Allosteric modulation of α4β2* nicotinic acetylcholine receptors: Desformylflustrabromine potentiates antiallodynic response of nicotine in a mouse model of neuropathic pain
Sign Up to like & getrecommendations! Published in 2018 at "European Journal of Pain"
DOI: 10.1002/ejp.1092
Abstract: Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand‐gated ion channels. The α4β2 subtype of nAChRs plays an important role in the mediation of pain and several nicotine‐evoked responses. Agonists and partial agonists of α4β2 nAChRs show… read more here.
Keywords: nicotine; acetylcholine receptors; nicotinic acetylcholine; allosteric modulation ... See more keywords
Allosteric modulation of dopamine D2L receptor in complex with Gi1 and Gi2 proteins: the effect of subtle structural and stereochemical ligand modifications
Sign Up to like & getrecommendations! Published in 2022 at "Pharmacological Reports"
DOI: 10.1007/s43440-021-00352-x
Abstract: Background Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays one of the hot topics in drug discovery. In particular, allosteric modulators of D2 receptor have been proposed as potential modern therapeutics to treat schizophrenia… read more here.
Keywords: modulator; d2l receptor; allosteric modulation; receptor ... See more keywords
Allosteric Modulation of Binding Specificity by Alternative Packing of Protein Cores.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2018.11.018
Abstract: Hydrophobic cores are often viewed as tightly packed and rigid, but they do show some plasticity and could thus be attractive targets for protein design. Here we explored the role of different functional pressures on… read more here.
Keywords: modulation binding; specificity; packing; allosteric modulation ... See more keywords
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00875
Abstract: G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR superfamily is highly represented, and continued drug discovery for this… read more here.
Keywords: class; chemistry; allosteric modulation; class gpcrs ... See more keywords
Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.6b00310
Abstract: The cannabinoid 1 receptor (CB1R) is one of the most widely expressed metabotropic G protein-coupled receptors in brain, and its participation in various (patho)physiological processes has made CB1R activation a viable therapeutic modality. Adverse psychotropic… read more here.
Keywords: cb1r; gat211; cannabinoid receptor; pharmacology ... See more keywords
Allosteric Modulation of Ionotropic Glutamate Receptors Special Issue.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00174
Abstract: Call for papers! ACS Medicinal Chemistry Letters is now accepting manuscript submissions for a special issue entitled "Allosteric Modulation of Ionotropic Glutamate Receptors". This special issue is a cross-thematic issue with Journal of Medicinal Chemistry… read more here.
Keywords: issue; medicinal chemistry; chemistry; modulation ionotropic ... See more keywords
Structural bases of TRP channel TRPV6 allosteric modulation by 2-APB
Sign Up to like & getrecommendations! Published in 2018 at "Nature Communications"
DOI: 10.1038/s41467-018-04828-y
Abstract: Transient receptor potential (TRP) channels are involved in various physiological processes, including sensory transduction. The TRP channel TRPV6 mediates calcium uptake in epithelia and its expression is dramatically increased in numerous types of cancer. TRPV6… read more here.
Keywords: trp channels; trp channel; trpv6; allosteric modulation ... See more keywords
Allosteric modulation of ghrelin receptor signaling by lipids
Sign Up to like & getrecommendations! Published in 2021 at "Nature Communications"
DOI: 10.1038/s41467-021-23756-y
Abstract: The membrane is an integral component of the G protein-coupled receptor signaling machinery. Here we demonstrate that lipids regulate the signaling efficacy and selectivity of the ghrelin receptor GHSR through specific interactions and bulk effects.… read more here.
Keywords: ghrelin receptor; modulation ghrelin; receptor signaling; receptor ... See more keywords
M1-selective muscarinic allosteric modulation enhances cognitive flexibility and effective salience in nonhuman primates
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1101/2022.10.05.511029
Abstract: Acetylcholine (ACh) in cortical neural circuits mediates how selective attention is sustained in the presence of distractors and how flexible cognition adjusts to changing task demands. The cognitive domains of attention and cognitive flexibility might… read more here.
Keywords: cognitive flexibility; flexibility; nonhuman primates; attention ... See more keywords
Allosteric modulation of G protein-coupled receptor signaling
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2023.1137604
Abstract: G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins, regulate a wide array of physiological processes in response to extracellular signals. Although these receptors have proven to be the most successful class of drug… read more here.
Keywords: coupled receptor; modulation protein; allosteric modulators; allosteric modulation ... See more keywords
Modulatory Actions of the Glycine Receptor β Subunit on the Positive Allosteric Modulation of Ethanol in α2 Containing Receptors
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Molecular Neuroscience"
DOI: 10.3389/fnmol.2021.763868
Abstract: Alpha1-containing glycine receptors (GlyRs) are major mediators of synaptic inhibition in the spinal cord and brain stem. Recent studies reported the presence of α2-containing GlyRs in other brain regions, such as nucleus accumbens and cerebral… read more here.
Keywords: actions glycine; modulatory actions; modulation; glycine receptor ... See more keywords