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Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.

Abstract：

:Hyperfibrinolytic situations can lead to life-threatening bleeding, especially during cardiac surgery. The approved antifibrinolytic agents such as tranexamic acid, ε-aminocaproic acid, 4-aminomethylbenzoic acid, and aprotinin were developed in the 1960s without the structural insight of their respective targets. Crystal structures of the main antifibrinolytic targets, the lysine binding sites on plasminogen's kringle domains, and plasmin's serine protease domain greatly contributed to the structure-based drug design of novel inhibitor classes. Two series of ligands targeting the lysine binding sites have been recently described, which are more potent than the most-widely used antifibrinolytic agent, tranexamic acid. Furthermore, four types of promising active site inhibitors of plasmin have been developed: tranexamic acid conjugates targeting the S1 pocket and primed sites, substrate-analogue linear homopiperidylalanine-containing 4-amidinobenzylamide derivatives, macrocyclic inhibitors addressing nonprimed binding regions, and bicyclic 14-mer SFTI-1 analogues blocking both, primed and nonprimed binding sites of plasmin. Furthermore, several allosteric plasmin inhibitors based on heparin mimetics have been developed.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Steinmetzer T,Pilgram O,Wenzel BM,Wiedemeyer SJA

doi

10.1021/acs.jmedchem.9b01060

subject

Has Abstract

pub_date

2020-02-27 00:00:00

pages

1445-1472

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

63

pub_type

杂志文章

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