方美娟博士，副教授

个人简历

   方美娟博士，厦门大学药学院副教授、福建省高层次人才。教学上，主讲本科生《波谱解析》、《药物合成反应》、《药物化学实验》、《药学综合科研训练》等课程；科研上，主要研究方向是发现人类疾病关键靶标（例如核受体，蛋白激酶和表观遗传酶）的选择性小分子调控剂，探索这些功能小分子调控靶标干预疾病的作用机制，并对功能小分子进行药学研究（构效关系、药代动力学和毒理学研究），以期发展针对癌症等相关疾病的“靶向治疗”药物。现已发现肿瘤、急性肺损伤等炎症相关疾病的多个靶向治疗创新小分子候选药物，包括RXRa小分子配体BPA-B9，CDK9小分子抑制剂XPW1、XM-A32、XM-B19等，Nur77小分子调控剂XN-8b、ja、NB1、XN-lq53、DHA-EA等。主持国家自然科学基金青年项目、福建省自然科学基金等项目；作为主要研究者参与863子课题、十一五重大新药创制专项等研究项目。至2023年12月，方美娟博士作为第一通讯或共同通讯，在本专业领域重要刊物上发表SCI论文约六十多篇；同时作为主要发明人获授权中国专利十三个。

工作经历：

2011起，厦门大学药学院，副教授，硕导。

2014.06-2015.06， 美国加州大学旧金山分校， Research Associate。

2006-2011起，厦门大学药学院，药学系，讲师，硕导。

教育背景：

2001.9—2006.7  厦门大学化学化工学院，有机化学专业，理学博士

1997.9—2001.7  厦门大学化学化工学院化学系，理学学士

研究兴趣：

1）核受体调控剂：核受体RXRα，Nur77，RARγ等生物大分子是炎症，痤疮和肿瘤治疗的良好靶标。我们发现不饱和脂肪酸衍生物、(氮杂)吲哚衍生物、喹啉衍生物等可以充当核受体调节剂，产生抗癌、抗炎、减肥等作用。

2）蛋白激酶抑制剂和表观遗传酶调节剂：基于结构的药物设计方法发现新型的蛋白激酶（CDKs和CKs）抑制剂和表观遗传酶（乙酰基转移酶和甲基转移酶）调控剂，用于治疗各种疾病，包括癌症、HIV、神经性疾病等。

3）生物活性化合物的靶标确证和作用机制分析：以生物活性小分子为探针，基于转录组、蛋白质组学、代谢组学等组学技术，探索其靶向调控的生物学功能及其治疗疾病和产生毒性的潜在机制和靶标。

4）中草药药效物质的研究与开发：中草药药效物质的鉴定和结构优化。

近五年代表性论文（2019-2023，JCR一区论文）:

1. Jingbo Qin^#, Boning Niu^#, Xiaohui Chen^#, Cheng Hu, Sheng Lu, Hongsheng Li, Weihao Liu, Jiayi Li, Zihao Teng, Yinghuang Yang, Hongyu Hu, Yang Xu, Shuaidong Huo, Zhen Wu, Yingkun Qiu*, Hu Zhou*, and Meijuan Fang*. Discovery of 5 (Pyrimidin-2-ylamino) 1H indole-2-carboxamide Derivatives as Nur77 Modulators with Selective and Potent Activity Against Triple-Negative Breast Cancer. Journal of Medicinal Chemistry, 2023, 66: 15847−15866 (药化TOP期刊)

2. Zhijian Kuang^#, Kaiqiang Guo^#, Yin Cao^#, Mengxue Jiang, Chaojie Wang, Qiaoqiong Wu, Guosheng Hu, Mingtao Ao, Mingfeng Huang, Jingbo Qin, Taige Zhao, Sheng Lu, Cuiling Sun, Mingyu Li, Tong Wu^*, Wen Liu^* and Meijuan Fang^*. The novel CDK9 inhibitor, XPW1, alone and in combination with BRD4 inhibitor JQ1, for the treatment of clear cell renal cell carcinoma. British Journal of Cancer, 2023, 129:1915 – 1929. (Nature Index, TOP期刊)

