孔德新[天津醫科大學教授，博士生導師]:天津市特聘教授，天津醫科大學“2 -百科知識中文網

基本信息

近幾年來主要從事分子靶向抗癌藥物的發現和作用機理研究。在日本癌研究會工作期間，與日本全藥工業株式會社合作研發分子靶向抗癌藥物PI3K 抑制劑ZSTK474，已獲美國FDA 批准進入臨床試驗。主持完成ZSTK474 抑制血管生成的研究成果被期刊European Journal of Cancer 評為最受矚目的論文。發表SCI 收錄論文27 篇，其中通訊和第一作者論文17 篇。已被引用400 余次，其中他引300 余次，他引期刊包括影響因子35.2 的Nature Genetics 等國際頂級期刊。關於PI3K 抑制劑的研究成果曾於2009 年在日本Medical Science Digest 的工業新聞中報導。分別於2012 年1月和2013 年5 月兩次獲得日本學術振興會國際交流基金。

個人資料

天津市特聘教授，天津醫科大學“211工程”特聘教授，天津市中青年骨幹創新人才，生物製藥教研室主任。

工作經歷

2010/10－至今，天津醫科大學藥學院教授，天津市基礎醫學研究中心PI

2010/04－2010/09，日本癌症研究所分子藥理部，資深研究員（永久職位）

2006/08－2010/03，日本癌症研究所分子藥理部，研究員

2005/04－2006/07，香港中文大學藥學院，副研究員

2000/10－2002/03，大阪大學藥學部，訪問學者

1996/12－2000/09，山東大學生命科學學院，講師

1994/08－1996/11，山東大學生命科學學院，助教

教育背景

2002/04－2005/03，大阪大學大學院藥學研究科，博士

1991/09－1994/07，山東大學藥學院（原山東醫科大學藥學系），碩士

1987/09－1991/07，山東大學藥學院（原山東醫科大學藥學系），學士

研究方向

分子靶向藥物的篩選、機理及轉化醫學研究

天然藥物的研發

生物製藥

主要科研項目

STELB抑制膠質母細胞瘤的作用、分子機制及靶點研究。國家自然科學基金面上項目，81673464，54萬元，2017.01-2020.12.

以小分子探針研究靶向抑制PI3K亞型抗前列腺癌轉移的作用及多重分子機理。國家自然科學基金面上項目，81373441，60萬元，2014.01-2017.12.

天津市高等學校臨床藥學方向創新團隊培養計畫。180萬元，2013.12-2015.12.

從天然資源(包括海洋生物)中發現分子靶向藥物的方法學研究，日本學術振興會“橋”項目國際交流基金(編號BR13102), 10萬元，2013年7月至2014年3月。

新型分子靶向藥物的發現，日本學術振興會外國資深研究者訪問交流基金(編號S-12105)，15萬元，2012年4月至2013年3月。

靶向抑制PI3K對前列腺癌轉移的影響及機理研究，天津市自然科學基金重點項目，20萬元，2012年4月至2015年3月。

基於癌細胞信息學藥物篩選系統的創新型分子靶向藥物發現子課題：利用各種信號傳導通路抑制劑對癌細胞信息學藥物篩選系統的功能驗證，日本學術振興會項目，50萬元，2010年4月至2012年3月。

新型PI3K抑制劑ZSTK474的研發和轉化研究子課題：ZSTK474的分子藥理研究，日本國家生物醫藥創新研究課題，160萬元，2006年4月至2010年3月。

癌症化學療法的基礎信息學研究子課題：基於JFCR39指紋圖譜的抗癌藥物靶點發現研究，日本文部科學省癌症特別領域研究課題，50萬元，2006年4月至2010年3月。

主要論文

一）近期主要SCI期刊論文

1) Wang R, Zhang Q , Peng X, Zhou C, Zhong Y, Chen X, Qiu Y, Jin M, Gong M, Kong D*. Stellettin B Induces G1 Arrest, Apoptosis and Autophagy in Human Non-small Cell Lung Cancer A549 Cells via Blocking PI3K/Akt/mTOR Pathway. Sci Rep, 2016, 6: 27071.

2) Wang Y, Liu J, Qiu Y, Jin M, Chen X, Fan G, Wang R, Kong D*. ZSTK474, a specific class I phosphatidylinositol 3-kinase inhibitor, induces G1 arrest and autophagy in human breast cancer MCF-7 cells. Oncotarget, 2016, 7 (15): 19897-19909.

