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药理学第一研究室
研究室简介
左建平研究组
丁健研究组
冷颖研究组
楼丽广研究组
俞强研究组
缪泽鸿研究组
耿美玉研究组
王逸平研究组
 您现在的位置:首页 > 机构设置 > 研究机构 > 研究室 > 药理学第一研究室 > 楼丽广研究组
楼丽广研究组
楼丽广研究组

    课题组现有19人,其中博士学位高级研究人员4人,大专及以上研究人员6人,博士后1人,博士生3人,硕士生5人。 

   

    抗肿瘤药物药理,尤其是抗肿瘤创新药物的临床前药效评价及作用机制研究。

 

实验室开展抗肿瘤创新药物药效、多药耐药性及作用机制研究。曾主持多项国家自然科学基金、科技部、中科院、上海市资助的项目。在国际核心期刊上发表多篇论文,申请多项国内、外专利,发现、发展多个有自主知识产权的抗肿瘤药物,其中喜诺替康已进入临床试验。

实验室建立分子、细胞、动物水平的抗肿瘤药物筛选及药效评价模型,开展抗肿瘤药物临床前药效学研究。目前实验室筛选细胞毒性药物、分子靶向药物(主要针对酪氨酸激酶如EGFR、VEGFR、Bcr-abl、c-Met等)以及免疫调节药物抗肿瘤活性,现有超过200多种不同类型的肿瘤细胞株,肿瘤类型包括白血病、脑胶质瘤、乳腺癌、非小细胞肺癌、小细胞肺癌、胃癌、结肠癌、肝癌、卵巢癌、前列腺癌、骨肉瘤、皮肤癌、黑色素瘤等。实验室同时还拥有国际接轨、系统、规范的抗肿瘤药物动物药效评价技术和模型,肿瘤模型几乎包括所有常见的肿瘤类型。实验室是“上海市抗肿瘤药物临床前药效研究技术平台”,已经利用该平台完成了80多个一类抗肿瘤创新药物的临床前研究,药物类型包括烷化剂、长春碱、蒽环类、受体酪氨酸激酶抑制剂(如EGFR、VEGFR、c-Met抑制剂)以及非受体酪氨酸激酶抑制剂(如Bcr-abl抑制剂)等;主要合作单位包括江苏恒瑞医药股份有限公司、江苏正大天晴药业股份有限公司、重庆复创医药研究有限公司,四川科伦药物研究院等。

实验室还开展肿瘤辅助用药的筛选以及临床前药效学研究,开展的项目包括止吐药、促红细胞生成、促中性粒细胞生成、促血小板生成药物的临床前研究。 

     

 近期发表的主要文章

1. Jie Zhao, Haitian Quan, Chengying Xie, Liguang Lou*. NL-103, a novel dual-targeted inhibitor of histone deacetylases and hedgehog pathway, effectively overcomes vismodegib resistance conferred by Smo mutations. Pharma Res Per, 2 (2), 2014, e00043.

2. Liping Sun, Haitian Quan, Chengying Xie, Lei Wang, Youhong Hu, Liguang Lou*. Phosphodiesterase 3/4 Inhibitor Zardaverine Exhibits Potent and Selective Antitumor Activity against Hepatocellular Carcinoma Both In Vitro and In Vivo Independently of Phosphodiesterase Inhibition. PLOS ONE 2014; e90627.

3. Jie Zhao, Haitian Quan, Yongping Xu, Xiangqian Kong, Lu Jin, Liguang Lou*. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes imatinib- and sunitinib- resistance of certain KIT mutants. Cancer Science 2014; 105:117-25.

4. Weiping Liu, Qingsong Ye, Jing Jiang, Liguang Lou*, Yongping Xu, Chengying Xie, Mingjin Xie. Cis-[Pt(II)(1R,2R-DACH)(3-Acetoxy- 1,1- cyclobutanedicarboxylato)]:a water-soluble,oxalate-free and stable analogue of oxaliplatin: synthesis, characterization and biological Valuations. ChemMedChem, 2013; 8(9):1465-7

5. Quanren Wang, Haitian Quan, Jie Zhao, Chengying Xie, Lei Wang, Liguang Lou*. RON confers lapatinib resistance in HER2-positive breast cancer cells. Cancer Letters 2013; 340:43-50

6. Weiping Liu, Xizhu Chen, Qingsong Ye, Shuqian Hou, Liguang Lou* and Chengying Xie. 3-Hydroxycarboplatin, a simple carboplatin derivative endowed withan improved toxicological profile. Platinum Metals Rev 2012; 56: 257–265.

