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Aspartic proteases in drug discovery.

Eder, Joerg, Hommel, Ulrich, Cumin, Frederic, Martoglio, Bruno and Gerhartz, Bernd (2007) Aspartic proteases in drug discovery. Current Pharmaceutical Design, 13 (3). pp. 271-285. ISSN 1873-4286


Aspartic proteases are the smallest class of human proteases with only 15 members. Over the past years, they have received considerable attention as potential targets for pharmaceutical intervention since many have been shown to play important roles in physiological and pathological processes. Despite numerous efforts, however, the only inhibitors for aspartic proteases currently on the market are directed against the HIV protease, an aspartic protease of viral origin. Nevertheless, several inhibitors including those targeting renin, BACE1 and gamma-secretase are in clinical or preclinical development, and some other aspartic proteases are discussed as potential drug target. The crystal structures of seven human aspartic proteases have now been solved and, together with a detailed kinetic understanding of their catalytic mechanism, this has greatly contributed to the design and discovery of novel inhibitors for this protease class. This review describes current aspartic protease drug targets and summarizes the drug discovery efforts in this field. In addition, it highlights recent developments which may lead to a new generation of aspartic protease inhibitors.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Protease; Aspartic protease inhibitor; BACE; HIV-protease; Renin; Presenilin
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Date Deposited: 14 Dec 2009 13:58
Last Modified: 31 Jan 2013 01:14


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