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Sci. Signal., 10 November 2009
Vol. 2, Issue 96, p. ec363
[DOI: 10.1126/scisignal.296ec363]


Caspases Small-Molecule Protease Activator

Valda Vinson

Science, AAAS, Washington, DC 20005, USA

Human proteases regulate numerous biological processes. Most are stored as inactive proenzymes that are activated either by upstream processes or by self-proteolysis. Wolan et al. have identified a small molecule that activates the apoptotic procaspases-3 and -6. These caspases are homodimers, and the compound probably competitively inhibits one active site but stabilizes an on-state conformation that promotes self-cleavage by the unoccupied site. It may thus be possible to find other small-molecule activators for other proenzymes that should facilitate functional and mechanistic studies.

D. W. Wolan, J. A. Zorn, D. C. Gray, J. A. Wells, Small-molecule activators of a proenzyme. Science 326, 853–858 (2009). [Abstract] [Full Text]

Citation: V. Vinson, Small-Molecule Protease Activator. Sci. Signal. 2, ec363 (2009).

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