3) Huang C, Yi X, Kong D, Chen L, Gong M. Controlled release strategy of paclitaxel by conjugating to matrix metalloproteinases-2 sensitive peptide. Oncotarget. 2016, in press. doi: 10.18632/oncotarget.10735.

4) Chen Y, Zhou Q, Zhang L, Wang R, Jin M, Qiu Y, Kong D*. Idelalisib induces G1 arrest and apoptosis in chronic myeloid leukemia K562 cells. Oncol Rep. 2016, in press, doi: 10.3892/or.2016.5176.

5) Wang P, He Y, Li D, Han R, Liu G, Kong D, Hao J. Class I PI3K inhibitor ZSTK474 mediates a shift in microglial/macrophage phenotype and inhibits inflammatory response in mice with cerebral ischemia/reperfusion injury. J Neuroinflammation. 2016, 13(1):192.

6) Zhao W, Qiu Y, Kong D*. Class I phosphatidylinositol 3-kinase inhibitors for cancer therapy. Acta Pharmaceutica Sinica B, 2016, in press.

7) Zhou Q, Chen Y, Chen X, Zhao W, Zhong Y, Wang R, Jin M, Qiu Y, Kong D*. In Vitro Antileukemia Activity of ZSTK474 on K562 and Multidrug Resistant K562/A02 Cells. Int J Biol Sci. 2016, 12(6): 631-8.

8) Xu J, Gao C, Zhang F, Ma X, Peng X, Zhang R, Kong D, Simard AR, Hao J. Differentially expressed lncRNAs and mRNAs identified by microarray analysis in GBS patients vs healthy controls. Sci Rep, 2016，6: 21819.

9) Li Y, Wang Y, Wei Q, Zheng X, Tang L, Kong D, Gong M*. Variant fatty acid-like molecules Conjugation, novel approaches for extending the stability of therapeutic peptides. Sci Rep, 2015; 5:18039.

10) Zhang F, Gao C, Ma X, Peng X, Zhang R, Kong D, Simard AR, Hao J*. Expression Profile of Long Noncoding RNAs in Peripheral Blood Mononuclear Cells from Multiple Sclerosis Patients. CNS Neurosci Ther, 2016, in press. doi: 10.1111/cns.12498.

11) Chen X, Xu H, Li B, Wang F, Chen X, Kong D, Lin X*. Preparation and Antitumor Activity of CS5931, A Novel Polypeptide from Sea Squirt Ciona Savignyi. Mar Drugs, 2016, 14: pii: E47.

12) Tang SA, Zhou Q, Guo W, Qiu Y, Wang R, Jin M, Zhang W, Li K, Yamori T, Dan S, Kong D*. In vitro Antitumor Activity of Stellettin B, a Triterpene from Marine Sponge Jaspis stellifera, on Human Glioblastoma Cancer SF295 Cells. Mar Drugs. 2014, 12: 4200-4213.

13) Chen X, Tang SA, Lee E, Qiu Y, Wang R, Duan HQ, Dan S, Jin M, Kong D*. IVSE, isolated from Inula japonica,suppresses LPS-induced NO production via NF-κB and MAPK inactivation in RAW264.7 cells. Life Sci, 2015; 124:8-15.

14) Wang X, Tang SA, Wang R, Qiu Y, Jin M, Kong D*. Inhibitory effects of JEUD-38, a new sesquiterpene lactone from Inula Japonica Thunb, on LPS-induced iNOS expression in RAW264.7 cells. Inflammation, 2015; 38(3):941-8.

15) Kong D*, Yamori T, Yamazaki K, Dan S*. In vitro multifaceted activities of a specific group of novel phosphatidylinositol 3-kinase inhibitors on hotspot mutant PIK3CA. Invest New Drugs, 2014, 32: 1134-1143.

16) Jin M, Zhou Q, Lee E, Dan S, Duan HQ, Kong D*. AS252424, a PI3K� Inhibitor, Downregulates Inflammatory Responsiveness in Mouse Bone Marrow-Derived Mast Cells. Inflammation, 2014, 37 (4): 1254-1260.

17）Zhao W, Guo W, Zhou Q, Ma S, Wang R, Qiu Y, Jin M, Duan HQ, Kong D*. In Vitro Antimetastatic Effect of Phosphatidylinositol 3-Kinase Inhibitor ZSTK474 on Prostate Cancer PC3 Cells. Int. J. Mol. Sci. 2013, 14, 13577-13591.

