Abstract
In comparison to the huge number of peptidic and peptidomimetic inhibitors of cysteine proteases which have been developed during the last twenty years the number of non-peptidic compounds with cysteine protease inhibiting properties is restricted to a few substance classes. In contrast to peptidic and peptidomimetic inhibitors the non-peptidic lead structures have mainly been discovered by computational or enzymatic industrial screenings and not by a rational approach. But, the growing number of resolved X-ray structures of the target enzymes as well as molecular modeling methods have supported the further development of potent inhibitors beginning from these lead structures. In this review we will focus on new non-peptidic cysteine protease inhibitors which have been developed during the last years. Discovery, structure-activity-relationship and inhibition mechanisms will be discussed.
Keywords: cysteine proteases, peptidomimetic cysteine protease inhibitors, papain-like cysteine
Mini-Reviews in Medicinal Chemistry
Title: Non-Peptidic Inhibitors of Cysteine Proteases
Volume: 3 Issue: 4
Author(s): T. Schirmeister and U. Kaeppler
Affiliation:
Keywords: cysteine proteases, peptidomimetic cysteine protease inhibitors, papain-like cysteine
Abstract: In comparison to the huge number of peptidic and peptidomimetic inhibitors of cysteine proteases which have been developed during the last twenty years the number of non-peptidic compounds with cysteine protease inhibiting properties is restricted to a few substance classes. In contrast to peptidic and peptidomimetic inhibitors the non-peptidic lead structures have mainly been discovered by computational or enzymatic industrial screenings and not by a rational approach. But, the growing number of resolved X-ray structures of the target enzymes as well as molecular modeling methods have supported the further development of potent inhibitors beginning from these lead structures. In this review we will focus on new non-peptidic cysteine protease inhibitors which have been developed during the last years. Discovery, structure-activity-relationship and inhibition mechanisms will be discussed.
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Cite this article as:
Schirmeister T. and Kaeppler U., Non-Peptidic Inhibitors of Cysteine Proteases, Mini-Reviews in Medicinal Chemistry 2003; 3 (4) . https://dx.doi.org/10.2174/1389557033488079
DOI https://dx.doi.org/10.2174/1389557033488079 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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