The design and evaluation of heparin-binding foldamers

被引:67
作者
Choi, S
Clements, DJ
Pophristic, V
Ivanov, I
Vemparala, S
Bennett, JS
Klein, ML
Winkler, JD
DeGrado, WE [1 ]
机构
[1] Univ Penn, Dept Chem, Philadelphia, PA 19104 USA
[2] Univ Penn, Dept Biochem & Biophys, Philadelphia, PA 19104 USA
[3] Univ Sci Philadelphia, Dept Chem & Biochem, Philadelphia, PA 19104 USA
[4] Univ Penn, Dept Med, Div Hematol & Oncol, Philadelphia, PA 19104 USA
关键词
antithrombin; heparin; inhibitors; oligomers; protein interactions;
D O I
10.1002/anie.200501279
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Controlling blood loss: The synthesis of a series of arylamide oligomers 1, which interact with heparin is described. The heparin-small molecule interaction inhibits the heparin's ability to activate antithrombin. These arylamide oligomers are the first example of low-molecular-weight antagonists that inhibit the anticoagulant function of heparin. (Chemical Equation Presented). © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:6685 / 6689
页数:5
相关论文
共 33 条
  • [1] Electrostatics of nanosystems: Application to microtubules and the ribosome
    Baker, NA
    Sept, D
    Joseph, S
    Holst, MJ
    McCammon, JA
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2001, 98 (18) : 10037 - 10041
  • [2] Capila I, 2002, ANGEW CHEM INT EDIT, V41, P391
  • [3] Capila I., 2002, ANGEW CHEM, V114, P426, DOI DOI 10.1002/1521-3757(20020201)114:33.0.CO
  • [4] 2-Q
  • [5] MOLECULAR MODELING OF PROTEIN-GLYCOSAMINOGLYCAN INTERACTIONS
    CARDIN, AD
    WEINTRAUB, HJR
    [J]. ARTERIOSCLEROSIS, 1989, 9 (01): : 21 - 32
  • [6] Chang LC, 2001, AAPS PHARMSCI, V3, part. no.
  • [7] Pattern and spacing of basic amino acids in heparin binding sites
    Fromm, JR
    Hileman, RE
    Caldwell, EEO
    Weiler, JM
    Linhardt, RJ
    [J]. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1997, 343 (01) : 92 - 100
  • [8] DIFFERENCES IN THE INTERACTION OF HEPARIN WITH ARGININE AND LYSINE AND THE IMPORTANCE OF THESE BASIC-AMINO-ACIDS IN THE BINDING OF HEPARIN TO ACIDIC FIBROBLAST GROWTH-FACTOR
    FROMM, JR
    HILEMAN, RE
    CALDWELL, EEO
    WEILER, JM
    LINHARDT, RJ
    [J]. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1995, 323 (02) : 279 - 287
  • [9] Foldamers: A manifesto
    Gellman, SH
    [J]. ACCOUNTS OF CHEMICAL RESEARCH, 1998, 31 (04) : 173 - 180
  • [10] A field guide to foldamers
    Hill, DJ
    Mio, MJ
    Prince, RB
    Hughes, TS
    Moore, JS
    [J]. CHEMICAL REVIEWS, 2001, 101 (12) : 3893 - 4011