NEW TRIPEPTIDIC THROMBIN INHIBITORS - INFLUENCE OF P2 AND P3 RESIDUES ON ACTIVITY AND SELECTIVITY

被引：14
|
作者：
DENANTEUIL, G
GLOANEC, P
LILA, C
PORTEVIN, B
BOUDON, A
RUPIN, A
VERBEUREN, TJ
机构：
[1] INST RECH SERVIER,DIV MED CHEM,F-92150 SURESNES,FRANCE
[2] INST RECH SERVIER,DIV MOLEC MODELING,F-92150 SURESNES,FRANCE
[3] INST RECH SERVIER,DIV ANGIOL,F-92150 SURESNES,FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 1995年 / 3卷 / 08期
关键词：
D O I：
10.1016/0968-0896(95)00107-R
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Structural variations of P2 and P3 residues in tripeptidic boroarginine thrombin inhibitors led to compounds with similar potency than reference compound DuP 714, but with enhanced selectivity for thrombin compared to plasmin.
引用
下载
收藏
页码：1019 / 1024
页数：6
相关论文
共 50 条
  • [21] Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif
    Kreutter, Kevin D.
    Lu, Tianbao
    Lee, Lily
    Giardino, Edward C.
    Patel, Sharmila
    Huang, Hui
    Xu, Guozhang
    Fitzgerald, Mark
    Haertlein, Barbara J.
    Mohan, Venkatraman
    Crysler, Carl
    Eisennagel, Stephen
    Dasgupta, Malini
    McMillan, Martin
    Spurlino, John C.
    Huebert, Norman D.
    Maryanoff, Bruce E.
    Tomczuk, Bruce E.
    Damiano, Bruce P.
    Player, Mark R.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (09) : 2865 - 2870
  • [22] AUTOMORPHISM GROUPS OF FINITE RINGS OF CHARACTERISTIC p2 AND p3
    Chikunji, Chiteng'A John
    GLASNIK MATEMATICKI, 2008, 43 (01) : 25 - 40
  • [23] PLASMIN SPECIFIC INHIBITORS: OPTIMIZATION OF THE P2 AND P1' RESIDUES
    Iwasa, N.
    Masuda, T.
    Kuno, M.
    Hidaka, K.
    Hojo, K.
    Gohda, K.
    Teno, N.
    Wanaka, K.
    Tsuda, Y.
    JOURNAL OF PEPTIDE SCIENCE, 2016, 22 : S146 - S146
  • [24] Design and synthesis of 6,6-fused bicyclic lactams as P2,P3 dipeptide mimetics of catalytic site directed thrombin inhibitors.
    Tarazi, M
    DiMaio, J
    Siddiqui, MA
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1997, 214 : 52 - MEDI
  • [25] Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes
    Jaishankar, Priyadarshini
    Hartsell, Elizabeth
    Zhao, Dong-Mei
    Doyle, Patricia S.
    McKerrow, James H.
    Renslo, Adam R.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (02) : 624 - 628
  • [26] Short Remark on (p1,p2,p3)-Complex Numbers
    Richter, Wolf-Dieter
    SYMMETRY-BASEL, 2024, 16 (01):
  • [27] RENIN INHIBITORS BASED ON NOVEL DIPEPTIDE ANALOGS - INCORPORATION OF THE HYDROXYETHYLENE ISOSTERE AT THE P2/P3 SITES
    KEMPF, DJ
    DELARA, E
    PLATTNER, JJ
    STEIN, H
    COHEN, J
    MARCOTTE, P
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1987, 194 : 85 - MEDI
  • [28] CIGS P1, P2, AND P3 LASER SCRIBING WITH AN INNOV
    Murison, R.
    Dunsky, C.
    Rekow, M.
    Dinkel, C.
    Pern, J.
    Mansfield, L.
    Panarello, T.
    Nikumb, S.
    35TH IEEE PHOTOVOLTAIC SPECIALISTS CONFERENCE, 2010,
  • [29] P2, P3, P4-free linear forests are antimagic
    Shang, Jen-Ling
    UTILITAS MATHEMATICA, 2016, 101 : 13 - 22
  • [30] Roles of the P1, P2, and P3 residues in determining inhibitory specificity of kallistatin toward human tissue kallikrein
    Chen, VC
    Chao, L
    Chao, J
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (49) : 38457 - 38466
12345