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]
^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]
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...
Bivalent DTIs (hirudin and analogs) bind both to the active site and exosite 1, while univalent DTIs bind only to the active site. The third class of...
"Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors". Journal of Medicinal Chemistry. 35 (24). American Chemical...
WITH THE EXOSITE INHIBITOR HIRUGEN AND ACTIVE SITE INHIBITOR PHCH2OCO-D-DPA-PRO-BOROMPG 1aix: HUMAN ALPHA-THROMBIN TERNARY COMPLEX WITH EXOSITE INHIBITOR...
domain makes numerous electrostatic interactions with an anion-binding exosite of thrombin, while the last five residues are in a helical loop that forms...
Ser-195. Thrombin also has two exosites (1 and 2). Thrombin is a little different from other serine proteases as exosite 1 is anion-binding and binds to...
2000). "Crystal structure of the human alpha-thrombin-haemadin complex: an exosite II-binding inhibitor". EMBO J. 19 (21): 5650–60. doi:10.1093/emboj/19.21...
Miller, C.J., Lou, H.J., Turk, B.E. Identification of a Substrate-selective Exosite within the Metalloproteinase Anthrax Lethal Factor. J. Biol. Chem. 2017...
TISSUE FACTOR 1dva: Crystal Structure of the Complex Between the Peptide Exosite Inhibitor E-76 and Coagulation Factor VIIA 1f7e: THE FIRST EGF-LIKE DOMAIN...
phospholipids for anticoagulation and to EPCR for cytoprotection. One particular exosite augments protein C's ability to inactivate Factor Va efficiently. Another...
factor Xa independent of the reactive center loop sequence. Evidence for an exosite determinant of factor Xa specificity in heparin-activated antithrombin"...
Thrombin acts on two exosites to fibrinogen. Exosite 1 mediates the binding of thrombin to the Aα- and Bβ-chains, and exosite 2 causes an interaction...
aptamers. Anti-thrombin aptamers – Oligonucleotides which recognize the exosites of human thrombin Deoxyribozyme – DNA oligonucleotides that can perform...
specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Thrombin is a serine proteinase...
spectrometry at nearly single amino acid residue resolution reveals novel exosites on ADAMTS13 critical for substrate recognition and mechanism of autoimmune...
protease-substrate discovery. As protease exosites play roles in protein-protein recognition and interaction, biologists have used exosites as tools to screen for protease...
both of these coagulation proteases also contain binding sites (called exosites) for heparin. Heparin, therefore, also acts as a template for binding of...
Protein L4-100K from adenoviruses can also inhibit granzyme B by binding at exosites and specific binding pockets. L4-100K is an assembly protein that can transport...
modifications) on its surface region, that has been termed the "anion binding exosite." This site consists of an area of excess positive charge, which has been...
sequences protrude from the globular structures of the proteases. Since this exosite was shown to be involved in the platelet aggregating activity of thrombin...
reaction Anti-thrombin aptamers – Oligonucleotides which recognize the exosites of human thrombin Bacterial one-hybrid system – Method for identifying...
for LABAs. The first explained the long action in terms of a putative “exosite” or “exoceptor” distinct from the β2-adrenoreceptor that long aliphatic...
1997). "Structure of the thrombin complex with triabin, a lipocalin-like exosite-binding inhibitor derived from a triatomine bug". Proceedings of the National...
Development of Idraparinux was discontinued. Krishnaswamy S (January 2005). "Exosite-driven substrate specificity and function in coagulation". J. Thromb. Haemost...
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