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1980-1990年就读于南京大学化学系,先后获得理学学士、硕士和博士学位。1990-2007年在南京大学化学化工学院和配位化学研究所工作,先后担任化学化工学院副院长和配位化学国家重点实验室副主任;1992-1993年在英国谢菲尔德大学开展博士后研究工作,1995-1996年在奥地利维也纳工业大学进行客座研究,1998年晋升为教授。2007年进入东南大学工作,现任东南大学药物研究中心主任、江苏省生物药物高技术研究重点实验室主任。担任国家新药审评中心咨询专家、国家重大新药创制专项评审专家、国家自然科学基金重点和面上项目通讯评审专家、江苏省高新企业审评专家。现任江苏省化学化工学会理事,曾任中国化学会第25届理事。长期从事药物化学应用基础研究和新药开发等方面的研发工作。
先后主持和参加完成了包括“十一五”、“十二五”国家“重大新药创制”专项课题和平台建设、国家自然科学基金、教育部和江苏省人才项目、江苏省自然科学基金和科技支撑项目以及江苏省重大基础设施建设等30多项项目,并主持完成横向项目30余项。
近五年以来的科研项目:
1. “基于抑制癌细胞干性克服顺铂耐药的研究”,国家自然科学基金面上项目(2021.1-2024.12),项目负责人。
2. “生物药物高技术研究重点实验室-2020省创”,江苏省科技厅(2020.01-2022.12),项目负责人。
3. “生物药物高技术研究重点实验室-2017省创”,江苏省科技厅(2017.01-2019.12),项目负责人。
4. “基于铂(IV)配合物的靶向或多靶点前药研究”,国家自然科学基金面上项目(2016.1-2019.12),项目负责人。
5. “抗体-药物偶联物(ADC)类抗肿瘤创新药物开发”,国家“重大新药创制”科技专项(2015.01-2019.12),参加单位项目负责人。
6. 多项横向项目。
在国内外刊物上发表论文两百余篇,授权国家发明专利30余项,美国、日本和欧洲授权专利各2项、许可实施2项。开发的药物产品和技术已创造了几十亿元的销售额,有十多项科研成果实现了产业化。近五年发表的主要论文如下:
2021年
1. Novel CK2 specific Pt(II) compound reverses cisplatin-mediated resistance by inhibiting cancer cell stemness and suppressing DNA damage repair in NSCLC treatments
Yuanjiang Wang#, Xinyi Wang#, Gang Xu, Shaohua Gou*
J. Med.Chem., 2021, 64(7), 4163-4178. Doi:10.1021/acs.jmedchem.1c00079
2. Discovery of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine derivatives as highly selective CK2 inhibitors with potent cancer cell stemness inhibition
Yuanjiang Wang, Zhaodan Lv, Feihong Chen, XingWang, Shaohua Gou*
J. Med. Chem., 2021,64(8), 5082-5098. DOI: 10.1021/acs.jmedchem.1c00131
3. Discoveryof 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol derivatives as glutathione transferase inhibitors with favorable selectivity and tolerated toxicity
Qingqing Liu#, Zhikun Liu#, Wuyang Hua, ShaohuaGou*
J. Med. Chem., 2021, 64(3), 1701-1702. DOI: 10.1021/acs.jmedchem.0c02048
4. Conjugatesderived from lapatinib derivatives with cancer cell stemness inhibitors effectively reversed drug resistance in triple- negative breast cancer.
Yuanjiang Wang, Zhaodan Lv, Feihong Chen, Xing Wang,Shaohua Gou*
J. Med. Chem., 2021, 64(17), 12877-12892.DOI: 10.1021/acs.jmedchem. 1c01013
5. Blood-brain barrier permeable and NO-releasing multifunctional nanoparticles for Alzheimer’s diseasetreatment: Targeting NO/cGMP/CREB signaling pathways.
