Results 41 to 50 of about 41,935 (256)
Pharmacology of Antagonism of GPCR
Biological and Pharmaceutical Bulletin, 2022 Agonists are defined as the ligands that activate intracellular signaling and evoke cellular responses. Synthetic and endogenous agonists should bind specific amino acids to activate G protein-coupled receptor (GPCR). Agonists that induce maximal responses are full agonists. Partial agonists cannot induce full responses unlike full agonists.
Hitoshi, Kurose, Sang Geon, Kim
openaire +2 more sources
BMC Microbiology, 2017 Background G-protein coupled receptors (GPCRs) are the largest family of transmembrane receptors in fungi, where they play important roles in signal transduction. Among them, the Pth11-related GPCRs form a large and divergent protein family, and are only
Xihui Xu +4 more
doaj +1 more source
ALIX binds a YPX(3)L motif of the GPCR PAR1 and mediates ubiquitin-independent ESCRT-III/MVB sorting. [PDF]
, 2012 The sorting of signaling receptors to lysosomes is an essential regulatory process in mammalian cells. During degradation, receptors are modified with ubiquitin and sorted by endosomal sorting complex required for transport (ESCRT)-0, -I, -II, and -III ...
Chen, Buxin +7 more
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Gi- and Gs-coupled GPCRs show different modes of G-protein binding. [PDF]
, 2018 More than two decades ago, the activation mechanism for the membrane-bound photoreceptor and prototypical G protein-coupled receptor (GPCR) rhodopsin was uncovered.
Altenbach, Christian +7 more
core +1 more source
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
Illuminating the life of GPCRs [PDF]
Cell Communication and Signaling, 2009 The investigation of biological systems highly depends on the possibilities that allow scientists to visualize and quantify biomolecules and their related activities in real-time and non-invasively. G-protein coupled receptors represent a family of very dynamic and highly regulated transmembrane proteins that are involved in various important ...
Beck-Sickinger Annette G, Böhme Ilka
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Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment
Molecular Oncology, EarlyView.This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley +1 more source
SLAS DiscoveryBioluminescence- and fluorescence-based resonance energy transfer assays have gained considerable attention in pharmacological research as high-throughput scalable tools applicable to drug discovery. To this end, G protein-coupled receptors represent the
Joanna J. Sajkowska +2 more
doaj +1 more source
Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective [PDF]
, 2019 The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses
Biebermann, Heike +10 more
core +1 more source