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卜憲章

鎖定
卜憲章,男,博士,中山大學藥學院教授,藥物化學、有機化學博士生導師。先後主持國家自然科學基金、國家高新技術計劃863項目、教育部重點科技項目、廣東省自然科學基金以及中山大學百人計劃引進人才“行動計劃”基金等多項研究課題。發表SCI論文80多篇,申請或授權國內外發明專利多項。J Med Chem等多個國際知名學術期刊審稿人,國家、省基金評審專家,省藥學會成員。
中文名
卜憲章
出生日期
1970年8月
學位/學歷
博士
職    業
教師
職    務
博士生導師
職    稱
教授

卜憲章人物經歷

1994及1997年分別獲武漢大學學士、碩士學位;
2000年7月獲中山大學生物有機化學專業博士學位;
2001.1-2002.1及2002.8-2003.8年在香港科技大學生物技術研究所進行訪問研究;
2003年底入職中山大學藥學院工作至今。 [1] 

卜憲章研究方向

藥學多學科融合基礎上的藥物設計與發現:
(1)活性多肽、類天然產物庫的構建;
(2)腫瘤、神經退行性疾病惡性事件中關鍵蛋白的降解與摺疊行為調控及藥理意義;
(3)重大疾病相關信號網絡關鍵因子的探針設計與藥物發現 [1] 

卜憲章學術成果

卜憲章科研項目

1.基於Aβ蛋白N端捕獲的活性環肽設計及其抗AD作用與分子機制研究(21672266),國家自然科學基金,2017.1-2020.12
2.靶向19SRP去泛素化酶的新機制蛋白酶體抑制劑的發現與抗腫瘤研究(81473083),國家自然科學基金,2015.1-2018.12
3.靶向NF-kappaB/p53交叉通路網絡的新型PAC類抗腫瘤活性分子的設計發現與機制研究(81172931),國家自然科學基金,2012.1-2015.12
4.抑制NF-κB激活通路的新型PACs類先導物的發現、作用機制及抗腫瘤研究(30973619),國家自然科學基金,2010.1-2012.12
5.神經退行性疾病信號轉導及新靶標研究(批准號:9351008901000003),廣東省自然科學基金研究團隊項目,2010.1-2012.12(核心成員)
6.多靶標內環境激活式抗耐藥腫瘤先導分子的設計(2008AA02Z304);國家高新技術863項目,2008.1-2010.12
7.基質細胞衍生因子衍生多肽庫的構建及其抗腫瘤轉移作用研究(5001773),廣東省自然科學基金2005.1-2007.12
8.抑制CXCR4的重組趨化因子衍生肽庫的構建及其生理意義(105133),國家教育部重點科技項目2005.1-2007.12
9.中山大學百人計劃引進人才“行動計劃”基金,2003年 [1] 

