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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
MeSH Review

Allosteric Site

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Disease relevance of Allosteric Site


High impact information on Allosteric Site


Chemical compound and disease context of Allosteric Site


Biological context of Allosteric Site


Anatomical context of Allosteric Site


Associations of Allosteric Site with chemical compounds

  • Stuart Forman and Keith Miller describe the physiological, biophysical and molecular biological evidence pointing to the location of a discrete allosteric site on the nicotinic acetylcholine receptor at which local anesthetics act [21].
  • Data are presented which suggest that methoctramine might interact with four acidic residues of the receptor: two residues are buried in the third transmembrane segment whereas the others are located extracellularly on the loop 4-5 which may represent the allosteric site where several antagonists such as gallamine bind [22].
  • In this article, Mark Robertson and colleagues propose that the properties of angiotensin AT1 receptors may be explained by a similar model, but without the need to evoke an allosteric site [23].
  • The activation of these receptors by GABA can be modulated by a range of compounds acting at distinct allosteric sites [24].
  • We conclude that the tyrosine kinase activity of IRs may be altered by peptide interaction at an allosteric site and, moreover, IRs require insulin to assume a conformation permitting phosphorylation by an independent kinase [25].

Gene context of Allosteric Site

  • A conformational switch in the I domain allosteric site (IDAS) and in CD18 regulates LFA-1 affinity for endothelial ligands including intercellular adhesion molecule 1 (ICAM-1) [26].
  • BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice [12].
  • Cooperativity in transcription factor binding to the coactivator CREB-binding protein (CBP). The mixed lineage leukemia protein (MLL) activation domain binds to an allosteric site on the KIX domain [27].
  • Coadministration studies of 873140 with the four other allosteric antagonists yielded data that are consistent with the notion that all five of these antagonists bind to a common allosteric site on the CCR5 receptor [28].
  • It binds to a novel allosteric site that resides within the seven-transmembrane domain of mGlu5 receptors [29].