18). Kong D, Yamori T*. JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs. Bioorg. Med. Chem. 2012, 20 (6): 1947-1951.

19). Kong D, Dan S, Yamazaki K, Yamori T*. Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39. Eur. J. Cancer. 2010, 46 (6): 1111-1121.

20). Kong D, Okamura M, Yoshimi H, Yamori T*. Anti-angiogenic effect of a novel phosphatidylinositol 3-kinase inhibitor, ZSTK474. Eur. J. Cancer. 2009, 45 (3): 857-865. cover paper.

21). Jin M, Zhao W, Zhang Y, Kobayashi M, Duan H, Kong D*. Antiproliferative Effect of Aaptamine on Human Chronic Myeloid Leukemia K562 cells. Int. J. Mol. Sci. 2011, 12 (11): 7352-7359.

22). Kong D*, Zhang Y, Yamori T, Duan H, Jin M. Inhibitory Activity of Flavonoids against Class I Phosphatidylinositol 3-Kinase Isoforms. Molecules. 2011, 16 (6): 5159-67.

23). Kong D*, Yamori T, Kobayashi M, Duan H. Antiproliferative and antiangiogenic activities of Smenospongine, a marine sponge Sesquiterpene Aminoquinone. Mar. Drugs. 2011, 9 (2): 154-161.

24). Kong D, Yamori T*. Advances in development of Phosphatidylinositol 3-kinase inhibitors. Curr. Med. Chem. 2009, 16 (22): 2839-2854.

25). Kong D, Aoki S, Sowa Y, Sakai T, Kobayashi M*. Smenospongine, a sesquiterpene aminoquinone from a marine sponge, induces G1 arrest or apoptosis in different leukemia cells. Mar. Drugs 2008, 6 (3): 480-488.

26). Kong D, Yamori T*. Phosphatidylinositol 3-kinase inhibitors: promising drug candidates for cancer therapy. Cancer Sci. 2008, 99 (9): 1734-1740.

27). Kong D, Yamori T*. ZSTK474 is an ATP-competitive inhibitor of class I PI3 kinase isoforms. Cancer Sci. 2007, 98 (10): 1638-1642.

28). Kong D*. PI3K inhibitors: novel molecular-targeted drug candidates for cancer therapy. Biochem. Pharmacol. 2012, 1 (6): e126.

29). Kong D, Yamazaki K, Yamori T*. Discovery of phosphatidylinositol 3-kinase inhibitory compounds from the SCADS library. Biol. Pharm. Bull. 2010, 33 (9): 1600-1604.

30). Kong D, Okamura M, Yoshimi H, Yamori T*. Anti-angiogenic activity of a novel PI3K inhibitor, ZSTK474. EJC Suppl. 2008, 6 (12): 71.

31). Kong D, Yamori T*. ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor identified by JFCR39 drug discovery system. Acta Pharmacol. Sin. 2010, 31 (9): 1189-1197.

32). Kong D, Yaguchi S, Yamori T*. Effect of ZSTK474, a Novel Phosphatidylinositol 3-kinase Inhibitor, on DNA-Dependent Protein Kinase. Biol. Pharm. Bull; 2009, 32 (2): 297-300.

33) Tang SA, Zhu H, Qin N, Zhou JY, Lee E, Kong DX, Jin MH, Duan HQ. Anti-inflammatory terpenes from flowers of Inula japonica. Planta Med. 2014, 80(7):583-9.

34) Ma Y, Jin YY, Wang YL, Wang RL, Lu XH, Kong DX, Xu WR.The discovery of a novel and selective inhibitor of PTP1B over TCPTP: 3D QSAR pharmacophore modeling, virtual screening, synthesis, and biological evaluation. Chem Biol Drug Des. 2014, 83(6):697-709.

35) Duan YQ, Ma Y, Wang XJ, Jin YY, Wang RL, Dong WL, Xu WR, Kong DX, Wang SQ. Design potential selective inhibitors for treating cancer by targeting the Src homology 2 (SH2) domain-containing phosphatase 2 (Shp2) with core hopping approach. Protein Pept Lett. 2014, 21(6):556-63.

36）Qiu Y, Lee KS, Choo YM, Kong D, Yoon HJ, Jin BR*. Molecular cloning and antifibrinolytic activity of a serine protease inhibitor from bumblebee (Bombus terrestris) venom. Toxicon, 2013, 63C: 1-6.