卜憲章論著專利

代表性論文:
  1. Gesi Wen1, Daoyuan Chen1, Wenjing Qin, Binhua Zhou, Youqiao Wang, Ziyi Liu, Jun Du, Qiang Zhou, Junmin Quan, Xianzhang Bu*,Stabilizing of Amyloid-β Peptide by the N-terminus Capture is Capable of Preventing and Eliminating Amyloid-β Oligomers.Chem. Commun.,2017, 53, 7673—7676
  2. Xin Yue1, Yinglin Zuo1, Hongpeng Ke, Jiaming Luo, lanlan Lou, Wenjing Qin, Youqiao Wang, Ziyi Liu, Daoyuan Chen, Haixia Sun, Weichao Zheng, Cuige Zhu, Ruimin Wang, Gesi Wen, Jun Du, Binhua Zhou*, Xianzhang Bu*, Identification of 4-arylidende curcumin analogues as novel proteasome inhibitors for potential anticancer agents targeting 19S regulatory particle associated deubiquitinase.Biochem Pharmacol2017, 137,29-50.
  3. Gesi Wen, Wenjing Qin, Daoyuan Chen, Youqiao Wang, Xin Yue, Ziyi Liu, Yingnan Cao, Jun Du, Binhua Zhou*, and Xianzhang Bu*, Stabilizing the monomeric amyloid-β peptide by Tyrocidine A prevents and reverses the amyloideogenesis without the accumulation of oligomersChem. Commun., 2017,53, 3886-3889.
  4. Baoxia Liang, Ziyi Liu, Yingnan Cao, Cuige Zhu, Yinglin Zuo, Lei Huang, Gesi Wen, Nana Shang, Yu Chen, Xin Yue, Jun Du, Baojian Li, Binhua Zhou*, Xianzhang Bua*,MC37, a new mono-carbonyl curcumin analog, induces G2/M cell cycle arrest and mitochondria-mediated apoptosis in human colorectal cancer cells.European Journal of Pharmacology2016, 796,139-148.
  5. Jianyong Zhu, Ruimin Wang, Lanlan Lou, Wei Li, Guihua Tang, Xianzhang Bu*, and Sheng Yin*, Jatrophane Diterpenoids as Modulators of P-Glycoprotein-Dependent Multidrug Resistance (MDR): Advances of Structure–Activity Relationships and Discovery of Promising MDR Reversal Agents,J. Med. Chem.,2016,59(13):6353-6369
  6. Baoxia Liang, Weiyan Shao, Cuige Zhu, Gesi Wen, Xin Yue, Ruimin Wang, Junmin Quan, Jun Du, and Xianzhang Bu*, Mitochondria-Targeted Approach: Remarkably Enhanced Cellular Bioactivities of TPP2a as Selective Inhibitor and Probe toward TrxR,ACS Chem. Biol., 2016, 11 (2), 425–434
  7. Zhang-Hua Sun, Yu Chen, Yan-Qiong Guo, Jie Qiu, Cui-Ge Zhu, Jing Jin, Gui-Hua Tang, Xian-Zhang Bu*, Sheng Yin*, Isolation and cytotoxicity evaluation of taxanes from the barks of Taxus wallichiana var. mairei,Bioorganic & Medicinal Chemistry Letters, 2015, 25, 1240–1243
  8. Cuige Zhu, Yinglin Zuo, Baoxia Liang, Hong Yue, Xin Yue, Gesi Wen, Ruimin Wang, Junmin Quan, Jun Du and Xianzhang Bu* Distinct tubulin dynamics in cancer cells explored using a highly tubulin-specific fluorescent probe,Chem. Commun., 2015, 51, 13400-13403.
