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- W2000482990 abstract "Proteases are well-established targets for pharmaceutical development because of their known enzymatic mechanism and their regulatory roles in many pathologies. However, many potent clinical lead compounds have been unsuccessful either because of a lack of specificity or because of our limited understanding of the biological roles of the targeted protease. In order to successfully develop protease inhibitors as drugs, it is necessary to understand protease functions and to expand the platform of inhibitor development beyond active site-directed design and in vitro optimization. Several newly developed technologies will enhance assessment of drug selectivity in living cells and animal models, allowing researchers to focus on compounds with high specificity and minimal side effects in vivo. In this review, we highlight advances in the development of chemical probes, proteomic methods and screening tools that we feel will help facilitate this paradigm shift in drug discovery." @default.
- W2000482990 created "2016-06-24" @default.
- W2000482990 creator A5003559845 @default.
- W2000482990 creator A5005853846 @default.
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- W2000482990 date "2012-01-01" @default.
- W2000482990 modified "2023-10-02" @default.
- W2000482990 title "New approaches for dissecting protease functions to improve probe development and drug discovery" @default.
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