Publisher： Bentham Science Publishers
E-ISSN： 1873-4294|10|3|231-231
ISSN： 1568-0266
Source： Current Topics in Medicinal Chemistry, Vol.10, Iss.3, 2010-02, pp. : 231-231
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Abstract
Members of the protease families discussed in this issue are of great interest for different therapeutic areas tackling contemporary afflictions of mankind such as cardiovascular, infective, or respiratory diseases as well as cancer. The proteases dealt with not only act as protein-degrading enzymes, their important function within signaling pathways makes them also highly attractive as valid drug targets. The search for as well as the identification of potent and selective inhibitors for this protein family has been very popular for decades and still is a highly competitive field in industrial and academic drug research development.This special issue of Current Topics in Medicinal Chemistry “The Medicinal Chemistry of Protease Inhibitors” focuses on inhibitors of different protease classes and is divided into three major parts: the first part discusses inhibitors for particular members of the threonine, serine, and cysteine protease family, the second gives an overview of proteases and their inhibitors involved in infectious diseases, and the third part reviews hit validation, conducting as well as pitfalls frequently occurring in protease assays.The issue starts with a review of Genin, Reboud-Ravaux, and Vidal on recent advances and new perspectives of proteasome inhibitors. The well-known covalent inhibitors for this member of the threonine protease family as well as recent developments towards first non-covalent derivatives are discussed.In the following, Straub, Rohrig, and Hillisch highlight the field of factor Xa, representing one example of the serine protease family, and its corresponding inhibitors. Their review concentrates on different non-basic P1-site inhibitors and describes in particular the development of Rivaroxaban (Xarelto™).The family of cysteine proteases and their inhibitors are presented within two contributions. Pietsch, Chua, and Abell introduce into the field of calpains as attractive drug targets and inhibitors thereof, followed by an article of Frizler, Stirnberg, Sisay, and Gütschow discussing nitrile-based peptidic inhibitors for the subfamily of cathepsins.The subsequent part of this issue focuses on proteases that are suitable drug targets to combat infectious diseases. The aim of this part is to give a survey of active compounds inhibiting proteases of different classes but share their quality of being active in only one therapeutic category.Steuber and Hilgenfeld describe the class of viral proteases which are investigated within the antiviral drug discovery. A second topic, summarized in a review of Wegscheid-Gerlach, Gerber and Diederich, deals with different malarial proteases of plasmodium falciparum and inhibitors thereof.In the final part of this issue, Ludewig, Kossner, Schiller, Baumann, and Schirmeister discuss in their contribution entitled “Enzyme kinetics and hit validation in fluorimetric protease assays” common problems frequently occurring in fluorimetric assays. They furthermore provide methods and strategies concerning problem solving as well as circumventive measures prior to assay determination.We very much appreciated the valuable contributions of all authors to this special issue of Current Topics in Medicinal Chemistry entitled “The Medicinal Chemistry of Protease Inhibitors”. We would also like to thank all reviewers for their very constructive comments.We are also grateful to the editor-in-chief, Dr. Allen Reitz, for the invitation and the opportunity to compile this special issue as guest editors and for all his support concerning the preparation of this special issue.
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