Strategies for the inhibition of serine proteases

被引：82

作者：

Walker, B ^{[1
]}

Lynas, JF ^{[1
]}

机构：

[1] Queens Univ Belfast, Sch Pharm, Div Biomed Chem, Ctr Med Biol, Belfast BT9 7BL, Antrim, North Ireland

来源：

CELLULAR AND MOLECULAR LIFE SCIENCES | 2001年 / 58卷 / 04期

关键词：

serine proteases; synthetic inhibitors; peptide-based inhibitors; heterocyclic inhibitors; inhibitor design;

D O I：

10.1007/PL00000884

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：

Serine proteases have been shown to play a multifarious role in health and disease. As a result, there has been considerable interest in the design and development of synthetic inhibitors of these enzymes. In view of their diverse roles in biological processing events, one of the great challenges in such endeavours has been the need to produce compounds with exquisite selectivity. Inhibitor design has been broadly guided by the use of either peptide- or heterocyclic-based compounds, designed to exploit the known substrate specificity characteristics of individual enzymes. This review describes the thinking and strategies employed in such efforts.

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收藏

页码：596 / 624

页数：29

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