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Insights That Move the GPCR Field Forward
Read the latest analyses, interviews, and discoveries shaping the GPCR ecosystem — from research breakthroughs to biotech strategy.
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Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its...
September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its N-terminal fragment 1 to...

GPCR News
Aug 31, 20221 min read
Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...
September 2022 Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells: Implications for Targeted...

GPCR News
Aug 31, 20221 min read
Opioid Ligands Addressing Unconventional Binding Sites and More Than One Opioid Receptor Subtype
August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and...

GPCR News
Aug 1, 20221 min read
In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...
August 2022 In vitro assays for the functional characterization of (psychedelic) substances at the serotonin receptor 5-HT2A R...

GPCR News
Aug 1, 20221 min read
Activation of the human chemokine receptor CX3CR1 regulated by cholesterol
August 2022 "As the only member of the CX3C chemokine receptor subfamily, CX3CR1 binds to its sole endogenous ligand CX3CL1, which shows...

GPCR News
Jul 31, 20221 min read
Murine bone marrow macrophages and human monocytes do not express atypical chemokine receptor 1
August 2022 "The atypical chemokine receptor 1 (ACKR1) was discovered on erythrocytes as the Duffy blood group antigen ( Cutbush et al.,...

GPCR News
Jul 31, 20221 min read
Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling
August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, and arrestins - preferentially bind...

GPCR News
Jul 31, 20221 min read
Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis...

GPCR News
Jul 31, 20221 min read
GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin...
August 2022 GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors "Serotonin (or...

GPCR News
Jul 31, 20221 min read
Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic di
August 2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic diabetes insipidus...

GPCR News
Jul 31, 20221 min read
The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends on different molecular...

GPCR News
Jul 31, 20221 min read
G protein-coupled receptor 21 in macrophages: An in vitro study
August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein Coupled Receptors (GPCRs)....

GPCR News
Jul 31, 20221 min read
Fusion protein strategies for cryo-EM study of G protein-coupled receptors
August 2022 "Single particle cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G...

GPCR News
Jul 31, 20221 min read
GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates axonal...
August 2022 GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates axonal regeneration after optic...

GPCR News
Jul 31, 20222 min read
Diversity and specificity in location-based signaling outputs of neuronal GPCRs
August 2022 "The common mechanisms by which members of the G protein-coupled receptor (GPCR) family respond to neurotransmitters in the...

GPCR News
Jul 31, 20221 min read
GRK2 in cardiovascular disease and its potential as a therapeutic target
August 2022 "Cardiovascular diseases (CVDs) represent the leading cause of death globally. Despite major advances in the field of...

GPCR News
Jul 31, 20221 min read
Targeting CXCR1 and CXCR2 receptors in cardiovascular diseases
August 2022 "CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), are expressed in a variety of cells...

GPCR News
Jul 31, 20221 min read
Adenosine receptor signalling in Alzheimer's disease
August 2022 "Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing prevalence presents treatment...

GPCR News
Jul 31, 20221 min read
Structures of β 1-adrenergic receptor in complex with Gs and ligands of different efficacies
August 2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies, and transduce to heterotrimeric...

GPCR News
Jul 31, 20221 min read
Tracking receptor motions at the plasma membrane reveals distinct effects of ligands on CCR5...
August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational and oligomeric states....

GPCR News
Jul 31, 20221 min read
Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
August 2022 "The X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism and anosmia, is due to mutations...

GPCR News
Jul 31, 20221 min read
GPCR kinases generate an APH1A phosphorylation barcode to regulate amyloid-β generation
August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated with the pathophysiology of...

GPCR News
Jul 31, 20221 min read
AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide range of physiological...

GPCR News
Jul 31, 20221 min read
Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
August 2022 "Abstract The β3 -adrenergic receptor (β3 -AR) is found in several tissues such as adipose tissue and urinary bladder. It is...

GPCR News
Jul 31, 20221 min read
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