  9. Cuige Zhu , Yinglin Zuo , Ruimin Wang , Baoxia Liang , Xin Yue , Gesi Wen , Nana Shang , Lei Huang , Yu Chen , Jun Du , and Xianzhang Bu * Discovery of Potent Cytotoxic Ortho-Aryl Chalcones as New Scaffold Targeting Tubulin and Mitosis with Affinity-Based Fluorescence,J. Med. Chem., 2014, 57 (15), 6364–6382.
  10. L. Huang, Y. Chen, B. Liang, B. XING, G. Wen, S. Wang, X. Yue, C. Zhu, J. Du and X. Bu, Furanyl Acryl Conjugated Coumarin as Efficient Inhibitor and Highly Selective Off-On Fluorescent Probe for Covalent Labelling of Thioredoxin ReductaseChem. Commun., 2014, 50, 6987--6990.
  11. Nana Shanga, Yongxian Shao, Yinghong Cai, Matthew Guan, Manna Huang, Wenjun Cui, Lin He, Yan-Jun Yu, Lei Huang, Zhe Li, Xianzhang Bu*, Hengming Ke*, Hai-Bin Luo*, Discovery of 3-(4-hydroxybenzyl)-1-(thiophen-2-yl)chromeno[2,3-c]pyrrol-9(2H)- one as a phosphodiesterase-5 inhibitor and its complex crystal structure,Biochemical Pharmacology 2014, 89, 86–98 .
  12. H. Liu, Y. Liu, F. Zhang, H. Wang, G. Zhang, B. Zhou, Y. Zuo, S. Cai, X. Bu* and J. Du*, Identification of potential pathways involved in induction of cell cycle arrest and apoptosis by a new 4-arylidene Curcumin analogue T63 in lung cancer cells: a comparative proteomic analysisMol. BioSyst., 2014, 10, 1320—1331.
  13. Binhua Zhou, Yinglin Zuo, Baojian Li, Hao Wang, Hao Liu, Xianfeng Wang, Xu Qiu, Yun Hu, Shijun Wen, Jun Du, Xianzhang Bu*, Deubiquitinase Inhibition of 19S Regulatory Particles by 4-Arylidene Curcumin Analogue AC17 Causes NF-κB Inhibition and p53 Reactivation in Human Lung Cancer Cells,Molecular Cancer Therapeutics, 2013, 12(8), 1381–1392.
  14. Yun Hu, Yaqi Yang, Yanjun Yu, Gesi Wen, Nana Shang, Wei Zhuang, Dihan Lu, Binhua Zhou, Xin Yue, Baoxia Liang, Jun Du, Feng Li, Xian-Zhang Bu*, Synthesis and Identification of New Flavonoids Targeting Liver X Receptor β Involved Pathway as Potential Facilitators of Aβ Clearance with Reduced Lipid Accumulation.Journal of Medicinal Chemistry, 2013, 56, 6033−6053.
  15. Binhua Zhou, Jianing Huang, Yinglin Zuo, Baojian Li, Qiang Guo, Baicheng Cui, Weiyan Shao, Jun Du, Xianzhang Bu*, 2a, a novel curcumin analogue, sensitizes cisplatin-resistant A549 cells to cisplatin by inhibiting thioredoxin reductase concomitant oxidative stress damage,European Journal of Pharmacology, 2013, 707, 130‐139.
  16. Hao Liu, BinHua Zhou, Xu Qiu, HongSheng Wang, Fan Zhang, Rui Fang, XianFeng Wang, ShaoHui Cai, Jun Du*, XianZhang Bu*,T63, a new 4-arylidene curcumin analogue,induces cell cycle arrest and apoptosis through activation of the reactive oxygen species–FOXO3a pathway in lung cancer cells,Free Radical Biology and Medicine, 2012, 53, 2204–2217.
