Results 41 to 50 of about 142,523 (351)
Below the Surface: IGF-1R Therapeutic Targeting and Its Endocytic Journey
Cells, 2019 Ligand-activated plasma membrane receptors follow pathways of endocytosis through the endosomal sorting apparatus. Receptors cluster in clathrin-coated pits that bud inwards and enter the cell as clathrin-coated vesicles.
Caitrin Crudden +7 more
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Agonist and antagonist TRUPATH assays for G protein-coupled receptors
STAR Protocols, 2022 Summary: TRUPATH is a bioluminescence resonance energy transfer-based platform for quantifying G protein-coupled receptor activity via dissociation of heterotrimeric G protein biosensors.
Jeffrey F. DiBerto +3 more
doaj +1 more source
Functional classification of G-Protein coupled receptors, based on their specific ligand coupling patterns [PDF]
, 2006 Functional identification of G-Protein Coupled Receptors (GPCRs) is one of the current focus areas of pharmaceutical research. Although thousands of GPCR sequences are known, many of them re- main as orphan sequences (the activating ligand is unknown ...
Bakır, Burcu, Sezerman, Uğur
core +1 more source
Cryo-EM structure of an activated GPCR–G protein complex in lipid nanodiscs
Nature Structural & Molecular Biology, 2020 G-protein-coupled receptors (GPCRs) are the largest superfamily of transmembrane proteins and the targets of over 30% of currently marketed pharmaceuticals.
Meng Zhang +14 more
semanticscholar +1 more source
Vascular Biology, 2019 The discovery and extension of G-protein-coupled receptor (GPCR) transactivation-dependent signalling has enormously broadened the GPCR signalling paradigm.
Raafat Mohamed +9 more
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CHIMIA, 2021 Nervous system disorders affect millions of people around the world, through a very broad range of diseases. Here we describe our contribution to find a treatment for patients suffering from three of those diseases.
Hasane Ratni
doaj +1 more source
Odorant receptors can mediate axonal identity and gene choice via cAMP-independent mechanisms [PDF]
Open Biology, 2016 Odorant receptors (ORs) control several aspects of cell fate in olfactory sensory neurons (OSNs), including singular gene choice and axonal identity.
Kiavash Movahedi +2 more
doaj +1 more source
Ligands can differentially and temporally modulate GPCR interaction with 14-3-3 isoforms
Current Research in Pharmacology and Drug Discovery, 2022 GPCR signaling and function depend on their associated proteins and subcellular locations. Besides G-proteins and β-arrestins, 14-3-3 proteins participate in GPCR trafficking and signaling, and they connect a large number of diverse proteins to form ...
Haifeng Eishingdrelo +4 more
doaj +1 more source
Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]
, 2010 To address the problem of specificity in G-protein coupled receptor (GPCR) drug discovery, there has been tremendous recent interest in allosteric drugs that bind at sites topographically distinct from the orthosteric site. Unfortunately, structure-based
Ivetac, Anthony, McCammon, J Andrew
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The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]
, 2013 G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D. +2 more
core +1 more source