Cancer Institute A national cancer institute
designated cancer center

Matthew Bogyo

Publication Details

  • New approaches for dissecting protease functions to improve probe development and drug discovery NATURE STRUCTURAL & MOLECULAR BIOLOGY Deu, E., Verdoes, M., Bogyo, M. 2012; 19 (1): 9-16

    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.

    View details for DOI 10.1038/nsmb.2203

    View details for Web of Science ID 000299046000004

    View details for PubMedID 22218294

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