Exosite
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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]
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.[page needed]
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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