An exosite is a secondary binding site, remote from the active site, on an enzyme or other protein.
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. Exosites have recently become a topic of increased interest in biomedical research as potential drug targets.
References
- Yegneswaran, S.; Tiefenbrunn, T. K.; Fernández, J. A.; Dawson, P. E. (October 2007). "Manipulation of thrombin exosite I, by ligand-directed covalent modification". Journal of Thrombosis and Haemostasis. 5 (10): 2062–2069. doi:10.1111/j.1538-7836.2007.02712.x. PMID 17883702. S2CID 38198958.
- Lockett, J. M.; Sheehan, J. P.; Mast, A. E. (July 2003). "Binding at two distinct exosites is required for activation of prothrombin by prothrombinase". Journal of Thrombosis and Haemostasis. 1 (Supplement 1). Archived from the original on 2004-11-26.
- Müller, Jens; Isermann, Berend; Dücker, Christina; Salehi, Mohammad; Meyer, Moritz; Friedrich, Max; Madhusudhan, Thati; Oldenburg, Johannes; Mayer, Günter; Pötzsch, Bernd (April 2009). "An Exosite-Specific ssDNA Aptamer Inhibits the Anticoagulant Functions of Activated Protein C and Enhances Inhibition by Protein C Inhibitor". Chemistry & Biology. 16 (4): 442–451. doi:10.1016/j.chembiol.2009.03.007. PMID 19389630.
- Serine Endopeptidases: Advances in Research and Application: 2011 Edition. ScholarlyEditions. 2012. ISBN 978-1-4649-2658-7.
External links
- Arnaud, E; Lafay, M; Gaussem, P; Picard, V; Jandrot-Perrus, M; Aiach, M; Rendu, F (15 September 1994). "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. 84 (6): 1843–1850. doi:10.1182/blood.V84.6.1843.1843. PMID 8080990.
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