  17. Yinglin Zuo, Jianing Huang, Binhua Zhou, Shuni Wang, Weiyan Shao, Cuige Zhu, Li Lin, Gesi Wen, Hongyang Wang, Jun Du, Xianzhang Bu* Synthesis, cytotoxicity of new 4-arylidene curcumin analogues and their multi-functions in inhibition of both NF-kB and Akt signaling,Europe Journal of Medicinal Chemistry, 2012, 55, 346-357.
  18. Yinglin Zuo, Yi Yu, Shuni Wang, Weiyan Shao, Binhua Zhou, Li Lin, Zhuoyu Luo, Ruogu Huang, Jun Du, Xianzhang Bu* Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNFa-induced nuclear factor-kB activation inhibitionEurope Journal of Medicinal Chemistry, 2012, 50, 393-404.
  19. Yanjun Yu, Yun Hu, Weiyan Shao, Jianing Huang, Yinglin Zuo, Yingpeng Huo, Linkun An, Jun Du, and Xianzhang Bu* Synthesis of Multi-Functionalized Chromeno[2,3-c]pyrrol-9(2H)-ones: Investigation and Application of Baker–Venkataraman Rearrangement Involved Reactions Catalyzed by 4-(Dimethylamino)pyridine,Europe Journal of Organic Chemistry, 2011, 4551–4563 (IF:3.344)
  20. X Qiu, YH Du, B Lou, YL Zuo, WY Shao, YP Huo, JL Huang, YJ Yu, BH Zhou,J Du,HA Fu* and XZ Bu*, Synthesis and Identification of New 4-Arylidene Curcumin Analogues as Potential Anticancer Agents Targeting Nuclear Factor-kB Signaling Pathway.J Med Chem, 2010. 53 (23), 8260–8273.
  21. MG Yuan, MX Luo, Y Zhang, X Qiu, J Gui, Y Cao, X. Bu*, YL Ren* and XP Hu, Identification of curcumin derivatives as human glyoxalase I inhibitors: A combination of biological evaluation, molecular docking, 3D-QSAR and molecular dynamics simulation studiesBioorg & Med Chem 2011,19(3):1189-1196
  22. Z Xiao, LM Lin, ZH Liu, FT Jia, WY Shao, MJ Wang,L Liu, SL Li, F Li* and Bu, X.*, Potential Therapeutic Effects of Curcumin: Relationship to Microtubule- associated Proteins 2 in Abeta1-42 Insult.Brain Res 2010, 1361, 115-123
  23. Y.Huo, X Qiu, WY Shao, JN Huang, YJ Yu, YL Zuo, LK An, J Du and Bu, X.* , New fluorescent trans-dihydrofluoren-3-ones from aldol-Robinson annulation- regioselective addition involved one-pot reaction.Org Biomol Chem 2010. 8, 5048–5052
  24. Shen, Y.D., Tian Y.X, Bu, X. Z.* and L.Q. Gu, Natural tanshinone-like heterocyclic-fused ortho-quinones from regioselective Diels-Alder reaction: Synthesis and cytotoxicity evaluation.Eur J Med Chem 2009, 44, 3915-3921.
  25. Qiu, X.; Liu, Z.; Shao, W.Y.; Liu,X.; Jing, D.P.; Lu, Y.J.; An, L.K.; Huang, S.L.; Bu, X.Z.*; Huang, Z. S.; Gu, L.Q., Synthesis and evaluation of curcumin analogues as potential thioredoxin reductase inhibitors.Bioorgan Med Chem 2008, 16, 8035-8041.
  26. Shao, W.Y.; Cao, Y.N.; Yu, Z.W.; Pan, W.J.; Qiu, X.; Bu, X.Z.*; An, L. K.; Huang, Z. S.; Gu, L.Q.*; Chan, A. S. C. Facile preparation of new unsymmetrical curcumin derivatives by solid-phase synthesis strategy.Tetrahedron Lett 2006, 47, 4085-4089.
