Allosteric Site
Research News and Information

Sunday, November 22, 2009

Multiple protonation states of vesicular acetylcholine transporter detected by binding of [3H]vesamicol.

27 Sep 2009 Vesicular acetylcholine transporter (VAChT) is inhibited by (-)-vesamicol [(-)-trans-2-(4-phenylpiperidino)cyclohexanol], which binds tightly to an allosteric site. The tertiary alkylamine center in (-)-vesamicol is protonated and positively charged ... Read more...

Probing the allosteric modulator binding site of GluR2 with thiazide derivatives.

13 Sep 2009 Ionotropic glutamate receptors mediate the majority of vertebrate excitatory synaptic transmission and are therapeutic targets for cognitive enhancement and treatment of schizophrenia. The binding domains of these tetrameric receptors consist of two ... Read more...

Kinetic and structural investigations of the allosteric site in human epithelial 15-lipoxygenase-2.

13 Sep 2009 Allosteric regulation of human lipoxygenase (hLO) activity has recently been implicated in the cellular biology of prostate cancer. In the current work, we present isotope effect, pH, and substrate inhibitor data of epithelial 15-hLO-2, which probe ... Read more...

Latest indexed articles for 'Allosteric Site'

These are the very latest articles for this heading:

• Multiple protonation states of vesicular acetylcholine transporter detected by binding of [3H]vesamicol. 27 Sep 2009
• Probing the allosteric modulator binding site of GluR2 with thiazide derivatives. 13 Sep 2009
• Kinetic and structural investigations of the allosteric site in human epithelial 15-lipoxygenase-2. 13 Sep 2009
• Identification of domains involved in the allosteric regulation of cytosolic Arabidopsis thaliana NADP-malic enzymes. 31 Aug 2009
• Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1. 28 Aug 2009
• Computation of conformational coupling in allosteric proteins. 26 Aug 2009
• Allosteric collaboration between elongation factor G and the ribosomal L1 stalk directs tRNA movements during translation. 25 Aug 2009
• Allosteric beta-propeller signalling in TolB and its manipulation by translocating colicins. 18 Aug 2009
• 3,5-Diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds. 11 Aug 2009
• Nucleotide regulation of soluble guanylate cyclase substrate specificity. 9 Aug 2009
• A new kind of drug target. 30 Jul 2009
• An allosteric binding site at the human serotonin transporter mediates the inhibition of escitalopram by R-citalopram: kinetic binding studies with the ALI/VFL-SI/TT mutant. 14 Jul 2009
• Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. 7 Jul 2009
• Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. 7 Jul 2009
• Identification of allosteric inhibitors blocking the hepatitis C virus polymerase NS5B in the RNA synthesis initiation step. 5 Jul 2009
• Allosteric site variants of Haemophilus influenzae beta-carbonic anhydrase. 5 Jul 2009
• Dissecting an allosteric switch in caspase-7 using chemical and mutational probes. 4 Jul 2009
• Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineages. 3 Jul 2009
• The search for potent, small molecule NNRTIs: A review. Jul 2009
• Effects of structural analogues of the substrate and allosteric regulator of the human mitochondrial NAD(P)+-dependent malic enzyme. 25 Jun 2009

See a longer list of these articles.

Technical information about 'Allosteric Site'

Definition: A site on an enzyme which upon binding of a modulator, causes the enzyme to undergo a conformational change that may alter its catalytic or binding properties.

Descriptor UI: D000495

Alternative terms: Allosteric Site; Allosteric Sites; Site, Allosteric; Sites, Allosteric;

Related Mesh Headings: Allosteric Regulation;

Allowable Qualifiers: drug effects; genetics; immunology; physiology; radiation effects;

Tree Number: G02.111.570.120.147;

Online Note: search BINDING SITES 1968-74

History Note: 91(75); was see under BINDING SITES 1975-90