杨忠金，副研究员，2013~2016年攻读南开大学博士研究生，主要研究课题为抗肿瘤干细胞天然产物小白菊内酯的全合成和构效关系探索。 曾分别就职于天津药明康德药物合成部（组长，2011-2013年）和凯莱英医药集团项目工艺研发中心（项目主管，2016-2017年）。2017年就职于广州医科大学，目前主要方向是抗肿瘤及免疫微环境调控的小分子药物发现及药物合成工艺研究。在J. Med. Chem.、Eur. J. Med. Chem.、Bioorg. Med. Chem. Lett. 、Free Radical Bio. Med.、Int. Immunopharmacol.等杂志上发表论文多篇；申请专利8项；承担国家自然科学基金1项。

联系邮箱:306645457@qq.com

研究方向:药物化学生物学；药物合成工艺

主要科研项目

1. 主持国家自然科学基金青年项目（81803364）。项目名称：Smad3磷酸化抑制剂SIS3的构效关系及抗肿瘤靶标探索

2. 主持广州市科技计划项目 (202102020546)。项目名称：基于PROTAC技术降解Smad3蛋白的药物设计及其对肺癌的治疗

3. 主持表观遗传药物研发培育计划项目 (06-410-2107213)。项目名称：选择性抑制 Smad3 蛋白的药物设计及其对免疫稳态失调相关疾病的治疗作用

4. 参与国家自然科学基金面上项目（81872743）。项目名称：神经胶质细胞调节剂AD110延缓阿尔茨海默氏症的作用及机制研究

主要论文及著作（代表性）

1) Xinyi Wu#, Ping Sun#, Xiuhui Chen#, Lei Hua, ……, Wenhui Hu*, and Zhongjin Yang*. Discovery of a novel oral proteasome inhibitor to block NLRP3 inflammasome activation with anti-inflammation activity. J. Med. Chem. 2022, 65, 11985–12001.

2) Hua Lei #, Shuli Liang#, Yinghua Zhou, Xinyi Wu, Haowei Cai, Zhuorong Liu, Yitao Ou, Yanhong Chen, Xiuhui Chen, Yuyun Yan , Dan Wu, Ping Sun*, Wenhui Hu*, Zhongjin Yang*. Artemisinin-derived Artemisitene Blocks ROS-Mediated NLRP3 Inflammasome and Alleviates Ulcerative Colitis. Int Immunopharmacol. 2022, 113, 109431

3) Xiuhui Chen#, Yanhong Chen#, Yitao Ou, Wenjie Min, Shuli Liang, Lei Hua, Yinghua Zhou, Cheng Zhang, Peifeng Chen, Zhongjin Yang*, Wenhui Hu*, Ping Sun*. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochem. Pharmacol. 2022, 206, 115326

4) Yanhong Chen#, Xiuhui Chen#, Shuli Liang, ……, Zhongjin Yang*, Wenhui Hu*, and Ping Sun*. Chlorquinaldol inhibits the activation of nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing protein 3 inflammasome and ameliorates imiquimod-induced psoriasis-like dermatitis in mice. Chem-Biol Interact, 2022, 365, 110122.

5) Shuli Liang#, Zhongjin Yang#, Lei Hua#, Yanhong Chen, ……, Wenhui Hu*, and Ping Sun*. Ciclopirox inhibits NLRP3 inflammasome activation via protecting mitochondria and ameliorates imiquimod-induced psoriatic inflammation in mice. Eur. J. Pharmacol. 2022, 930, 175156.

6) Cheng Zhang#, Hu Yue#, Ping Sun#, ……, Wenhui Hu*, and Zhongjin Yang*. Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities. Eur. J. Med. Chem. 2021, 219, 113417.

7) Hao Chen#, Xiuhui Chen#, Ping Sun#, ……, Wenhui Hu*, and Zhongjin Yang*. Discovery of dronedarone and its analogues as NLRP3 inflammasome inhibitors with potent anti-inflammation activity. Bioorg. Med. Chem. Lett. 2021, 46, 128160.

8) Hu Yue#, Zhongjin Yang#, ……, Wenhui Hu*, and Ping Sun*. Tanshinones inhibit NLRP3 inflammation activation by alleviating mitochondrial damage to protect against septic and gouty inflammation. Int Immunopharmacol. 2021, 97, 107819.

9) Ping Sun#, Wei Zhou#, ……, Zhongjin Yang*, Wenhui Hu*. Compound AD110 acts as therapeutic management for Alzheimer’s disease and stroke in mouse and rat models. ACS Chemical Neuroscience, 2020, 11(6), 929–938.

10) Wenmin Deng#, Zhongjin Yang#, ……, Wenhui Hu*, Ping Sun*. Disulfiram suppresses NLRP3 inflammasome activation to treat peritoneal and gouty inflammation. Free Radical Biology and Medicine, 2020, 152, 8–17.

11) Nannan Wu#, Guangyu Lian#, Jingyi Sheng#, ……, Wenhui Hu*, Zhongjin Yang*. Discovery of a Novel Selective Water-Soluble SMAD3 Inhibitor as an Antitumor Agent. Bioorg. Med. Chem. Lett. 2020, 30 (17), 127396.

12) Yitao Ou#, Ping Sun#, NanNan Wu#, Hao Chen, Wenhui Hu*, Zhongjin Yang*. Synthesis and biological evaluation of parthenolide derivatives as potential inhibitors of the NLRP3 inflammasome. Bioorg. Med. Chem. Lett. 2020, 30 (17), 127399.

13) Yahui Ding#, Zhongjin Yang#, Weizhi Ge#, ……, Yue Chen* and Quan Zhang*. Synthesis and biological evaluation of dithiocarbamate esters of parthenolide as potential anti-acute myelogenous leukemia agents. J. Enzym. Inhib. Med. Ch. 2018, 33, 1376-1391.

14) Zhong-Jin Yang#, Bei-Jia Kuang#, Quan Zhang, and Yue Chen. Synthesis and anti-acute myeloid leukemia activity of C-14 modified parthenolide derivatives. Eur. J. Med. Chem. 2017, 127, 296–304.

15) Zhong-Jin Yang#, ……，Quan Zhang*, and Yue Chen*. Syntheses and biological evaluation of costunolide, parthenolide and their fluorinated analogues. J. Med. Chem. 2015, 58 (17), 7007–7020.

16) 胡文辉, 杨忠金, 孙平, 吴欣忆, 陈秀会, 熊兮, 华磊, 硼酸类化合物及其应用, 中国，CN202210451312.9（实审）。

17) 胡文辉，杨忠金，孙平，张成，岳虎，1, 3-二苯基丙-2-烯-1-酮衍生物及其应用，中国，ZL202110317148.8（实审）。

18) 胡文辉，杨忠金，孙平，陈浩，陈秀会，苯并呋喃类化合物及其应用，中国，ZL202110513101.9（实审）。

19) 余细勇，胡文辉，蓝辉耀，杨忠金,武楠楠，氮杂吲哚类化合物及其应用，中国，ZL202010265070.5。

20) 陈悦，张泉，杨忠金，小白菊内酯衍生物，其药物组合物及其制备方法和用途，中国，ZL201510442126.9。

21) 陈悦，张泉，杨忠金，邝蓓佳，小白菊内酯衍生物，其药物组合物及其用途，中国，ZL201610770862.1。

22) 张泉，陈悦，丁亚辉，杨忠金等，小白菊内酯二硫代氨基甲酸酯衍生物及其盐，药物组合物及其用途，中国，ZL201710932515.9。