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β-Arrestin-independent endosomal cAMP signaling by a polypeptide hormone GPCR
Many G protein-coupled receptors (GPCRs) initiate a second phase of stimulatory heterotrimeric G protein (G s )-coupled cAMP signaling after...
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Cardiac contraction and relaxation are regulated by distinct subcellular cAMP pools
Cells interpret a variety of signals through G-protein-coupled receptors (GPCRs) and stimulate the generation of second messengers such as cyclic...
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The role of G protein conformation in receptor–G protein selectivity
G protein-coupled receptors (GPCRs) selectively activate at least one of the four families of heterotrimeric G proteins, but the mechanism of...
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Mass spectrometry captures biased signalling and allosteric modulation of a G-protein-coupled receptor
G-protein-coupled receptors signal through cognate G proteins. Despite the widespread importance of these receptors, their regulatory mechanisms for...
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The dynamics of agonist-β2-adrenergic receptor activation induced by binding of GDP-bound Gs protein
There is considerable uncertainty about the mechanism by which the β 2 -adrenergic receptor (β 2 AR) is activated. Here we use molecular metadynamics...
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Profiling the proximal proteome of the activated μ-opioid receptor
The μ-opioid receptor (μOR) represents an important target of therapeutic and abused drugs. So far, most understanding of μOR activity has focused on...
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Selective G protein signaling driven by substance P–neurokinin receptor dynamics
The neuropeptide substance P (SP) is important in pain and inflammation. SP activates the neurokinin-1 receptor (NK1R) to signal via G q and G s ...
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Islet MC4R Regulates PC1/3 to Improve Insulin Secretion in T2DM Mice via the cAMP and β-arrestin-1 Pathways
Melanocortin-4 receptor (MC4R) plays an important role in energy balance regulation and insulin secretion. It has been demonstrated that in the...
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Adenosine A2A Receptor Antagonists: Chemistry, SARs, and Therapeutic Potential
Many physiological processes are modulated by the naturally occurred nucleoside adenosine after interaction with four G-protein-coupled receptor...
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Roles of lysophosphatidic acid (LPA) receptor-mediated signaling in cancer cell biology
Lysophosphatidic acid (LPA) is a simple lipid which is endogenously synthesized from lysophosphatidylcholine (LPC) by autotaxin (ATX). LPA mediates a...
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G Protein-Coupled Receptors
G protein-coupled receptors (GPCRs) are important drug targets for FDA-approved drugs. Understanding the biology, structure, and pharmacology of...
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Identification and mechanism of G protein-biased ligands for chemokine receptor CCR1
Biased signaling of G protein-coupled receptors describes an ability of different ligands that preferentially activate an alternative downstream...
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Spatial decoding of endosomal cAMP signals by a metastable cytoplasmic PKA network
G-protein-coupled receptor-regulated cAMP production from endosomes can specify signaling to the nucleus by moving the source of cAMP without...
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Update and Potential Opportunities in CBP [Cyclic Adenosine Monophosphate (cAMP) Response Element-Binding Protein (CREB)-Binding Protein] Research Using Computational Techniques
CBP [cyclic adenosine monophosphate (cAMP) response element-binding protein (CREB)-binding protein] is one of the most researched proteins for its...
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Structural insight into selectivity of amylin and calcitonin receptor agonists
Amylin receptors (AMYRs), heterodimers of the calcitonin receptor (CTR) and one of three receptor activity-modifying proteins, are promising obesity...
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Identification of G protein-coupled receptor 55 (GPR55) as a target of curcumin
The identification of molecular targets of bioactive food components is important to understand the mechanistic aspect of their physiological...
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Chemometric Study, Homology Modeling of G Protein-Coupled Bile Acids Receptor (GPBAR_HUMAN) of Type-2 Diabetes Mellitus, Virtual Screening Evaluation, Drug-Likeness and ADME Prediction for Newly Designed Compounds
Chemometric validation of the reported experimental activities of nicotinamide and carboxamide analogues against diabetes were determined via ...
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The relaxin receptor RXFP1 signals through a mechanism of autoinhibition
The relaxin family peptide receptor 1 (RXFP1) is the receptor for relaxin-2, an important regulator of reproductive and cardiovascular physiology....
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Molecular basis for the selective G protein signaling of somatostatin receptors
G protein-coupled receptors (GPCRs) modulate every aspect of physiological functions mainly through activating heterotrimeric G proteins. A majority...
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Endosome positioning coordinates spatially selective GPCR signaling
G-protein-coupled receptors (GPCRs) can initiate unique functional responses depending on the subcellular site of activation. Efforts to uncover the...
