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Review
. 2007 Feb;113(2):354-68.
doi: 10.1016/j.pharmthera.2006.09.001. Epub 2006 Sep 22.

Protease inhibitors and their peptidomimetic derivatives as potential drugs

Georgie Fear  1 , Slavko Komarnytsky, Ilya Raskin
Affiliations
Review

Protease inhibitors and their peptidomimetic derivatives as potential drugs

Georgie Fear et al. Pharmacol Ther. 2007 Feb.

Abstract

Precise spatial and temporal regulation of proteolytic activity is essential to human physiology. Modulation of protease activity with synthetic peptidomimetic inhibitors has proven to be clinically useful for treating human immunodeficiency virus (HIV) and hypertension and shows potential for medicinal application in cancer, obesity, cardiovascular, inflammatory, neurodegenerative diseases, and various infectious and parasitic diseases. Exploration of natural inhibitors and synthesis of peptidomimetic molecules has provided many promising compounds performing successfully in animal studies. Several protease inhibitors are undergoing further evaluation in human clinical trials. New research strategies are now focusing on the need for improved comprehension of protease-regulated cascades, along with precise selection of targets and improved inhibitor specificity. It remains to be seen which second generation agents will evolve into approved drugs or complementary therapies.

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Figures

Fig. 1
Fig. 1
Examples of naturally occurring and peptidomimetic protease inhibitors which have been approved or are currently in advanced clinical trials.
See this image and copyright information in PMC

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