7. Lei Wang, Yongping Xu, Li Fu, Yuanchao Li, Liguang Lou*. (5R)-5- hydroxytriptolide (LLDT-8), a novel immunosuppressant in clinical trials, exhibits potent antitumor activity via transcription inhibition. Cancer Letters, 2012:324:75-82

8. Qiong Wu, Haitian Quan, Yongping Xu, Yun Li, Youhong Hu, Liguang Lou*. p38 MAPK is required for the antitumor activity of the vascular disrupting agent DMXAA. J Pharmacol Exp Ther 2012; 341:709-17.

9. Cheng-Ying Xie, Yong-Ping Xu, Wei Jin, Li-Guang Lou*. Antitumor activity of lobaplatin alone or in combination with antitubulin agents in non-small cell lung cancer. Anti-Cancer Drugs 2012; 23:698-705.

10. Cheng-Ying Xie, Yong-Ping Xu, Hong-Bing Zhao, Li-Guang Lou*. A novel and simple hollow-fiber assay for in vivo evaluation of nonpeptidyl thrombopoietin receptor agonists. Exp Hematol 2012; 40: 386-92

11. Hongbing Zhao, Haitian Quan, Chengying Xie, Yongping Xu, Fuchun Xie, Youhong Hu, Liguang Lou*. YHHU0895, a novel synthetic small-molecule microtubule-destabilizing agent, effectively overcomes P-glycoprotein-mediated tumor multidrug resistance. Cancer Letters 2012; 314: 54-62.

12. Weiping Liu, Xizhu Chen, Qingsong Ye, Yongping Xu, Chengying Xie, Mingjin Xie, Qiaowen Chang, and Liguang Lou*. A Novel Water-Soluble Heptaplatin Analogue with Improved Antitumor Activity and Reduced Toxicity. Inorganic Chemistry 2011; 50:5324-5326

13. Fuchun Xie, Hongbing Zhao, Dewen Li, Hong Chen, Haitian Quan, Xiaojing Shi, Liguang Lou,* and Youhong Hu*. Synthesis and Biological Evaluation of 2, 4, 5-substituted Pyrimidines as a New Class of Tubulin Polymerization Inhibitors. J Med Chem 2011; 54:3200-3205.

14. Tian S, Quan H, Xie C, Guo H, Lu F, Xu Y, Li J*, Lou L*. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci 2011; 102:1374-1380.

15. Luo H, Quan HT, Xie C, Xu Y, Fu L, Lou L*. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia 2010; 24: 1807-9.

16. Xie F, Zhao H, Zhao L, Lou L*, Hu Y*. Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activity. Bioorg Med Chem Lett 2009; 19: 275-8.

17. Quan H, Liu H, Li C, Lou L*. 1,4-Diamino-2,3-dicyano-1,4-bis(methylthio) butadiene (U0126) enhances the cytotoxicity of combretastatin A4 independently of mitogen-activated protein kinase kinase. J Pharmacol Exp Ther. 2009 ; 330:326-33 

 

   实验室配有近300 m2实验场地,4个生物安全柜,8台二氧化碳培养箱,1台细胞自动计数仪,2台-80℃冰箱,2台-45 oC冰箱, 12台普通冰箱,1个Thermo层析柜,5个Statebourne液氮罐(Biorack 3000和Biorack 6000),1台Olympus荧光倒置显微镜,2台普通倒置显微镜,1台凝胶成像系统,2台水平离心机,5台台式高速离心机,1台冷冻离心机,1台Bio-teck 多功能酶标仪(吸收、荧光、化学发光),1台Bio-Rad普通PCR仪,1台real-time PCR仪,1台影像分析系统,1台全温震荡培养箱,19台与高速Internet相连的个人计算机,1台Symex Poch-100自动血球计数仪。另外,实验室还配有专用的SPF级动物房。

 

 
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