syndrome characterized by the reduction in cardiac function and still remains the disease with the highest mortality which block the effects of angiotensin II (AngII) and aldosterone on the failing heart, are part of the mainstay The adrenal gland plays an important role in the modulation of cardiac neurohormonal stress because it aldosterone, of all epinephrine, and of a significant amount of norepinephrine reaching the failing myocardium Read more at the source #DrGPCR #GPCR #IndustryNews

protein standards for quantitative Western blot analysis of cannabinoid CB1 receptor density in cell membranes : an alternative to radioligand binding methods "Background: Replacement of radioligand binding assays highly soluble and stable recombinant protein constructs GST-CB1414-472 and GST-CB1414-442 containing much different antibodies, all raised against a peptide comprising the C-terminal residues 443-473 of the mouse Read more at the source #DrGPCR #GPCR #IndustryNews

receptors (GPCRs) in the cardiovascular system is well understood in cardiomyocytes and vascular smooth muscle In VSMCs, stimulation of GPCRs also modulates contractile and cell growth phenotypes. machinery are localized in these cells with an emphasis on nuclear membrane-localized receptors. Finally, we explore what such connections between the cell surface and nuclear GPCR signaling might mean Read more at the source #DrGPCR #GPCR #IndustryNews

Neuropeptides and their receptors have been documented in many hemipteran insects, but the differences This research provides more knowledge on neuropeptide systems and sets the groundwork for the creation of novel D. vitifoliae management strategies that specifically target these signaling pathways." Read more at the source #DrGPCR #GPCR #IndustryNews

receptors shown to transactivate other receptors: noticeably, these interactions are not limited to members In this review, we will focus on the evidence for PAR interactions with members of their own family, the physiological and pathological relevance of these interactions, since this additional level of molecular cross-talk between receptors and signaling pathways is only beginning to be explored and represents a novel mechanism Read more at the source #DrGPCR #GPCR #IndustryNews

Here, we characterize divergent signaling signatures in mouse astrocytes of the PFC and primary sensory Instead, fast calcium signals in PFC astrocytes are time locked to dopamine release and are mediated Read more at the source #DrGPCR #GPCR #IndustryNews

The recently determined structures of B2R have provided molecular insights into the functions and regulation Read more at the source #DrGPCR #GPCR #IndustryNews

However, the molecular mechanisms engaged downstream of GPR183 in the spinal cord are not known. protein kinase (MAPK) and nuclear factor κB (NF-κB). hypersensitivity through MAPK and NF-κB activation. SIGNIFICANCE STATEMENT: Using a multi-disciplinary approach, we have characterized the molecular mechanisms Read more at the source #DrGPCR #GPCR #IndustryNews

Most acquired genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing Despite a better understanding of the disease, the current mainstay of treatment cannot modify pathogenesis or effectively address the associated cognitive and memory deficits. improving cognition and memory. Read more at the source #DrGPCR #GPCR #IndustryNews

protein-coupled receptors in placental development and preeclampsia "Preeclampsia, a clinical syndrome mainly characterized by hypertension and proteinuria, with a worldwide incidence of 3–8% and high maternal mortality, is a risk factor highly associated with maternal and offspring cardiovascular disease. Obesity, immunological diseases and endocrine metabolic diseases are high-risk factors for the development Read more at the source #DrGPCR #GPCR #IndustryNews

To interrogate the molecular mechanisms underlying this interaction, we conducted a host-directed CRISPR-Cas9 screen and identified 361 genes that modify macrophage susceptibility to Hc infection, greatly expanding , mitochondrial respiration genes, solute transporters, and the ER membrane complex (EMC). and uncover a novel and specific role for C3aR in macrophage recognition of fungi." Read more at the source #DrGPCR #GPCR #IndustryNews

Recent evidence indicates that GPR15 may be associated with modulation of the chronic inflammatory response The expression of GPR15 and c10orf99/gpr15l mRNA was analyzed by RT-qPCR. Statistical analysis included Kruskal-Wallis test, T-test, or Mann-Whitney U test, according to data A higher expression in the mRNA for GPR15 was identified in early RA subjects. Read more at the source #DrGPCR #GPCR #IndustryNews

emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate multiple characteristics with the 2 cases we previously reported as follows: (a) elderly (74-87 years at diagnosis), (b) male Our observations with these prominent commonalities may provide new insights into the phenotype and characteristics of AHH and the mechanisms by which the biased agonism of GPCRs operate." Read more at the source #DrGPCR #GPCR #IndustryNews