3. Guiping Gao^#, Jiayi Li^#, Yin Cao, Xudan Li, Yuqing Qian, Xiumei Wang, Mengyu Li, Yingkun Qiu, Tong Wu^*, Liqiang Wang*, Meijuan Fang^*. Design, synthesis, and biological evaluation of novel 4,4′-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer. European Journal of Medicinal Chemistry, 2023, 261: 115858. (药化TOP期刊)

4. Hua Fang, Mengyu Li, Xiumei Wang, Weizhu Chen, Fengming He, Yiping Zhang, Kaiqiang Guo, Wenhui Jin, Baicun Li^*, Meijuan Fang^*. Discovery of new DHA ethanolamine derivatives as potential anti-inflammatory agents targeting Nur77. Bioorganic Chemistry, 2023, 141: 106887.

5. Hongyu Hu^#, Gang Lin^#, Fengming He, Jie Liu, Rong Jia, Kun Li, Wenbin Hong, Meijuan Fang^*, Jin-Zhang Zeng^*. Design, synthesis, and biological evaluation of carbonyl-hydrazine-1-carboxamide derivatives as anti-hepatic fibrosis agents targeting Nur77. Bioorganic Chemistry, 2023, 140: 106795.

6. Yuqing Qian^#, Siyu Zhou^#, Jiayi Li^#, Mingyuan Ma^#, Huanwen Chen, Yin Cao, Yuxiang Zhang, Chaoyu Sun, Kang Li, Yizhao Liu, Shutong Dai, Mingtao Ao, Meijuan Fang*, Zhen Wu*, Mingdong Li*. Discovery of 4-((3,4-dichlorophenyl)amino)-2-methylquinolin-6-ol derivatives as EGFR and HDAC dual inhibitors. European Journal of Pharmacology 960 (2023) 176114.

7. Fengming He^#, Jun Chen^#, Taige Zhao^#, Qiaoqiong Wu, Na Yin, Xiumei Wang, Yijing Zhong, Xiaodan Guo, YingKun Qiu, Baicun Li^*, Meijuan Fang^*, Zhen Wu^*. Design, synthesis, and evaluation of novel benzoylhydrazone derivatives as Nur77 modulators with potent antitumor activity against hepatocellular carcinoma, Journal of Enzyme Inhibition and Medicinal Chemistry, 2023, 38(1): 2227777.

8. Chaojie Wang^#, Fengming He^#, Ke Sun^#, Kaiqiang Guo, Sheng Lu, Tong Wu^*, Xiang Gao^*, Meijuan Fang^*. Identification and characterization of 7-azaindole derivatives as inhibitors of the SARS-CoV-2 spike-hACE2 protein interaction. International Journal of Biological Macromolecules, 2023, 244: 125182.

9. Chenli Chang, Fengming He, Mingtao Ao, Jun Chen, Tao Yu, Weiyu Li, Baicun Li*, Meijuan Fang*, and Ting Yang*. Inhibition of Nur77 expression and translocation by compound B6 reduces ER stress and alleviates cigarette smoke-induced inflammation and injury in bronchial epithelial cells. Frontiers in Pharmacology. 2023, 14: 1200110.

10. Jun Chen^#, Taige Zhao^#, Fengming He, Yijing Zhong, Susu Wang, Ziqing Tang, Yingkun Qiu, Zhen Wu^*, Meijuan Fang^*. Discovery of bipyridine amide derivatives targeting pRXRα-PLK1 interaction for anticancer therapy. European Journal of Medicinal Chemistry, 2023, 254: 115341. (药化TOP期刊)

11. Hua Fang^#, Yin Cao^#, JianYu Zhang, Xiumei Wang, Mengyu Li, Zhuan Hong, Zhen Wu, Meijuan Fang^*. Lipidome Remodeling Activities of DPA-EA in Palmitic Acid-Stimulated HepG2 Cells and The in vivo Anti-obesity Effect of the DPA-EA and DHA-EA Mixture Prepared from Algae Oil. Frontiers in Pharmacology,2023, 14: 1146276.

