彭师奇
在基于氨基酸的寡肽先导结构研究、基于氨基酸的杂环先导结构研究、基于甾体和多肽相互作用的先导结构研究,以及基于糖胺的先导结构研究等四个方向展开基础和应用基础研究。
个性化签名
- 姓名:彭师奇
- 目前身份:
- 担任导师情况:
- 学位:
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学术头衔:
博士生导师
- 职称:-
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学科领域:
药物化学
- 研究兴趣:在基于氨基酸的寡肽先导结构研究、基于氨基酸的杂环先导结构研究、基于甾体和多肽相互作用的先导结构研究,以及基于糖胺的先导结构研究等四个方向展开基础和应用基础研究。
1969年毕业于北京医学院、1981年获硕士学位、1984年获博士学位、1986年晋升为副教授、1987-1989 为联邦德国洪堡学者、1990年晋升为教授及博士生导师(已培养19名博士和6名硕士)、1992年为联邦德国洪堡学者、1998年联邦德国洪堡学者、1998-1999年任北京医科大学药学院副院长、1999-2000年任北京医科大学药学院院长、2000-2004年任北京大学药学院院长。2004年7月调首都医科大学任药学院院长。
主要社会兼织有:国家新药审评委员、国家自然科学基金委化学科学部有机化学学科评审专家、中国药学会药化专业委员会副主任委员、北京药学会副秘书长、“药学教育” 副主编、“北京大学学报医学版” 副主编、“中国新药杂志”常务编委、“中国药物化学杂志”常务编委、“全国高等医药院校药学类教材” 编委会副主编。在基于氨基酸的寡肽先导结构研究、基于氨基酸的杂环先导结构研究、基于甾体和多肽相互作用的先导结构研究,以及基于糖胺的先导结构研究等四个方向展开基础和应用基础研究。
获得的荣誉有:卫生部“全国卫生系统优秀留学回国人员” (1990年)、国家教委“有突出贡献的中国博士学位获得者”(1991年)、1993年开始享受国务院颁发的特殊津贴、北京市师德个人先进(2001年)。
出版了六部专著。申请了39项发明专利。获得了10项国家和省部级科技进步及教学成果奖。有5种产品上市、参研的1个一类新药获得临床批文、主研的1个二类新药和1个四类新药正在申请新药证书。在国内核心期刊发表了大约160篇学术论文、在国际知名期刊发表了41篇(SCI)学术论文。
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266
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成果数
10
彭师奇, Caixia Huo, † Chao Wang, † Ming Zhao, † and Shiqi Peng*, ‡
Chem. Res. Toxicol. 2004, 17, 1112-1120,-0001,():
-1年11月30日
N-(1-Deoxy-D-fructos-1-yl)-L-amino acids isolated from hog liver are endogenous lead decorporation substances with low toxicity and cell membrane crossing ability. To simulate the effect of the natural N-(1-deoxy-D-fructos-1-yl)-L-amino acids on lead decorporation, a ser ies of the epimerically pure N-(1-deoxy-D-fructos-1-yl)-L-amino acids (6a-eβ) were synthesized, and their usefulness as antagonists of lead intoxication was investigated. The results suggest that after treatment with 6a-eβ the liver, kidney, bone, and brain, lead levels of mice were significantly reduced in comparison with the control group. Except for bone and brain lead levels of the mice after chelating treatment with 6dβ, all of the other tissue lead levels of mice after chelating treatment with 6a-eβ are significantly lower than those of mice after treatment with DL-penicillamine (p<0.05). All fecal lead levels of mice after treatment with 6a-eβ are significantly higher than those of mice after treatment with 0.9% saline (controls) and DLpenicillamine (p<0.05-0.01). The effects of all chelating agents on urinary excretion of lead in mice are clearly superior to the control (p<0.05-0.01). The results of the present studies on repeated lead exposure indicated that at tested levels of i.p. injections, the fructose-amino acids were effective antagonists of lead poisoning under the experimental conditions. After treatment with the chelators, the concentration of essential metals in mice did not exhibit change as compared to the control. The effects of the compounds on cadmium decorporation were also investigated, and similar results were observed.
