Die Funktion der Helix 8 für die Regulation des Bradykinin B2 Rezeptors [PDF]
, 2012 Upon activation the human bradykinin B2 receptor (B2R) acts as guanine nucleotide exchange factor for the G proteins Gq/11 and Gi. Thereafter, it gets phosphorylated by G protein-coupled receptor kinases (GRKs) and recruits beta-arrestins, which block ...
Feierler, Jens
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Regulation of metabotropic glutamate receptor subtype 7a by PDZ-domain protein PICK1 [PDF]
, 2007 Metabotropic glutamate receptor subtype 7 (mGluR7) belongs to the family of G-protein coupled receptors. mGluR7 is widely distributed in the brain and primarily localized at presynaptic terminals, where it is thought to regulate neurotransmitter release ...
Zhang, C., Zhang, Chuansheng
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Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators
Frontiers in PharmacologyTargeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds).
Brent Van Bosstraeten +8 more
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Membrane cholesterol access into a G-protein-coupled receptor
Nature Communications, 2017 G-protein-coupled receptors trigger several signalling pathways and their activity was proposed to be allosteric modulated by cholesterol. Here the authors use molecular dynamics simulations and ligand binding assays to show that membrane cholesterol can
Ramon Guixà-González +10 more
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Receptor for activated C kinase-1 facilitates protein kinase C-dependent phosphorylation and functional modulation of GABA(A) receptors with the activation of G-protein-coupled receptors [PDF]
, 2002 GABA(A) receptors are the principal sites of fast synaptic inhibition in the brain. These receptors are hetero-pentamers that can be assembled from a number of subunit classes: alpha(1-6), beta(1-3), gamma(1-3), delta(1), epsilon, theta, and pi, but the ...
Trevor G Smart +7 more
core
Brazilian Journal of Medical and Biological Research, 1998 G protein-coupled receptor (GPCR) activation is followed rapidly by adaptive changes that serve to diminish the responsiveness of a cell to further stimulation.
S.S.G. Ferguson
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Mutational and computational characterization of transmembrane domains in the fungal G protein-coupled pheromone receptors STE2 and Mam2 [PDF]
G protein-coupled receptors (GPCRs) comprise the largest family of cell-surface receptors involved in sensing a multitude of ligands and are consequently attractive pharmacological targets.
Nilsson Lock, Gun Antonia Evelina
core
Inferring the lifetime of endosomal protein complexes by fluorescence recovery after photobleaching [PDF]
, 2008 Cellular signal transduction is dynamic, with signaling proteins continually associating and dissociating into and from protein complexes. Here we present a fluorescence recovery after photobleaching technique to determine the lifetime of protein ...
Gousseva, Veronika +5 more
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Novel role for proteinase-activated receptor 2 (PAR2) in membrane trafficking of proteinase-activated receptor 4 (PAR4) [PDF]
, 2012 Proteinase-activated receptors 4 (PAR4) is a class A G protein-coupled receptor (GPCR) recognized through the ability of serine proteases such as thrombin and trypsin to mediate receptor activation.
Robben, Joris +9 more
core +2 more sources
Mechanistic insights into G-protein coupling with an agonist-bound G-protein-coupled receptor [PDF]
G-protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by promoting guanine nucleotide exchange. Here, we investigate the coupling of G proteins with GPCRs and describe the events that ultimately lead to the ejection of GDP from its ...
Mathiesen, Jesper M. +18 more
core +1 more source