12. Fengming He^#, Xiumei Wang^#, Qiaoqiong Wu, Shunzhi Liu, Yin Cao, Xiaodan Guo, Sihang Yin, Na Yin, Baicun Li*, Meijuan Fang*, Identification of potential ATP-competitive cyclin-dependent kinase 1 inhibitors: De novo drug generation, molecular docking, and molecular dynamics simulation. Computers in Biology and Medicine, 2023, 155: 106645.

13. Mingtao Ao^#, Jun Wu^#, Yin Cao, Yaohui He, Yuxiang Zhang, Xiang Gao, Yuhua Xue*, Meijuan Fang*, Zhen Wu*, The synthesis of PROTAC molecule and new target KAT6A identification of CDK9 inhibitor iCDK9. Chinese Chemical Letters, 2023, 34: 107741.

14. Jingbo Qin^#, Xiaohui Chen^#, Weihao Liu^#, Jun Chen, Weirong Liu, Yongzhen Xia , Zhehui Li, Mingyu Li, Shaojuan Wang, Quan Yuan, Yingkun Qiu*, Zhen Wu*, Meijuan Fang*, Discovery of 5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-indole-2-carboxamide derivatives as novel anti-cancer agents targeting Nur77. European Journal of Medicinal Chemistry, 2022, 244: 114849. (药化TOP期刊)

15. Yuqing Qian^#, Mingtao Ao^#, Boqun Li^#, Zhijian Kuang, Xiumei Wang, Yin Cao, Jiayi Li, Yingkun Qiu, Kaiqiang Guo*, Meijuan Fang*, Zhen Wu*. Design and synthesis of N-(1-(6-(substituted phenyl)-pyridazin-3-yl)-piperidine-3-yl)-amine derivatives as JMJD6 inhibitors. Bioorganic Chemistry, 2022, 129: 106119.

16. Baicun Li^#, Jiangang Huang^#, Jie Liu^#, Fengming He, Fangfang Wen, Changming Yang, Wang Wang, Tong Wu, Taige Zhao, Jie Yao, Shunzhi Liu, Yingkun Qiu, Meijuan Fang*, Jinzhang Zeng*, Zhen Wu*. Discovery of a Nur77-mediated cytoplasmic vacuolation and paraptosis inducer (4-PQBH) for the treatment of hepatocellular carcinoma. Bioorganic Chemistry, 2022, 121: 105651.

17. Mingtao Ao^#, Jianyu Zhang^#, Yuqing Qian^#, Boqun Li, Xiumei Wang, Jun Chen, Yuxiang Zhang, Yin Cao, Yingkun Qiu, Yang Xu^*, Zhen Wu^* and Meijuan Fang^*. Design and synthesis of adamantyl-substituted flavonoid derivatives as anti-inflammatory Nur77 modulators: Compound B7 targets Nur77 and improves LPS-induced inflammation in vitro and in vivo. Bioorganic Chemistry, 2022, 120: 105645.

18. Jun Wu^#, Hongyu Hu^#, Mingtao Ao^#, Zhenzhen Cui, Xiaoping Zhou, Jingbo Qin, Yafei Guo, Jingwei Chen*, Yuhua Xue* and Meijuan Fang*. Design, synthesis, and biological evaluation of 5-((4-(pyridin-3-yl)pyrimidin-2-yl) amino)-1H-Indole-2-Carbohydrazide derivatives: the methuosis inducer 12A as a novel and selective anticancer agent. Journal of Enzyme Inhibition and Medicinal Chemistry, 2021, 36(1): 1436–1453.

