Protease inhibitors in the clinic

Abbenante, Giovanni and Fairlie , David P. (2005) Protease inhibitors in the clinic. Medicinal Chemistry, 1 1: 71-104. doi:10.2174/1573406053402569

Author Abbenante, Giovanni
Fairlie , David P.
Title Protease inhibitors in the clinic
Journal name Medicinal Chemistry   Check publisher's open access policy
ISSN 1573-4064
Publication date 2005-01-01
Sub-type Article (original research)
DOI 10.2174/1573406053402569
Volume 1
Issue 1
Start page 71
End page 104
Total pages 24
Place of publication Oak Park, IL, USA
Publisher Bentham Science Publishers Ltd.
Language eng
Subject 03 Chemical Sciences
Abstract This review describes the clinical status (based on available information) of experimental drugs that inhibit enzymes called proteases, or more precisely a sub-class of proteases called peptidases that catalyse the hydrolysis of polypeptide main chain amide bonds. These peptidases are classified by the key catalytic residue in the active site of the enzyme that effects hydrolysis, namely aspartic, serine, cysteine, metallo or threonine proteases. In this review we show structures for 108 inhibitors of these enzymes and update the clinical disposition of over 100 inhibitors that have been considered worthy enough by pharmaceutical, biotechnology or academic researchers and their financial backers to be trialed in humans as prospective medicines. We outline some of their chemical and pharmacological characteristics and compare the current status of protease inhibitors in the clinic with what was observed about 5 years ago (Leung et al, J. Med. Chem. 2000, 43, 305-341). We assess the progress of protease inhibitors into man, predict their futures, and outline some of the hurdles that have been overcome and that still remain for this promising class of new therapeutic agents.
Keyword Protease
Q-Index Code C1
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Excellence in Research Australia (ERA) - Collection
Institute for Molecular Bioscience - Publications
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Created: Sat, 16 May 2009, 00:35:26 EST by Ms Lynette Adams on behalf of Institute for Molecular Bioscience