Increased stability of peptidesulfonamide peptidomimetics towards protease catalyzed degradation

被引:63
作者
de Bont, DBA [1 ]
Sliedregt-Bol, KM [1 ]
Hofmeyer, LJF [1 ]
Liskamp, RMJ [1 ]
机构
[1] Univ Utrecht, Dept Med Chem, Utrecht Inst Pharmaceut Sci, NL-3508 TB Utrecht, Netherlands
关键词
peptides and polypeptides; isosteres; aminoacids and derivatives; solid-phase synthesis;
D O I
10.1016/S0968-0896(99)00021-8
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
Replacement of amide bonds in peptides by sulfonamide moieties resulted in peptidosulfonamides with an increased stability towards protease catalyzed degradation. In addition to protection of the protease cleavage site, it was found that introduction of a sulfonamide also influenced the stability of adjacent amide bonds. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1043 / 1047
页数:5
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