19. Mingtao Ao^#, Xianwen Hu^#, Yuqing Qian^#, Boqun Li, Jianyu Zhang, Yin Cao, Yuxiang Zhang, Kaiqiang Guo, Yingkun Qiu, Fuquan Jiang*, Zhen Wu*, Meijuan Fang*. Discovery of new chalone adamantyl arotinoids having RXRα-modulating and anticancer activities. Bioorganic Chemistry, 2021, 113: 104961.

20. Baicun Li^#, Jie Yao^#, Fengming He^#, Jie Liu, Zongxin Lin, Shunzhi Liu, Wang Wang, Tong Wu, Jiangang Huang, Kun Chen, Meijuan Fang*, Jingwei Chen*, Jin-Zhang Zeng*. Synthesis, SAR study, and bioactivity evaluation of a series of Quinoline-Indole-Schiff base derivatives: Compound 10E as a new Nur77 exporter and autophagic death inducer. Bioorganic Chemistry, 2021, 113: 105008.

21. Jingbo Qin^#, Jie Liu^#,, Chunxiao Wu, Jianwen Xu, Bowen Tang, Kaiqiang Guo, Xiaohui Chen, Weihao Liu, Tong Wu, Hu Zhou*, Meijuan Fang*, Zhen Wu*. Synthesis and biological evaluation of (3/4-(pyrimidin-2-ylamino)benzoyl)-based hydrazine-1-carboxamide/carbothioamide derivatives as novel RXRα antagonists. Journal of Enzyme Inhibition and Medicinal Chemistry, 2020, 35(1): 880–896.

22. Hua Fang, Jianyu Zhang, Mingtao Ao, Fengming He, Weizhu Chen, Yuqing Qian, Yuxiang Zhang, Yang Xu*, Meijuan Fang*. Synthesis and discovery of ω-3 polyunsaturated fatty acid- alkanolamine (PUFA-AA) derivatives as anti-inflammatory agents targeting Nur77. Bioorganic Chemistry, 2020, 105: 104456.

23. Hongyu Hu^#, Jun Wu^#, Mingtao Ao^#, Xiaoping Zhou, Boqun Li, Zhenzhen Cui, Tong Wu, Lijuan Wang, Yuhua Xua⁎, Zhen Wu⁎, Meijuan Fang*. Design, synthesis and biological evaluation of methylenehydrazine-1-carboxamide derivatives with (5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-indole scaffold: Novel potential CDK9 inhibitors. Bioorganic Chemistry, 2020, 102: 104064.

24. Baicun Li^#, Jie Yao^#, Kaiqiang Guo^#, Fengming He, Kun Chen, Zongxin Lin, Shunzhi Liu, Jiangang Huang, Qiaoqiong Wu, Meijuan Fang*, Jinzhang Zeng*, Zhen Wu*. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. European Journal of Medicinal Chemistry, 2020, 204: 112608.（药化TOP期刊）

25. Baicun Li^#, Feifeng Zhu^#, Fengming He^#, Qingqing Huang, Xiaoguang Liu, Tong Wu, Taige Zhao, Yingkun Qiu, Zhen Wu, Yuhua Xue^⁎, Meijuan Fang^⁎. Synthesis and biological evaluations of N’-substituted methylene-4-(quinoline-4-amino) benzoylhydrazides as potential anti-hepatoma agents. Bioorganic Chemistry, 2020, 96: 103592.

26. Guozhang Lu, Jun Chen, Xinlei Huangfu,a Xueyan Li, Meijuan Fang,* Guo Tang* and Yufen Zhao. Visible-light-mediated direct synthesis of phosphorotrithioates as potent anti-inflammatory agents from white phosphorus. Organic Chemistry Frontiers, 2019, 6(2): 190-194.

27. Shanshan Shi, Jun Chen, Shaohua Zhuo, Zi’ang Wu, Meijuan Fang,* Guo Tang,* and Yufen Zhao. Iodide-Catalyzed Phosphorothiolation of Heteroarenes Using P(O)H Compounds and Elemental Sulfur, Advanced Synthesis & Catalysis,2019, 361, 3210–3216.

