Biology:Exosite

From HandWiki

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

  1. 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. 
  2. 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). http://www.blackwellpublishing.com/isth2003/abstract.asp?id=9231. 
  3. Müller, Jens; Isermann, Berend; Dücker, Christina; Salehi, Mohammad; Meyer, Moritz; Friedrich, Max; Madhusudhan, Thati; Oldenburg, Johannes et al. (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. 
  4. 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.