One potent form of inhibition is mediated by the activation of two inhibitory G protein-coupled receptors The heterologous facilitation was modelled based on the known cooperative interaction between the G protein KEY POINTS: Inhibitory D2 and GABAB receptors modulate dopamine neuron activity through shared G protein-coupled Results demonstrate that the activity of either G protein-coupled receptor system must be considered Read more at the source #DrGPCR #GPCR #IndustryNews

With continued study of their function and mechanism of action, there is a greater understanding of how effector molecules interact with a receptor to initiate downstream effector signaling. pathways, dynamic structures, and physiological relevance in the cardiovascular system of the three most that mediate intracellular signaling and function." Read more at the source #DrGPCR #GPCR #IndustryNews

Our previous work demonstrated that GPR3-mediated β-arrestin signaling modulates amyloid-β (Aβ) generation Here, we generated a G protein-biased GPR3 mouse model to investigate the physiological and pathophysiological In contrast to Gpr3-deficient mice, G protein-biased GPR3 mice do not display elevated anxiety levels model. AD mice.

GPCR Virtual Cafe with Matthew Eddy scheduled for tomorrow (Sep 29th, 2022) due to Hurricane Ian that

receptor an intriguing target for treating schizophrenia, a disease where novel interventions that move The development of new CB2-related pharmacological and genetic tools, including the first small molecule positive allosteric modulator of CB2 receptors, has greatly advanced our understanding of this receptor While more work is needed to further elucidate the translational value of selectively targeting CB2 receptors Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "GPCRs modulate a plethora of physiological processes and mediate the effects of one-third Ligands eliciting biased signalling may constitute better drugs with higher efficacy and fewer adverse However, ligand bias is very complex, making reproducibility and description challenging. Scientific insight, biosensors, and analytical methods are still evolving and should benefit from and Read more at the source #DrGPCR #GPCR #IndustryNews

Extensive efforts of structural biology have been made on the study of GPCRs. Recently, AlphaFold2 has been developed to predict structure models of many functionally important proteins including all members of the GPCR family. However, the predicted models and experimental structures were different in many aspects including the Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing prevalence Despite a better understanding of the disease, the current mainstay of treatment cannot modify pathogenesis or effectively address the associated cognitive and memory deficits. improving cognition and memory. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), are expressed in a variety of cells including, leukocytes, fibroblasts, endothelial cells, and smooth muscle Numerous intracellular mediators are activated by these G protein-coupled receptors based on several CXCR1/2 inhibitors show beneficial effects in various animal models of CVD. Read more at the source #DrGPCR #GPCR #IndustryNews

Despite major advances in the field of pharmacological CVD treatments, particularly in the field of heart contractility, growth, adaptation and metabolism. Additionally, GPCR dysregulation underlies multiple models of cardiac pathology, and most pharmacological Current literature strongly establishes increased levels and activity of GRK2 in multiple models of CVD Read more at the source #DrGPCR #GPCR #IndustryNews

dynamics of GPCR binding to different types of partners rather than the structures of the final complexes might Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors By means of these studies, we developed 14 as a fluorescent CCR2 ligand, enabling cell-free as well as cellular NanoBRET-based binding studies in a non-isotopic and high-throughput manner. Thus, our small-molecule-based fluorescent CCR2 ligand 14 represents a promising tool for future studies Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Background and purpose: Misuse of opioids has greatly affected our society. Experimental approach: We used a series of behavioural assays to evaluate the acute responses of mice to painful thermal stimulation while administering YM-254890 alone and in combination with morphine. Read more at the source #DrGPCR #GPCR #IndustryNews

cells contributes to neuron survival and accelerates axonal regeneration after optic nerve crush in mice "Glaucoma is an optic neuropathy and is currently one of the most common diseases that leads to irreversible Surprisingly, RGCs in GPR3 knockout mice were vulnerable to neural death during aging without affecting regeneration after ONC in mice." Read more at the source #DrGPCR #GPCR #IndustryNews