Results 1 to 10 of about 6,937,440 (273)
Molecular basis of anaphylatoxin binding, activation, and signaling bias at complement receptors [PDF]
Cell, 2023 Summary The complement system is a critical part of our innate immune response, and the terminal products of this cascade, anaphylatoxins C3a and C5a, exert their physiological and pathophysiological responses primarily via two GPCRs, C3aR and C5aR1 ...
Manisankar Ganguly, Sudha Mishra
exaly +3 more sources
Resonating with the signaling bias of CXCR7. [PDF]
Mol Cell, 2022 Kleist et al. combine NMR spectroscopy and residue contact network analysis to identify a potential allosteric network in CXCR7, a β-arrestin-biased chemokine receptor, which links the extracellular ligand-binding pocket and the intracellular transducer-coupling region through the receptor transmembrane core.
Sarma P, Shukla AK.
europepmc +4 more sources
In Silico Study of Allosteric Communication Networks in GPCR Signaling Bias [PDF]
International Journal of Molecular Sciences, 2022 Signaling bias is a promising characteristic of G protein-coupled receptors (GPCRs) as it provides the opportunity to develop more efficacious and safer drugs.
Mariona Torrens-Fontanals +2 more
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Structural Insights into M1 Muscarinic Acetylcholine Receptor Signaling Bias between Gαq and β-Arrestin through BRET Assays and Molecular Docking [PDF]
International Journal of Molecular Sciences, 2023 The selectivity of drugs for G protein-coupled receptor (GPCR) signaling pathways is crucial for their therapeutic efficacy. Different agonists can cause receptors to recruit effector proteins at varying levels, thus inducing different signaling ...
Jianrong Xu, Yunjin Yao, Yifei Hou
exaly +3 more sources
Human Gain-of-Function MC4R Variants Show Signaling Bias and Protect against Obesity [PDF]
Cell, 2019 Summary The melanocortin 4 receptor (MC4R) is a G protein-coupled receptor whose disruption causes obesity. We functionally characterized 61 MC4R variants identified in 0.5 million people from UK Biobank and examined their associations with body mass ...
Jacek Mokrosiński +2 more
exaly +3 more sources
Ligand bias in receptor tyrosine kinase signaling [PDF]
Journal of Biological Chemistry, 2020 Ligand bias is the ability of ligands to differentially activate certain receptor signaling responses compared with others. It reflects differences in the responses of a receptor to specific ligands and has implications for the development of highly specific therapeutics.
Michael Paul +2 more
exaly +4 more sources
Arrestins: Introducing Signaling Bias Into Multifunctional Proteins. [PDF]
Prog Mol Biol Transl Sci, 2018 Arrestins were discovered as proteins that bind active phosphorylated G protein-coupled receptors (GPCRs) and block their interactions with G proteins, i.e., for their role in homologous desensitization of GPCRs. Mammals express only four arrestin subtypes, two of which are largely restricted to the retina.
Gurevich VV, Chen Q, Gurevich EV.
europepmc +5 more sources
CD40 ligand dictated signaling bias
BLDE University Journal of Health Sciences, 2020 T cells are pivotal for innate and adaptive immune response. On, T cell a co-stimulatory molecule CD40 ligand is present that binds to the CD40 receptor.
Akshata Ganesh Bammigatti
doaj +3 more sources
G Protein and β-Arrestin Signaling Bias at the Ghrelin Receptor [PDF]
Journal of Biological Chemistry, 2014 Background: The G protein coupled receptor GHSR1a mediates feeding and addictive behaviors. Results: Mutagenesis of the second intracellular loop of GHSR1a generates biased receptors, favoring distinct signaling events. Conclusion: Receptor conformations
Marc G Caron +2 more
exaly +3 more sources
Temporal Bias: Time-Encoded Dynamic GPCR Signaling [PDF]
Trends in Pharmacological Sciences, 2017 Evidence suggests that cells can time-encode signals for secure transport and perception of information, and it appears that this dynamic signaling is a common principle of nature to code information in time. G-protein-coupled receptor (GPCR) signaling networks are no exception as their composition and signal transduction appear temporally flexible. In
Evi Prof Kostenis, Manuel Grundmann
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