代表性专利：

1. 吴振，方美娟，刘文，钱宇卿，敖名涛，曹银，王秀美，李博群，张宇翔，N-(1-(6-(取代苯基)哒嗪-3-基)哌啶-3-基)胺/酰胺衍生物及制备方法，专利号：ZL 2022 1 0149370.6，专利授权日：2023年6月13日。

2. 吴振，郭凯强，方美娟，王超杰，吴巧琼，钱宇卿，刘伟豪，何凤明，高原；3-取代基-5-（取代芳基）-7-氮杂吲哚衍生物及其应用，专利号：202110554512.2，专利授权日：2022年4月12日。

3. 方美娟，吴振，郭凯强，王超杰，曹银，秦静波，陈静威，赵泰格；(1H-咪唑并[4,5-b]吡啶-6-基)吡啶衍生物及其应用，专利号：202010240017.X，专利授权日：2021年10月15日。

4. 吴振，周虎，方美娟，秦静波，牛播宁，王超杰，陈晓惠，唐博文，曹银，吕奔；嘧啶吲哚类Nur77受体调控剂及其制备方法和应用，专利号：201910105476.4；专利授权日：2021年04月09日。

5. 刘文，吴振，方美娟，李柏村，黄建刚，杨沫，唐博文，李博群，王浩杰，主父学良；一类4-（（2-取代喹啉-4-基）氨基）苯甲酰肼类衍生物及其制备方法与应用，专利号：201810253238.3；专利授权日：2020年11月10日。

6. 吴振，方美娟，秦静波，陈晓惠，唐博文，郭凯强；N-取代-5-（（4-取代嘧啶-2-基）氨基）吲哚类衍生物及其制备方法和用途，专利号：201710950061.8；专利授权日：2020年02月14日。

7. 吴振，方美娟，秦静波，胡鸿雨，林春蓉，钱宇卿；1-(2-(碳酰肼取代基团)-1H-吲哚-5-基)-3-取代脲衍生物及制备方法，专利号：2015107498281；专利授权日：2019年02月05日。

8. 吴振，周强，方美娟，薛玉花，胡鸿雨，吴俊，廖超，王慧茹；1H-吲哚-2-碳酰肼衍生物及其制备方法和用途，专利号：201510269949.6；专利授权日：2018年07月17日。

9. 吴振，周强，方美娟，薛玉花，胡鸿雨，吴俊，廖超，王慧茹；5-(取代碳酰氨基)-1H-吲哚-2-碳酰肼衍生物及其制备方法和应用，专利号： 201510269973.X；专利授权日：2018年07月17日。

10. 吴振，方美娟，曾锦章，胡鸿雨，林春蓉，敖名涛，钱宇卿；1-(2-(金刚烷-1-基)-1H-吲哚-5-基)-3-取代脲衍生物及制备和用途，专利号：201510749625.2；专利授权日：2018年04月10日

11. 吴振，周强，方美娟，薛玉花，敖名涛，吴俊，何焯，纪玉峰，余雕，钱宇卿；一系列查尔酮、二氢查尔酮和黄酮化合物及其制备方法和用途，专利号：ZL 201510278231.3；专利授权日：2017年06月23日.

12. 吴振，方美娟，周强，薛玉花，敖明涛，吴俊，何焯，纪玉峰；一类查尔酮衍生物及其制备方法和用途，专利号：201410056278.0；专利授权日：2015年09月02日。

13. 方美娟，唐果，郑振宇，吴振，赵玉芬，一类布雷菲德菌素A的碳酸酯类化合物及其制备方法和用途，专利号：ZL 2014 1 0056393.8；2015年05月13日。

    
    

联系方式：

地址：福建省厦门市翔安区翔安南路，厦门大学药学院205室

Email: fangmj@xmu.edu.cn