Zhikun Liua#, Qingqing Liu#,Bin Zhang, Qiao Liu, Lei Fang*, Shaohua Gou*
J. Med. Chem., 2021,64(18), 13853-13872.
6. ROS-Responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenylboronate linker
Zhikun Liu#, Bin Zhang#, Shengjin Xia, Lei Fang *, Shaohua Gou *
Eur. J. Med. Chem., 2021, 212, 112997. doi: 10.1016/j.ejmech.2020.112997
7. Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potentia lEGFR/CAIX dual inhibitors
Bin Zhang#, Zhikun Liu#, Shengjin Xia, Qingqing Liu, Shaohua Gou *
Eur. J. Med. Chem., 2021, 216, 113300.
Jian Zhao, Kaiwen Yan, Gang Xu, Qiang Zhao,Chenjie Xu*, Shaohua Gou*
Adv. Func. Materials, 2021, 31(11), 2008325.
9. A light-controlled multi-step drug release nanosystem targeting tumor hypoxia for synergistic cancer therapy.
Bin Zhang#, Zichen Xu#, Wen Zhou, Zhikun Liu, Jian Zhao*, Shaohua Gou*
Chem. Sci., 2021, 12, 11810–11820. DOI: 10.1039/D1SC01888D.
10 The introduction of immunosuppressor (TDO inhibitor) significantly improved theefficacy of irinotecan in treating hepatocellular carcinoma
Qingqing Liu#, Shixian Hua#, XinyiWang, Feihong Chen*, Shaohua Gou*
Cancer ImmunologyImmunotherapy, 21, 70, 497-508. DOI: 10.1007/s00262-020- 02697-3
11. Breakdown of chemo-immune resistance by a TDO2-targeted Pt(IV) prodrug via attenuating endogenous Kyn-AhR-AQP4 metabolic circuity andTLS-promoted genomic instability
Feihong Chen, Gang Xu, Wenyuan Tian, Shaohua Gou*
Biochem. Pharmacology, 2021, doi: 10.1016/j.bcp.2021.114785
2020年
1. Platinum-based modification of styrylbenzylsulfonesas multifunctional antitumor agents: Targeting the RAS-RAF pathway, enhancing antitumor activity and overcoming multidrug resistance
Zhikun Liu#, Meng Wang#, Hengshan Wang, Lei Fang*, Shaohua Gou*
J. Med. Chem., 2020,63, 186-204. DOI: 10.1021/acs.jmedchem.9b01223
2. Targeting RAS-RAF pathway significantly improves antitumor activity of Rigosertib-derived platinum(IV) complexes and overcome cisplatin resistance
Zhikun Liu,# Meng Wang,# Hengshan Wang, Lei Fang*, Shaohua Gou*
Eur. J. Med. Chem., 2020, 194, 12269.
3. Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3 -dioxygenase
Shixian Hua, Feihong Chen, Xinyi Wang, Shaohua Gou*
Eur. J. Med. Chem., 2020, 189, 112041
4. Iridium (III) complexes derived polymeric micelles with low dark toxicity and strong NIR excitation for phototherapy and chemotherapy
Jian Zhao, Xinzhong Zhang, LeiFang*, Chuanzhu Gao, Chenjie Xu*, Shaohua Gou*
Small, 2020, 16(14), 2000363.
5. Bifunctional ruthenium(ii) polypyridyl complexes of curcumin as potential anticancer agents
Shuang Li#, Gang Xu#, Yuhua Zhu, Jian Zhao*, Shaohua Gou*
Dalton Trans., 2020, 49(27), 9454-9463.