Analytical, diagnostic and therapeutic context of Allosteric Site


  1. Mutations in the human UDP-N-acetylglucosamine 2-epimerase gene define the disease sialuria and the allosteric site of the enzyme. Seppala, R., Lehto, V.P., Gahl, W.A. Am. J. Hum. Genet. (1999) [Pubmed]
  2. Crystal structures of ligand complexes of P450eryF exhibiting homotropic cooperativity. Cupp-Vickery, J., Anderson, R., Hatziris, Z. Proc. Natl. Acad. Sci. U.S.A. (2000) [Pubmed]
  3. Hybrid tetramers reveal elements of cooperativity in Escherichia coli D-3-phosphoglycerate dehydrogenase. Grant, G.A., Hu, Z., Xu, X.L. J. Biol. Chem. (2003) [Pubmed]
  4. Arginine294 is essential for the inhibition of Anabaena PCC 7120 ADP-glucose pyrophosphorylase by phosphate. Sheng, J., Preiss, J. Biochemistry (1997) [Pubmed]
  5. Affinity labelling of the allosteric site of the L-lactate dehydrogenase of Lactobacillus casei. Hensel, R., Mayr, U., Woenckhaus, C. Eur. J. Biochem. (1983) [Pubmed]
  6. Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. Weitz-Schmidt, G., Welzenbach, K., Brinkmann, V., Kamata, T., Kallen, J., Bruns, C., Cottens, S., Takada, Y., Hommel, U. Nat. Med. (2001) [Pubmed]
  7. Reactions between nitric oxide and haemoglobin under physiological conditions. Gow, A.J., Stamler, J.S. Nature (1998) [Pubmed]
  8. A protein phosphorylation switch at the conserved allosteric site in GP. Lin, K., Rath, V.L., Dai, S.C., Fletterick, R.J., Hwang, P.K. Science (1996) [Pubmed]
  9. Indole-2-carboxylic acid: a competitive antagonist of potentiation by glycine at the NMDA receptor. Huettner, J.E. Science (1989) [Pubmed]
  10. Behavioral differences between subgroups of rats with high and low threshold to clonic convulsions induced by DMCM, a benzodiazepine inverse agonist. Contó, M.B., de Carvalho, J.G., Benedito, M.A. Pharmacol. Biochem. Behav. (2005) [Pubmed]
  11. Primary structure of three peptides at the catalytic and allosteric sites of the fructose-1,6-bisphosphate-activated pyruvate kinase from Escherichia coli. Speranza, M.L., Valentini, G., Iadarola, P., Stoppini, M., Malcovati, M., Ferri, G. Biol. Chem. Hoppe-Seyler (1989) [Pubmed]
  12. BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice. Burke, J.R., Pattoli, M.A., Gregor, K.R., Brassil, P.J., MacMaster, J.F., McIntyre, K.W., Yang, X., Iotzova, V.S., Clarke, W., Strnad, J., Qiu, Y., Zusi, F.C. J. Biol. Chem. (2003) [Pubmed]
  13. A binding study of the interaction of beta-D-fructose 2,6-bisphosphate with phosphofructokinase and fructose-1,6-bisphosphatase. Kitajima, S., Uyeda, K. J. Biol. Chem. (1983) [Pubmed]
  14. Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors. Lazareno, S., Popham, A., Birdsall, N.J. Mol. Pharmacol. (2002) [Pubmed]
  15. Amino acid sequence at the citrate allosteric site of rabbit muscle phosphofructokinase. Kemp, R.G., Fox, R.W., Latshaw, S.P. Biochemistry (1987) [Pubmed]
  16. Regulation of allosteric coupling and function of stably expressed gamma-aminobutyric acid (GABA)A receptors by chronic treatment with GABAA and benzodiazepine agonists. Klein, R.L., Mascia, M.P., Harkness, P.C., Hadingham, K.L., Whiting, P.J., Harris, R.A. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  17. Tetrahydroaminoacridine and other allosteric antagonists of hippocampal M1 muscarine receptors. Potter, L.T., Ferrendelli, C.A., Hanchett, H.E., Hollifield, M.A., Lorenzi, M.V. Mol. Pharmacol. (1989) [Pubmed]
  18. Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5. Maliga, Z., Kapoor, T.M., Mitchison, T.J. Chem. Biol. (2002) [Pubmed]
  19. Interactions of edrophonium with neostigmine in the rat trachea. Shibata, O., Saito, M., Yoshimura, M., Yamaguchi, M., Makita, T., Sumikawa, K. Anesth. Analg. (2003) [Pubmed]
  20. Interaction of glutathione-insulin transhydrogenase (disulfide interchange enzyme) with phospholipids. Varandani, P.T., Nafz, M.A. Biochim. Biophys. Acta (1976) [Pubmed]
  21. Molecular sites of anesthetic action in postsynaptic nicotinic membranes. Forman, S.A., Miller, K.W. Trends Pharmacol. Sci. (1989) [Pubmed]
  22. Polymethylene tetraamines as muscarinic receptor probes. Melchiorre, C., Minarini, A., Angeli, P., Giardinà, D., Gulini, U., Quaglia, W. Trends Pharmacol. Sci. (1989) [Pubmed]
  23. Agonist-antagonist interactions at angiotensin receptors: application of a two-state receptor model. Robertson, M.J., Dougall, I.G., Harper, D., McKechnie, K.C., Leff, P. Trends Pharmacol. Sci. (1994) [Pubmed]
  24. The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit. Wingrove, P.B., Wafford, K.A., Bain, C., Whiting, P.J. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  25. Inhibition of insulin receptor phosphorylation by peptides derived from major histocompatibility complex class I antigens. Hansen, T., Stagsted, J., Pedersen, L., Roth, R.A., Goldstein, A., Olsson, L. Proc. Natl. Acad. Sci. U.S.A. (1989) [Pubmed]
  26. Dynamic regulation of LFA-1 activation and neutrophil arrest on intercellular adhesion molecule 1 (ICAM-1) in shear flow. Lum, A.F., Green, C.E., Lee, G.R., Staunton, D.E., Simon, S.I. J. Biol. Chem. (2002) [Pubmed]
  27. Cooperativity in transcription factor binding to the coactivator CREB-binding protein (CBP). The mixed lineage leukemia protein (MLL) activation domain binds to an allosteric site on the KIX domain. Goto, N.K., Zor, T., Martinez-Yamout, M., Dyson, H.J., Wright, P.E. J. Biol. Chem. (2002) [Pubmed]
  28. The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor. Watson, C., Jenkinson, S., Kazmierski, W., Kenakin, T. Mol. Pharmacol. (2005) [Pubmed]
  29. Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. Malherbe, P., Kratochwil, N., Zenner, M.T., Piussi, J., Diener, C., Kratzeisen, C., Fischer, C., Porter, R.H. Mol. Pharmacol. (2003) [Pubmed]
  30. Functional expression of Arabidopsis thaliana anthranilate synthase subunit I in Escherichia coli. Bernasconi, P., Walters, E.W., Woodworth, A.R., Siehl, D.L., Stone, T.E., Subramanian, M.V. Plant Physiol. (1994) [Pubmed]
  31. Immobilization of nucleoside diphosphatase at its allosteric site using immobilized derivatives of pyridoxal 5'-phosphate. Kawakita, N., Yamazaki, M. Arch. Biochem. Biophys. (1980) [Pubmed]
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