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
Class B1 GPCRs: insights into multireceptor pharmacology for the treatment of metabolic disease
Sign Up to like & getrecommendations! Published in 2024 at "American Journal of Physiology - Endocrinology and Metabolism"
DOI: 10.1152/ajpendo.00371.2023
Abstract: The secretin-like, class B1 subfamily of seven transmembrane-spanning G protein-coupled receptors (GPCRs) consists of 15 members that coordinate important physiological processes. These receptors bind peptide ligands and use a distinct mechanism of activation that is… read more here.
Keywords: receptor; treatment; class gpcrs; pharmacology ... See more keywords
The Role of ICL1 and H8 in Class B1 GPCRs; Implications for Receptor Activation
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Endocrinology"
DOI: 10.3389/fendo.2021.792912
Abstract: The first intracellular loop (ICL1) of G protein-coupled receptors (GPCRs) has received little attention, although there is evidence that, with the 8th helix (H8), it is involved in early conformational changes following receptor activation as… read more here.
Keywords: class gpcrs; receptor activation; icl1;
Molecular Characterization and Expression Analysis of Putative Class C (Glutamate Family) G Protein-Coupled Receptors in Ascidian Styela clava
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DOI: 10.3390/biology11050782
Abstract: Simple Summary Ascidians, known as the closest invertebrate relative to the vertebrate group, have a biphasic life cycle including the larval and sessile adult stages with strong adaptability to diverse environments. The nervous system of… read more here.
Keywords: class gpcrs; class; expression; gpcrs ... See more keywords
Cholesterol in Class C GPCRs: Role, Relevance, and Localization
Sign Up to like & getrecommendations! Published in 2023 at "Membranes"
DOI: 10.3390/membranes13030301
Abstract: G-protein coupled receptors (GPCRs), one of the largest superfamilies of cell-surface receptors, are heptahelical integral membrane proteins that play critical roles in virtually every organ system. G-protein-coupled receptors operate in membranes rich in cholesterol, with… read more here.
Keywords: cholesterol class; class gpcrs; gpcrs role; gpcrs ... See more keywords