6. Enhancing photodynamic therapy efficacy of upconversion-based nanoparticles conjugated with a long-lived triplet excited state iridium(III)-naphthalimide complex: toward highly enhanced hypoxia-inducible factor-1
Jian Zhao, Shuchen Sun, Xiaoyan Li, Wenjing Zhang,* Shaohua Gou*
ACS Appl. Bio Mater. 2020, 3, 252−262. DOI: 10.1021/acsabm.9b00774
7. Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3- dioxygenase
Shixian Hua ,Feihong Chen, Shaohua Gou*
Eur. J. Med. Chem., 2020, 187,
8. Design of a tris-heteroleptic Ru(II) complex with red-light excitation and remarkably Improved photobiological activity
Shuang Li, JianZhao*, Xinyi Wang, Gang Xu, Shaohua Gou*, Qiang Zhao*
Inorg. Chem., 2020, 59(15), 11193-11204. DOI: 10.1021/acs.inorgchem.0c01860
2019年
1. Construction of dual stimuli-responsive platinum(IV) hybrids with NQO1 targeting ability andovercoming cisplatin resistance
Lei Fang#, Xiaodong Qin#, Jian Zhao, Shaohua Gou*
Inorg. Chem., 2019, 58, 2291-2200. DOI: 10.1021/acs.inorgchem.8b03386
2. Dinuclear organoruthenium complexes exhibit antiproliferative activity through DNA damage and ROS-mediated ER stress pathway
JianZhao, Shuang Li, Xinyi Wang, Gang Xu, Shaohua Gou*
Inorg. Chem., 2019, 58, 2208-2217. DOI: 10.1021/acs.inorgchem.8b03447
3. Multifunctional platinum(IV) complexes as immuno stimulatory agents to promote cancer immunochemotherapy by inhibiting tryptophan-2,3-dioxygenase
ShixianHua#, Feihong Chen#,Gang Xu, Shaohua Gou*
Eur. J. Med. Chem., 2019, 169, 29-41.
4. SHR-A1403, a c-Met antibody-drug conjugate, exerts encouraging anti-tumor activity in c-Met-overexpressed models
Changyong Yang, Lei Wang, Xing Sun, Mi Tang, Haitian Quan, Lianshan Zhang, Liguang Lou*, Shaohua Gou*
Acta Pharmcologic Sinica, 2019, 40(7),971-979. DOI:10.1038/s41401-018- 0198-0
5. Promoting antitumor efficacy by suppressing hypoxia via nano self-assembly of two irinotecan-based dual drug conjugates owning a HIF-1a inhibitor
Bin Zhang#, Xiaochao Huang#, Hengshan Wang*, Shaohua Gou*
J. Materials Chem. B, 2019, 7, 5352 - 5362. DOI:10.1039/C9TB00541B
2018年
1. Pt(IV) complexes conjugating with chalcone analogue as inhibitors of microtubule polymerizationexhibited selective inhibition in humancancer cells.
Xiaochao Huang#, Rizhen Huang#, Zhimei Wang, Lingxue Li, Shaohua Gou*, Zhixin Liao, Hengshan Wang*
Eur. J. Med. Chem., 2018, 146, 435-450.
2. Dual-targeting antitumor hybrids derived from Pt(IV) species and millepachine analogues
Xiaochao Huang#, Shixian Hua#, Rizhen Huang#, Zhikun Liu, Shaohua Gou*, Zhimei Wang, Zhixin Liao, Hengshan Wang*
Eur. J. Med. Chem., 2018, 148, 1-25.
3. Theranostic Pt(IV) conjugatewith target selectivity for androgen receptor
Xiaodong Qin#, Lei Fang#, Jian Zhao, Shaohua Gou*
Inorg. Chem., 2018, 57(9),5019-5029. DOI: 10.1021/acs.inorgchem.8b00083
4. Pt(IV)prodrugs containing microtubulin inhibitors displayed potent antitumor activityand ability to overcome cisplatin resistance
Lingxue Li#, Xiaochao Huang#, Rizhen Huang, Shaohua Gou*, Zhimei Wang, HengshanWang*
Eur. J. Med. Chem., 2018, 156, 666-679 .