37). Zhai, HY, Zhao C, Zhang N, Jin MN, Tang SA, Qin N, Kong DX, Duan HQ*. Alkaloids fromPachysandra terminalisInhibit Breast Cancer Invasion and Have Potential for Development As Antimetastasis Therapeutic Agents. J. Nat. Prod. 2012, 75, 1305-1311.

38). Sugita H, Dan S, Kong D, Tomida A, Yamori T*. A new evaluation method for quantifying PI3K activity. Biochem. Biophys. Res. Commun. 2008, 377 (3): 941-945.

39). Aoki S, Kong D, Suna H, Sowa Y, Sakai T, Setiawan A, Kobayashi M. Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner. Biochem. Biophys. Res. Commun. 2006, 342 (1): 101-106.

40). Aoki S, Kong D, Matsui K, Kobayashi M. Erythroid differentiation in K562 chronic myelogenous cells induced by crambescidin 800, a pentacyclic guanidine alkaloid. Anticancer Res. 2004, 24(4):2325-2330.

41). Aoki S, Kong D, Matsui K, Kobayashi M. Sesquiterpene aminoquinones, from a marine sponge, induce erythroid differentiation in human chronic myelogenous leukemia, K562 cells. Chem. Pharm. Bull. 2004, 52(8):935-937.

42). Aoki S, Kong D, Matsui K, Kobayashi M. Smenospongine, a spongean sesquiterpene aminoquinone, induces erythroid differentiation in K562 cells. Anti-Cancer Drugs, 2004, 15(4):363-369.

二）近期代表性國際會議論文

1). Kong D. Discovery and development of a novel PI3K inhibitor-ZSTK474. Symposium on Screening of Anticancer Drugs. 日本，東京. Jul. 2012. Abstract: S12. Page: 13. 大會報告。

2). Kong D, Yamori T. Inhibition profiles of novel PI3K inhibitors against PI3K superfamily and human cancer cell line panel JFCR39. The 69 th annual meeting of the Japanese Cancer Association. 日本，大阪. Sep. 2010. Abstract: IS11-6. Page: 385. 大會報告。

3). Kong D, Dan S, Yamzaki K, Yamori T. JFCR39 COMPARE system can predict molecular targets of phosphatidylinositol 3-kinase inhibitors with high resolution. 21st EORTC-NCI-AACR symposium on Molecular targets and cancer therapeutics.美國，波士頓. Nov. 2009. Abstract: C67. Page: 273. Poster presentation.

4). Kong D, Yamori T. Inhibition profiles of novel PI3K inhibitors against PI3K superfamily. The 69 th annual meeting of the Japanese Cancer Association. 日本，橫濱. Oct. 2009. Abstract: IS4-2. Page: 37. 大會報告。

5). Kong D, Yoshimi H, Yamori T. Anti-angiogenic activity of a novel PI3K inhibitor, ZSTK474. 20th EORTC-NCI-AACR symposium on Molecular targets and cancer therapeutics. 瑞士，日內瓦. Oct. 2008. Abstract: 226. Page: 71. Poster presentation.

6). Kong D, Yaguchi Y, Yamori T. ZSTK474 is a specific class I PI3K inhibitor. Proceedings of 100 th AACR. 美國，聖迭亞格. Apr. 2008. Abstract: 2307. Page: 544. Poster presentation.

主要教材

參編專著《生化藥物研究》，人民衛生出版社出版，1997年12月第一版。

主要社會兼職

日本學術振興會中國同學會會長

國家衛計委專業技術資格評審專家

教育部學位評審專家

科技部創新人才評審專家

中國藥理學會腫瘤藥理專業委員會委員

中國抗癌協會抗癌藥物專業委員會委員

中國藥理學會補益藥藥理專業委員會委員

中國生物化學與分子生物學會工業生化與分子生物學分會理事

中國生物化學與分子生物學會海洋生化與分子生物學分會理事

國家自然科學基金、教育部博士點基金、博士後基金等評審專家

天津市藥品化妝品評審專家

天津醫藥集團項目評審專家

Journal of Cancer期刊編委

E-Journal of Chemistry期刊編委

Biochemistry and Pharmacology期刊編委

OA Cancer期刊編委

《中國醫藥導報》、《食品與藥品》期刊編委

美國癌症學會(AACR)會員

日本癌症學會會員，日本分子靶向癌治療學會會員

日本藥學會會員，日本生藥學會會員

圖集資料

孔德新[天津醫科大學教授，博士生導師]