  27. Pei, L. X.; Li, Y.M.; Bu, X.Z.*; Gu, L.Q.; Chan, A. S. C. One-pot synthesis of 5,6-dihydroxylated benzo[b]furan derivatives.Tetrahedron Lett 2006,47, 2615-2618.
  28. Shen, Y.D.; Wu, H.Q.; Zhang, S.L.; Bu, X.Z.*; An, L.K.; Huang, Z.S.; Liu, P.Q.; Gu, L.Q.; Li, Y.M. and Chan, A.S.C. Novel synthesis of o-naphthothiophenequinone derivatives via regioselective Diels-Alder reaction.Tetrahedron 2005, 61, 9097-9101.
  29. Pei, L.X.; Huang, S.L.; Shen, Y.D.; An, L.Q.; Huang, Z.S.; Li, Y.M.; Gu, L.Q.*; Bu, X.Z.* and Chan, A.S.C. Synthesis of novel dihydrofuro[b]-pyridinone derivatives: oxidation coupling of 3-hydroxy-4(1H)-pyridinone with beta-dicarbonyl compounds.Tetrahedron Lett 2005, 46, 5085-5088.
  30. Bu, X.Z.; Wu, X.M.; Ng, N.L.J.; Mak, C.K.; Qin, C.G.; Guo, Z.H. Synthesis of gramicidin S and its analogues via an on-resin macrolactamization assisted by a predisposed conformation of the linear precursors.J Org Chem 2004, 69, 2681-2685.
  31. Bu, X.Z.; Xie, G.Y.; Law, C.W.; Guo, Z.H. An improved deblocking agent for direct Fmoc solid-phase synthesis of peptide thioesters.Tetrahedron Lett 2002, 43, 2419-2422.
  32. Bu, X.Z.; Wu, X.M.; Xie, G.Y.; Guo, Z.H. Synthesis of tyrocidine A and its analogues by spontaneous cyclization in aqueous solution.Org Lett 2002, 4, 2893-2895.
  33. Bu, X.Z.; Huang, Z.S.; Zhang, M.; Ma, L.; Xiao, G.W.; Gu, L.Q. Synthesis of new 1,1-dimethyl-1,2,3,4-tetrahydrophenanthrene derivatives.Tetrahedron Lett 2001, 42, 5737-5740.發明專利:
  34. 卜憲章,陳道遠,温格思,一類環十肽分子及其應用,申請號:201710104115.9;申請日期:2017.02.24
  35. 卜憲章,朱翠革,嶽欣,左應林,陳雨,温格思,鄰苯基查爾酮類化合物及其製備方法和應用,申請號:PCT/CN2015/070651,申請日期:2015.01.14;國際專利PCT申請
  36. 卜憲章,朱翠革,左應林,杜軍,温格思,嶽欣,陳雨,一種鄰苯基查爾酮類化合物在熒光探針中的應用,申請號:201410353793.5;申請日期:2014.07.23
  37. 卜憲章,朱翠革,嶽欣,左應林,陳雨,温格思,鄰苯基查爾酮類化合物及其製備方法和應用,申請號:201410032845.9;申請日期:2014.01.23,授權公告日,2016.06.08
  38. 卜憲章,吳海強,黃磊,一種硫氧還蛋白還原酶熒光探針及其製備方法和用途,申請號:201410137070.1;申請日期:2014.04.08
  39. 卜憲章,羅海彬,商娜娜,於豔君,杜軍,李哲,蔡穎紅,邵詠賢,何琳,一種取代吡咯色原酮類化合物在製備治療5型磷酸二酯酶相關疾病的藥物中的應用,申請號:201310017288.9;申請日期:2013.01.17,授權公告日:2015.8.26
  40. 卜憲章,劉培慶,於豔君,汪煜華,胡云,邵偉豔,杜軍,羥基取代的黃酮類化合物及其製備方法和應用。中華人民共和國知識產權局。申請號:201110269084.5.申請日期:2011年9月13日
  41. 卜憲章,胡云,於豔君,杜軍,邵偉豔,商娜娜,莊瑋,陸迪涵,劉巍,陳藝貞,温格思,氨基取代的黃酮類化合物及其製備方法和應用。中華人民共和國知識產權局。申請號:201110269753.9申請日期:2011年9月13日,授權公告日:2014.6.11
  42. 卜憲章左應林杜軍温格斯周斌華商娜娜,芳基取代查爾酮類化合物及其製備方法和應用中國專利申請號:201110217094.4授權公告日:2013年12月25日
  43. 卜憲章於豔君邵偉豔胡云黃壯裕左應林,一種多多取代色原酮並吡咯環類衍生物及其合成方法和應用,中國發明專利,專利號:ZL200910214553.6,申請日:2009.12.31授權公告日:2012.6.27
  44. 卜憲章,仇旭,霍應鵬,於豔君,金達平,古練權,具有抗腫瘤作用的多芳乙烯取代beta-二酮類化合物,中國發明專利,申請號:200810220580.X,申請日:2008.12.30,授權公告號CN101700995B,授權公告日:2013.06.05
  45. 卜憲章,邵偉豔,古練權,曹穎男,於志文,一種合成多肽及其應用,中國發明專利,專利號:ZL 200410077777.4,授權公告日:2007.2.21 [1] 
參考資料