Exosite Explained

An exosite is a secondary binding site, remote from the active site, on an enzyme or other protein.^[1]

This is similar to allosteric sites, but differs in the fact that, in order for an enzyme to be active, its exosite typically must be occupied.^[2] Exosites have recently become a topic of increased interest in biomedical research as potential drug targets.^{[3] [4]}

External links

• Arnaud . E . Lafay . M . Gaussem . P . Picard . V . Jandrot-Perrus . M . Aiach . M . Rendu . F . An autoantibody directed against human thrombin anion-binding exosite in a patient with arterial thrombosis: effects on platelets, endothelial cells, and protein C activation . Blood . 15 September 1994 . 84 . 6 . 1843–1850 . 10.1182/blood.V84.6.1843.1843 . 8080990 . free .

Notes and References

1. Yegneswaran . S. . Tiefenbrunn . T. K. . Fernández . J. A. . Dawson . P. E. . Manipulation of thrombin exosite I, by ligand-directed covalent modification . Journal of Thrombosis and Haemostasis . October 2007 . 5 . 10 . 2062–2069 . 10.1111/j.1538-7836.2007.02712.x . 17883702 . 38198958 .
2. Lockett . J. M. . Sheehan . J. P. . Mast . A. E. . Binding at two distinct exosites is required for activation of prothrombin by prothrombinase . Journal of Thrombosis and Haemostasis . 1 . Supplement 1 . July 2003 . https://web.archive.org/web/20041126131935/http://www.blackwellpublishing.com/isth2003/abstract.asp?id=9231 . 2004-11-26 .
3. Müller . Jens . Isermann . Berend . Dücker . Christina . Salehi . Mohammad . Meyer . Moritz . Friedrich . Max . Madhusudhan . Thati . Oldenburg . Johannes . Mayer . Günter . Pötzsch . Bernd . An Exosite-Specific ssDNA Aptamer Inhibits the Anticoagulant Functions of Activated Protein C and Enhances Inhibition by Protein C Inhibitor . Chemistry & Biology . April 2009 . 16 . 4 . 442–451 . 10.1016/j.chembiol.2009.03.007 . 19389630 .
4. Book: Serine Endopeptidases: Advances in Research and Application: 2011 Edition . 2012 . ScholarlyEditions . 978-1-4649-2658-7 .