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- Allosteric_modulator abstract "In biochemistry and pharmacology, an allosteric modulator (allo- from the Greek meaning \"other\") is a substance which indirectly influences (modulates) the effects of an agonist or inverse agonist at a target protein, for example a receptor. Allosteric modulators bind to a site distinct from that of the orthosteric agonist binding site. Usually they induce a conformational change within the protein structure. A positive allosteric modulator (PAM) or allosteric enhancer induces an amplification of the orthosteric agonist's effect, either by enhancing the binding affinity or the functional efficacy of the orthosteric agonist for the target protein. A negative modulator (NAM) reduces the effects of the orthosteric ligand, but is inactive in the absence of the orthosteric ligand. Substances that occupy the allosteric binding site and are functionally neutral are called silent allosteric modulators (SAMs). Classic benzodiazepines are well-known PAMs.The modulatory activity can be first-order or second-order (or both). Second-order modulators alter the modulatory activity of first-order modulators. (−)‐Epigallocatechin‐3‐gallate is one such example of a second-order modulator at GABAA receptors.Allosteric agonists are to be distinguished from pure allosteric modulators. They are defined as ligands able to directly activate a receptor by binding to a receptor site distinct from the primary (orthosteric) site, the allosteric site. They are able to bind the target protein and exert their effect in the absence of an orthosteric ligand, whereas the presence of an orthosteric ligand is typically required to observe the indirect effects of pure allosteric modulators.Ago-allosteric modulators are both allosteric agonists and allosteric modulators. An ago-allosteric modulator acts as an agonist and an enhancer for endogenous agonists in increasing agonist potency (the dose range over which a response is produced) and providing \"superagonism\". Superagonism results when the efficacy is greater than 100 percent. Ago-allosteric modulators can be neutral, negative, or positive. Neutral ago-allosteric modulators increase efficacy, but have no effect on potency. A negative ago-allosteric modulator has a negative effect on the potency but a positive effect on the efficacy of an agonist. A positive ago-allosteric modulator increases both efficacy and potency.".
- Allosteric_modulator wikiPageID "23214707".
- Allosteric_modulator wikiPageLength "4405".
- Allosteric_modulator wikiPageOutDegree "16".
- Allosteric_modulator wikiPageRevisionID "657169077".
- Allosteric_modulator wikiPageWikiLink Agonist.
- Allosteric_modulator wikiPageWikiLink Allosteric_regulation.
- Allosteric_modulator wikiPageWikiLink Benzodiazepine.
- Allosteric_modulator wikiPageWikiLink Binding_site.
- Allosteric_modulator wikiPageWikiLink Category:Neuropharmacology.
- Allosteric_modulator wikiPageWikiLink Chemical_substance.
- Allosteric_modulator wikiPageWikiLink Dissociation_constant.
- Allosteric_modulator wikiPageWikiLink Epigallocatechin_gallate.
- Allosteric_modulator wikiPageWikiLink Intrinsic_activity.
- Allosteric_modulator wikiPageWikiLink Inverse_agonist.
- Allosteric_modulator wikiPageWikiLink Ligand_(biochemistry).
- Allosteric_modulator wikiPageWikiLink Protein_structure.
- Allosteric_modulator wikiPageWikiLink Receptor_(biochemistry).
- Allosteric_modulator wikiPageWikiLink Second-order.
- Allosteric_modulator wikiPageWikiLink Target_protein.
- Allosteric_modulator wikiPageWikiLinkText "Allosteric agonists".
- Allosteric_modulator wikiPageWikiLinkText "Allosteric modulator".
- Allosteric_modulator wikiPageWikiLinkText "First order allosteric modulators".
- Allosteric_modulator wikiPageWikiLinkText "NAM".
- Allosteric_modulator wikiPageWikiLinkText "PAM".
- Allosteric_modulator wikiPageWikiLinkText "Second order modulators".
- Allosteric_modulator wikiPageWikiLinkText "allosteric agonist".
- Allosteric_modulator wikiPageWikiLinkText "allosteric antagonist".
- Allosteric_modulator wikiPageWikiLinkText "allosteric binding sites".
- Allosteric_modulator wikiPageWikiLinkText "allosteric modulator".
- Allosteric_modulator wikiPageWikiLinkText "allosteric".
- Allosteric_modulator wikiPageWikiLinkText "modulator".
- Allosteric_modulator wikiPageWikiLinkText "modulatory".
- Allosteric_modulator wikiPageWikiLinkText "positive allosteric agonism".
- Allosteric_modulator wikiPageWikiLinkText "positive allosteric modulator".
- Allosteric_modulator wikiPageWikiLinkText "positive allosteric modulators".
- Allosteric_modulator wikiPageWikiLinkText "positive modulatory".
- Allosteric_modulator wikiPageUsesTemplate Template:Cite_journal.
- Allosteric_modulator wikiPageUsesTemplate Template:Neuromodulation.
- Allosteric_modulator wikiPageUsesTemplate Template:Pharmacology-stub.
- Allosteric_modulator wikiPageUsesTemplate Template:Reflist.
- Allosteric_modulator subject Category:Neuropharmacology.
- Allosteric_modulator hypernym Substance.
- Allosteric_modulator type ChemicalCompound.
- Allosteric_modulator comment "In biochemistry and pharmacology, an allosteric modulator (allo- from the Greek meaning \"other\") is a substance which indirectly influences (modulates) the effects of an agonist or inverse agonist at a target protein, for example a receptor. Allosteric modulators bind to a site distinct from that of the orthosteric agonist binding site. Usually they induce a conformational change within the protein structure.".
- Allosteric_modulator label "Allosteric modulator".
- Allosteric_modulator sameAs Q2649417.
- Allosteric_modulator sameAs Allosterischer_Modulator.
- Allosteric_modulator sameAs Modulador_alostérico.
- Allosteric_modulator sameAs Modulador_alostérico.
- Allosteric_modulator sameAs m.064kshx.
- Allosteric_modulator sameAs Pozitivni_alosterni_modulator.
- Allosteric_modulator sameAs Pozitivni_alosterni_modulator.
- Allosteric_modulator sameAs Q2649417.
- Allosteric_modulator wasDerivedFrom Allosteric_modulator?oldid=657169077.
- Allosteric_modulator isPrimaryTopicOf Allosteric_modulator.