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【期刊论文】The synthesis, distribution, and anti-hepatic cancer activity of YSL
彭师奇, Wenfeng Ding, b Jiali Zhang, c Zhi Yao, d Rong Lu, d Dezhu Wu, e Ginfu Li, e Zilong Shen, c Yingji Sun, c Gang Lin, f Chao Wang, b Ming Zhao b and Shiqi Peng a, *
Bioorganic & Medicinal Chemistry 12(2004)4989-4994,-0001,():
-1年11月30日
YSL was prepared stepwise from C terminal to N terminal with the side chain un-protective amino acids, Boc-Leu-OMe, Boc-Ser-OH, and Boc-Tyr-OH, as the starting materials in 39.5% total yield (31.2g/per batch). With the side chain un-protective Boc-(3,5-dibromo)-Tyr-OH and HCl
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【期刊论文】The synthesis and immunosuppressive activities of steroid-urotoxin linkers
彭师奇, Chao Wang, b Ming Zhao, b Xuecai Qiub and Shiqi Peng a, *
Bioorganic & Medicinal Chemistry 12(2004)4403-4421,-0001,():
-1年11月30日
as prolongation of heterotopic transplanted cardiac tissue survival in vivo, inhibitory effects on phagocytosis of mouse peritoneal macrophages and concanavalin (ConA) or lipopolysaccharide (LPS) induced proliferation of mouse spleen lymphocytes in vitro show that at the comparable concentrations the immunosuppressive activities of the steroid-urotoxin linkers 7a-d, 8a-d, 9a,b, and 10a,b were higher than that of hydrocortisone, prednisolone, and the urotoxins alone, as well as significantly higher than that of the mixture of hydrocortisone and urotoxins or prednisolone and urotoxins. The so-called 'permissive action' may be responsible for the enhancement of the mentioned bioactivities of the steroid–urotoxin linkers 7a-d, 8a-d, 9a,b, and 10a,b.
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彭师奇, Ming Zhao, a Chao Wang, a Jiangyuan Liu, a Kexiang Zhou c and Shiqi Peng b, *
Bioorganic & Medicinal Chemistry 12(2004)2275-2286,-0001,():
-1年11月30日
The in vitro and in vivo thrombolytic activities of Ala-Arg-Pro-Ala-Lys-OH, its analogs and the related peptides were assayed. The results indicate that when 5Lys of Ala-Arg-Pro-Ala-Lys-OH is changed into 5Arg, and 3Lys of Pro-Ala-Lys-OH is changed into 3Arg the thrombolytic activities are collapsed; when Pro-Ala-Lys-OH is changed into Ala-Pro-Lys-OH, and Ala-Arg-Pro-Ala-Lys-OH is changed into Ala-Arg-Ala-Pro-Lys-OH the thrombolytic activities are also collapsed; when 5Lys of Ala-Arg- Pro-Ala-Lys-OH is changed into 5nLeu the thrombolytic activities are again collapsed. All of the results indicate that for the thrombolytic activities of Ala-Arg-Pro-Ala-Lys-OH and the related peptides Pro-Ala-Lys-OH exhibits either amino acid composition specificity or sequence specificity. The composition and sequence specificity of Pro-Ala-Lys-OH reflects its rule as the pharmacophore of P6A and the related peptides.
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【期刊论文】Synthesis and Thrombolytic Activity of Fibrinogen Fragment Related Cyclopeptides
彭师奇, Ming Zhao, Na Lin, Chao Wang and Shiqi Peng*
Bioorganic & Medicinal Chemistry Letters 13(2003)961-964,-0001,():
-1年11月30日
In the modification of the fibrinogen fragment related sequences ARPAK, QRPAK GRPAK and KRPAK, the corresponding cyclo-ARPAK, cyclo-QRPAK, cyclo-GRPAK, and cyclo-KRPAK were prepared in the diluted solution. The bioassay in vivo indicated that the thrombolytic potencies of cyclo-ARPAK, cyclo-GRPAK, cyclo-QRPAK, and cyclo-KRPAK were significantly higher than that of ARPAK, QRPAK, GRPAK, and KRPAK. In water, the cyclopeptides were incubated with pepsin or trypsin at 37 C for 64h. There was no degradation product observed, on the other hand, with the same condition, the peptides were completely hydrolyzed in 8h. The relationships among the rigidity or the conformation and the thrombolytic activity in vivo and the stability to enzyme-induced hydrolysis in vitro of the cyclopeptides were discussed.
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【期刊论文】Synthesis and Bioactivities of Nitronyl Nitroxide and RGD Containing Pseudopeptides
彭师奇, Junling Liu, Ming Zhao, Chao Wang and Shiqi Peng*
Bioorganic & Medicinal Chemistry Letters 13(2003)4065-4069,-0001,():
-1年11月30日
1-(1′,3′-Dioxyl-4′,4′,5′,5′-tetramethyldihydroimidazol-2′-yl)-phenyl-4-yloxylacetic acid (3), and 1-(1′,3′-dioxyl-4′,4′,5′,5′-tetramethyldihydroimidazol-2′-yl)-phenyl-4-yloxylacetyl-RGDS (13), -RGDV (14), -RGDF (15) were synthesized. The ESR measurement gave the same spectroscopy for 3 and 13-15. The NO scavenging tests in vitro, anti-platelet aggregation tests in vitro and the anti-thrombosis assay in vivo indicated that introducing 3 into the N-terminal of RGDS, RGDV and RGDF the corresponding bioactivities for both of 3 and RGD peptides can be remained completely. The present combinations provided a beneficial strategy for simultaneous scavenging NO and anti-thrombosis, and for the use of spin label of RGD peptides in the conformational researches.