5. Hypoxia-targeting organometallic Ru(II) arene complexes with enhanced anticancer activity in hypoxic cancer cells
Jian Zhao, Wanchun Li, Shaohua Gou*, Shuang Li, Shengqiu Lin, Qianhui Wei, Gang Xu*
Inorg. Chem., 2018, 57, 8396-8403.DOI: 10.1021/acs.inorgchem.8b01070
2017年
1. Novel hypoxia-targeting Pt(IV) prodrugs
Zichen Xu#, Jian Zhao#, Shaohua Gou*, Gang Xu
Chem.Commun., 2017,53, 3749-3752. DOI: 10.1039/C7CC01320E
2. A CK2-targeted Pt(IV) prodrug to disrupt DNA damage response.
Feihong Chen#, Xiaochao Huang#, Mian Wu,Shaohua Gou*,Weiwei Hu
Cancer Lett., 2017, 385(28), 168-178. DOI:10.1016/j.canlet.2016.10.026
3. Anticancer platinum(IV) prodrugs containing mono-aminophosphonateester as a targeting group inhibit matrix metalloproteinases and reverse multidrugresistance
Xiaochao Huang#, Rizhen Huang#, Shaohua Gou*, Zhimei Wang, Hengshan Wang*
Bioconjugate Chem., 2017, 28, 1305-1323. DOI:10.1021/acs.bioconjchem.7b00117
4. Reversal of cisplatin resistance in human gastric cancer cells by a wogonin-conjugated Pt(IV) prodrugvia attenuating Casein Kinase 2-mediated Nuclear Factor-kB pathways
Feihong Chen, Xiaodong Qin,Gang Xu, Shaohua Gou*, Xiufeng Jin
Biochem. Pharmacology, 2017, 135, 50-68. DOI:10.1016/j.bcp.2017.03.004
5. Synthesis and biological evaluation of novel chalcone derivatives as a new class of microtubule destabilizing agents
Xiaochao Huang#, Rizhen Huang#, Lingxue Li, ShaohuaGou*, Hengshan Wang*
Eur. J. Med. Chem., 2017, 132, 11-25. DOI:10.1016/j.ejmech.2017.03.031
6. Conjugationof platinum(IV) complexes with chlorambucil to overcome cisplatin resistance via a “joint action” mode toward DNA
Xiaodong Qin#, Lei Fang#, Feihong Chen, Shaohua Gou*
Eur. J. Med. Chem., 2017, 137, 167-175. DOI: 10.1016/j.ejmech.2017.05.056
7. Exploring the hydrolytic behavior of the platinum(IV) complexes with axial acetato ligands
Jian Zhao#, Zichen Xu#, Jing Lin, Shaohua Gou*
Inorg. Chem., 2017, 56(16): 9851-9859. DOI:10.1021/acs.inorgchem.7b01355
8. Platinum(IV) prodrugs multiply targeting genomic DNA, histone deacetylases and PARP-1
Zichen Xu#, Weiwei Hu#, Zhimei Wang, Shaohua Gou*
Eur. J. Med. Chem., 2017, 141, 211-2
1995年获中国化学会“青年化学”奖、国家教委“资助优秀年轻教师基金”
1996年获江苏省首届“江苏青年科学家”奖、被评为江苏省优秀青年骨干教师
1997年被江苏省列为333工程培养对象
2000年获国家教育部青年骨干教师研究基金
2002年被教育部评为全国高等学校优秀骨干教师
2007年被评为江苏省“333高层次人才培养工程”首批中青年科学技术带头人、获第一届“中国百篇最具影响优秀国际学术论文”奖
2008年获江苏省“六大人才高峰”高层次人才项目资助
2014年获中华全国工商业联合会科技进步奖(一等奖)
2016年获中华全国工商业联合会科技进步奖(一等奖)
2018年获江苏省教育科学研究成果奖二等奖(高校自然科学类)
2019年获日内瓦国际发明银奖
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