Molecular mechanism of Gαi activation by non-GPCR proteins with a Gα-Binding and Activating motif [PDF]
, 2017 Heterotrimeric G proteins are quintessential signalling switches activated by nucleotide exchange on Gα. Although activation is predominantly carried out by G-protein-coupled receptors (GPCRs), non-receptor guanine-nucleotide exchange factors (GEFs) have
Baillie, George S. +14 more
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G-Protein Coupled Receptors Targeted by Analgesic Venom Peptides
Toxins, 2017 Chronic pain is a complex and debilitating condition associated with a large personal and socioeconomic burden. Current pharmacological approaches to treating chronic pain such as opioids, antidepressants and anticonvulsants exhibit limited efficacy in ...
James T. Daniel, Richard J. Clark
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Fusion protein strategies for cryo-EM study of G protein-coupled receptors
Nature Communications, 2022 Here, Zhang et al. explore fusion protein strategies to facilitate cryo-EM structural studies of GPCRs alone- without signal transducers- in ligand bound or unliganded form.
Kaihua Zhang +4 more
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Functional selectivity of GPCR-directed drug action through location bias. [PDF]
, 2017 G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco +6 more
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Stabilization of G protein-coupled receptors by point mutations
Frontiers in Pharmacology, 2015 G protein-coupled receptors (GPCRs) are flexible integral membrane proteins involved in transmembrane signaling. Their involvement in many physiological processes makes them interesting targets for drug development.
Franziska eHeydenreich +7 more
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Allostery of atypical modulators at oligomeric G protein-coupled receptors
Scientific Reports, 2021 Many G protein-coupled receptors (GPCRs) are therapeutic targets, with most drugs acting at the orthosteric site. Some GPCRs also possess allosteric sites, which have become a focus of drug discovery.
Rabindra V. Shivnaraine +7 more
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G protein–coupled receptors: from radioligand binding to cellular signaling [PDF]
The Journal of Clinical InvestigationHoward A. Rockman, Robert J. Lefkowitz
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Crystallization of G Protein-Coupled Receptors [PDF]
, 2013 Oligomerization is one of several mechanisms that can regulate the activity of G protein-coupled receptors (GPCRs), but little is known about the structure of GPCR oligomers. Crystallography and NMR are the only methods able to reveal the details of receptor-receptor interactions at an atomic level, and several GPCR homodimers already have been ...
Pius S. Padayatti +2 more
openaire +3 more sources
Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
, 2019 In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie +3 more
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G protein-coupled receptors: the evolution of structural insight
AIMS Biophysics, 2017 G protein-coupled receptors (GPCR) comprise a diverse superfamily of over 800 proteins that have gained relevance as biological targets for pharmaceutical drug design.
Samantha B. Gacasan +2 more
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