PT  - JOURNAL ARTICLE
AU  - Vinson, Valda
TI  - Small-Molecule Protease Activator
AID  - 10.1126/scisignal.296ec363
DP  - 2009 Nov 10
TA  - Science Signaling
PG  - ec363--ec363
VI  - 2
IP  - 96
4099  - http://stke.sciencemag.org/content/2/96/ec363.short
4100  - http://stke.sciencemag.org/content/2/96/ec363.full
SO  - Sci. Signal.2009 Nov 10; 2
AB  - 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]