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【期刊论文】Studies on the Synthesis and Anti-Osteoporosis of Estrogen-GHRPs Linkers
彭师奇, Chao Wang, Weina Cui, Ming Zhao, Jian Yang and Shiqi Peng*
Bioorganic & Medicinal Chemistry Letters 13(2003)143-146,-0001,():
-1年11月30日
The linkers of estrogen-GHRPs were prepared by the combination of estradiol, estrone, TyrGlyGlyPheLeuOH, and TyrGlyGlyPheLeuOH. Their anti-osteoporosis effect was evaluated by analyzing the data, for instance the weight of the body, femur, femur ash, the content of calcium and phosphor in the femur, the content of calcium and ALP activity in the serum, obtained from the corresponding bioassay in vivo. The results indicated that the anti-osteoporosis potency for estradiol, estrone, TyrGlyGlyPheLeuOH and TyrGlyGlyPheLeuNH2 may be totally enhanced each other via the corresponding linkers.
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【期刊论文】Synthesis and analgesic effects of kyotorphin-steroid linkers
彭师奇, Chao Wang, Ming Zhao, Jian Yang, Shiqi Peng*
Steroids 66(2001)811-815,-0001,():
-1年11月30日
Kyotorphin (KTP, H-Tyr-Arg-OH) was covalently bonded with hydrocortisone or estrone to form the corresponding hydrocortisone-21-O-yl-succinyl-Tyr-ArgOH or estrone-3-O-yl-acyl-Tyr-Arg-OH. Their analgesic activities were investigated using the tail flick test. The potency of the two linkers were significantly higher than that of KTP and the mixture of KTP and hydrocortisone or estrone in the CNS and/or the periphery administration.
Hydrocortisone, Estrone, Kyotorphin, Linker, Analgesia
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【期刊论文】Diasteroselective Cyclizations with Enantiopure Malonaldehyde Monocycloacetals
彭师奇, Lanrong Bi, † Ming Zhao, † Chao Wang, † Shiqi Peng, *, † and Ekkehard Winterfeldt‡
J. Org. Chem. 2002, 67, 22-26,-0001,():
-1年11月30日
The synthesis of a series of enantiopure malonaldehyde monocycloacetals is described. Treatment of 8b with L-tryptophan methyl ester, 5-methoxytryptamine, and tryptamine, respectively, in the Pictet-Spengler condensation gave the corresponding enantiomerically pure key precursors 1-3 and 17-21 in only two steps. Using a chiral amino-diol successfully realized the kinetic resolution of racemic carbolines 23 and 24.
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【期刊论文】Identification, Synthesis and Bioassay for the Metabolites of P6A
彭师奇, Ming Zhao, Chao Wang, Jian Yang, Jiangyuan Liu, Youxuan Xu, Yanfen Wu and Shiqi Peng*
Bioorganic & Medicinal Chemistry 11(2003)4913-4920,-0001,():
-1年11月30日
The metabolites Ala-Arg-Pro-Ala-OH, Ala-Arg-Pro-OH, Arg-Pro-Ala-Lys-OH and Pro-Ala-Lys-OH were identified by HPLC/ESI/MS from the in vivo blood of Ala-Arg-Pro-Ala-Lys-OH (P6A) received mice. The in vitro incubation of P6A in the blood of mice the same metabolites were also found by use of the Prep LC System. The protective intermediates of these metabolites were prepared via the solution method using the stepwise synthesis in 77.4, 90, 88, and 80% yield, respectively. After deprotection with catalytic hydrogenation the intermediates were converted into the corresponding sequences Arg-Pro-Ala-Lys-OH, Pro-Ala-Lys-OH, Ala-Arg-Pro-Ala-OH, and Ala-Arg-Pro-OH in 90, 95, 85% and 86% yield, respectively. In the thrombolysis in vivo assay the synthetic Ala-Arg-Pro-Ala-OH, and Ala-Arg-Pro-OH exhibited no activity. On the other hand the thrombolytic activity of Arg-Pro-Ala-Lys-OH was comparable to P6A, and an enhanced thrombolytic activity was observed for Pro-Ala-Lys-OH. In the in vitro fibrinolytic lysis tests the approximate results were obtained and an enhanced activity was also observed for Pro-Ala-Lys-OH. In the euglobulin clot lysis time tests P6A, Arg-Pro-Ala-Lys-OH and Pro-Ala-Lys-OH gave significantly shorter time than that given by UK, demonstrating their fast action.
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