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Inhibitors of kallikrein‐related peptidases: An overview
Author(s) -
Masurier Nicolas,
Arama Dominique P.,
El Amri Chahrazade,
Lisowski Vincent
Publication year - 2018
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.21451
Subject(s) - kallikrein , chemistry , pharmacology , computational biology , medicine , biology , biochemistry , enzyme
Kallikrein‐related peptidases (KLKs) are a family of 15 secreted serine proteases that are involved in various physiological processes. Their activities are subtly regulated by various endogenous inhibitors, ranging from metallic ions to macromolecular entities such as proteins. Furthermore, dysregulation of KLK activity has been linked to several pathologies, including cancer and skin and inflammatory diseases, explaining the numerous efforts to develop KLK‐specific pharmacological inhibitors as potential therapeutic agents. In this review, we focus on the huge repertoire of KLKs inhibitors reported to date with a special emphasis on the diversity of their molecular mechanisms of inhibition.