID: 23517293.

[23]        Zhao, P.; Chen, S.K.; Cai, Y.H.; Lu, X.; Li, Z.; Cheng, Y.K.; Zhang, C.; Hu, X.; He, X.*; Luo, H.-B.* The molecular basis for the inhibition of phosphodiesterase-4D by three natural resveratrol analogs. Isolation, molecular docking, molecular dynamics simulations, binding free energy, and bioassay. Biochim Biophys Acta. 2013, 1834(10): 2089-2096. PMID: 23871879.

[24]        Zhong, J.; Huang, Y.; Ding, W.; Wu, X.; Wan, J.*; Luo, H.-B.* Chemical constituents of Aloe barbadensis Miller and their inhibitory effects on phosphodiesterase-4D. Fitoterapia. 2013, 91:159-165. PMID: 24028970.

[25]        Li, Y.P.; Weng, X.; Ning, F.X.; Ou, J.B.; Hou, J.Q.; Luo, H.-B.*; Li, D.; Huang, Z.S.; Huang, S.L.*; Gu, L.Q. 3D-QSAR studies of azaoxoisoaporphine, oxoaporphine, and oxoisoaporphine derivatives as anti-AChE and anti-AD agents by the CoMFA method. J. Mol. Graph. Model. 2013, 41: 61-67. PMID: 23500628.

[26]        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 selective phosphodiesterase-9A inhibitors and implications for inhibitor design. J. Med. Chem. 2012, 55(19): 8549-8558. PMID: 22985069.

[27]        Park, S.J.; Ahmad, F.; Philp, A.; Baar, K.; Williams, T.; Luo, H.B.; Ke, H.M.; Rehmann, H.; Taussig, R.; Brown, A.L.; Kim, M.K.; Beaven, M.A.; Burgin, A.B.; Manganiello, V.; Chung, J.H. Resveratrol ameliorates aging-related metabolic phenotypes by inhibiting cAMP phosphodiesterases. Cell 2012, 148(3): 421-433. PMID: 22304913.

[28]        Chen, S.-K.; Zhao, P.; Shao, Y.-X.; Li, Z.; Liu, M.; Zhang, C.X.; Liu, P.Q.; He, X.X.*; Luo, H.-B.*; Hu, X.P. Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor. Bioorg. Med. Chem. Lett. 2012, 22: 3261–3264. PMID:22483586

[29]        Zheng, X.H.; Shao, Y.X.; Li, Z.; Liu, M.; Bu, X.Z.; Luo, H.-B.*; Hu, X.P. Quantitative structure-retention relationship of curcumin and its analogues. J. Sep. Sci. 2012, 35: 505-512. PMID:22282411

[30]        Shao, Y.X; Zhao, P.; Li, Z.; Liu, M.; Liu, P.Q.; Huang, M.; Luo, H.-B.* The molecular basis for the inhibition of human cytochrome P450 1A2 by oroxylin and wogonin. Eur. Biophys. J. 2012, 41: 297-306.

[31]        Zheng, X.H.; Zhang, L.P.; Zhai, J; Chen, Y.Y.; Luo, H.-B.*; Hu, X.P.* The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Lett. 2012, 586: 55-59. PMID:22228220

[32]        Fang, J.; Huang, D.; Zhao, W.; Ge, H.;Luo, H.-B.*; Xu, J.* A new protocol for predicting novel GSK-3 beta ATP competitive inhibitors. J. Chem. Inf. Model. 2011, 51: 1431-1438.

[33]        Hou, J.; Xu, J.; Liu, M.; Zhao, R.; Luo, H.-B.*; Ke, H.* Structural asymmetry of phosphodiesterase-9, potential protonation of a glutamic acid, and role of the invariant glutamine. PLoS ONE 2011, 6. e18092.

[34]        Liu, M.; Yuan, M.G.; Li, Z.; Cheng, Y.K.; Luo, H.-B.*; Hu, X.P.* Structural investigation into the inhibitory mechanisms of indomethacin and its analogues towards human glyoxalase I. Bioorg. Med. Chem. Lett. 2011, 21: 4243-4247.

[35]        Chen, Y.Y.; Chen, G.W.; Luo, H.-B.* Molecular insight into the inhibitory mechanism of galangin towards human cytochrome P450 1A2. A modeling study. Lett. Drug Des. Discov. 2011, 8: 216-222.

[36]        Luo, H.-B.; Zheng, H.-P.; et al. Crystal structure and molecular modeling study of N-carbamoylsarcosine amidase Ta0454 from Thermoplasma acidophilum. J. Struct. Biol.2010, 169: 304-311.

[37]        He, L; He, F.; Bi, H.C.; Li, J.K.; Zeng, S.;Luo, H.-B.*; Huang, M. Isoform-selective inhibition of chrysin towards human cytochrome P450 1A2. Kinetics analysis, molecular docking, and molecular dynamics simulations. Bioorg. Med. Chem. Lett.2010. 20: 6008-6012.

[38]        Liu, M.; He, L.; Hu, X.P.; Liu, P.Q.; Luo, H.-B.* 3D-QSAR, homology modeling, and molecular docking studies on spiropiperidines analogues as agonists of nociceptin/orphanin FQ receptor. Bioorg. Med. Chem. Lett. 2010, 20: 7004-7010.

[39]        Liu, M.; Yuan, M.G.; Luo, M.X.; Bu, X.Z.; Luo, H.-B.*; Hu, X.P.* Binding of curcumin with glyoxalase I: Molecular docking, molecular dynamics simulations, and kinetics analysis. Biophys. Chem. 2010, 147: 28-34.

 

获奖情况

中国药学会施维雅青年药物化学奖