Negative Allosteric Modulation of Agonist-Induced M<sub>2</sub> Muscarinic Receptor/β-Arrestin Interaction by Serum Autoantibodies from Patients with Chronic Chagas Disease. [PDF]
Carrera Páez LC +7 more
europepmc +1 more source
Conformational diversity in class C GPCR positive allosteric modulation. [PDF]
Cannone G +11 more
europepmc +1 more source
Preferential allosteric modulation of Otop1 channels by small molecule compounds. [PDF]
Kong X +10 more
europepmc +1 more source
Correction for Mittal et al., Mechanisms underlying allosteric modulation of antiseizure medication binding to synaptic vesicle protein 2A (SV2A). [PDF]
europepmc +1 more source
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Olfaction: Allosteric modulation
Current Biology, 2023New research indicates that the odor-evoked responses of human olfactory receptors can be enhanced via the non-competitive binding of an allosteric modulator. This modulatory mechanism adds an additional layer of complexity to the peripheral encoding of odors.
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Allosteric modulation of caspases
Pharmacology & Therapeutics, 2011Caspases are proteolytic enzymes mainly involved in the induction and execution phases of apoptosis. This type of programmed cell death is an essential regulatory process required to maintain the integrity and homeostasis of multicellular organisms. Inappropriate apoptosis is attributed a key role in many human diseases, including neurodegenerative ...
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Allosteric modulation of G-protein coupled receptors
The superfamily of G-protein coupled receptors (GPCRs) has more than 1000 members and is the largest family of proteins in the body. GPCRs mediate signalling of stimuli as diverse as light, ions, small molecules, peptides and proteins and are the targets
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Allosteric modulation of nicotinic acetylcholine receptors
Allosteric modulation refers to the concept that proteins could exist in multiple conformational states and that binding of allosteric ligands alters the energy barriers or "isomerization coefficients" between various states.
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This article discusses a model to describe the effects of molecules that bind to a site on the receptor separate from that of the endogenous agonist to actively produce receptor signals (direct agonism). In addition, these molecules also modify the biological responses of the endogenous agonist (either potentiation or antagonism).
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Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator
Biochemistry, 2023The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activity, induces opioid-independent analgesia, and regulates food intake.
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