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陆小云

发布时间:2018-03-12 发布单位:药学院

      1、个人简介:

陆小云,博士研究生,研究员,博士生导师,国家优秀青年基金获得者。20056月毕业于中国药科大学制药工程专业,获学士学位,20106月毕业于中国药科大学药物化学专业,获理学博士学位,20107-20162月在中国科学院广州生物医药与健康研究院从事科研工作,20163月加入暨南大学药学院,从事教学科研工作。。

2、讲授课程:

1)《Medicinal Chemistry》国际学院

2)《药物化学专论》

3)《有机化学实验》

3、研究方向:

1)新型激酶抑制剂的发现研究

2)诱导耐药突变激酶抑制剂的发现研究

3)激酶抑制剂的计算设计方法研究

4、主要学术兼职:

1)担任广东省药物化学专业委员会委员

2)担任Acta Pharmaceutica Sinica B》期刊青年编委

3担任《Chinese Chemical Letters》期刊青年编委

5、主要获奖情况:

1广东省自然科学二等奖2017

2广州市科技进步一等奖2016

6、代表性科研项目:

1)国家自然科学优秀青年基金(81922062),基于肺部疾病的靶向药物研究(2020.1-2022.12

2)国家重大研发计划国际合作项目(2018YFE0105800),新型抗肝癌药物FGFR4 选择性抑制剂的研究项目名称(2019.08- 2022.07

3)国家自然科学基金面上项目 (81874285),FGFR4降解剂的设计合成及其抗肝癌活性研究(2019.01 - 2022.12

7、代表性论文和专著:

(1)Zuqin Wang#, Jie Wang#, Yongjin Wang#, Shuang Xiang , Xiaojuan Song , Zhengchao Tu , Yang ZhouZhi-Min Zhang*, Zhang Zhang*, Ke Ding*, Xiaoyun Lu*.Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance. J. Med. Chem. 2022,10.1021/acs.jmedchem.2c00308.

(2)Hao Chen#, Mengzhen Lai #, Tao ZhangYuqing ChenLinjiang TongSujie Zhu , Yang ZhouXiaomei RenJian DingHua Xie*, Xiaoyun Lu *Ke Ding*. Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations. J. Med. Chem. 2022, doi: 10.1021/acs.jmedchem.2c00168.

(3)Min Shao#, Xiaojuan Chen,# Fang Yang, Xiaojuan Song, Yang Zhou, Qianmeng Lin, Ying Fu, Raquel Ortega, Xiaojing Lin, Zhengchao Tu, Adam V. Patterson, Jeff B. Smaill*, Yongheng Chen*, and Xiaoyun Lu*. Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4. J. Med. Chem. 2022, 65, 5113−5133

(4)Xiaoyun Lu*, Jeff B Smaill, Adam V Patterson, Ke Ding. Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors. J Med Chem. 2022, 65, 58-83.

(5)Fang Yang, Yalei Wen, Chaofan Wang, Yuee Zhou, Yang Zhou, Zhi-Min Zhang, Tongzheng Liu*, Xiaoyun Lu*. Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC. Eur J Med Chem. 2022, 230, 114088.

(6)Zuqin Wang, Ting Ran, Fang Xu, Chang Wen, Shukai Song, Yang Zhou*, Hongming Chen*, Xiaoyun Lu*. Deep learning-driven scaffold hopping in the discovery of Akt kinase inhibitors. Chem Commun (Camb). 2021, 57, 10588-10591.

(7)Liang Jiang, Yuting Wang, Qian Li, Zhengchao Tu, Sihua Zhu, Sanfang Tu*, Zhang Zhang*, Ke Ding*, Xiaoyun Lu*. Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Acta Pharm Sin B. 2021, 11, 315-1328.

(8)Xiaoyun Lu*, Jeff B. Smaill, Ke Ding*, Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. J Med. Chem. 2020, 63, 19, 10726–10741.

(9)Xiaoyun Lu*, Jeff B. Smaill, and Ke Ding*, New Promise and Opportunities for Allosteric Kinase Inhibitors. Angew. Chem. Int. Edit., 2020, 59, 13764-13776.

(10)Jianzhang Yang, Marthandam Asokan Shibu, Lulu Kong, Jinfeng Luo, Farheen BadrealamKhan, Yanhui Huang, Zheng-Chao Tu, Cai-Hong Yun, Chih-Yang Huang, Ke Ding*, Xiaoyun Lu*.Design, Synthesis and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as new Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. J. Med. Chem. 2020, 63, 2114-2130.

8、联系方式:

联系邮箱:luxy2016@jnu.edu.cn