October 2022 "Systolic heart failure (HF) is a chronic clinical syndrome characterized by the reduction in cardiac function and still remains the disease with the highest mortality worldwide. Despite considerable advances in pharmacological treatment, HF represents a severe clinical and social burden. Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both the autonomic nervous system and the adrenal glands. Circulating catecholamines (norepinephrine and epinephrine) and aldosterone elevations are among the salient alterations that confer significant hormonal burden on the already compromised function of the failing heart. This is why sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor antagonists, which block the effects of angiotensin II (AngII) and aldosterone on the failing heart, are part of the mainstay HF pharmacotherapy presently. The adrenal gland plays an important role in the modulation of cardiac neurohormonal stress because it is the source of almost all aldosterone, of all epinephrine, and of a significant amount of norepinephrine reaching the failing myocardium from the blood circulation. Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs), such as adrenergic receptors and AngII receptors. In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain to modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1 Rs). Particular emphasis is given to findings from the past decade and a half that highlight the emerging roles of the GPCR-kinases and the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs in all tissues, including the myocardium and the adrenal gland." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs ; (d) RGS20 was found to be significantly associated with some tumor-related signaling pathways and long

extracellular domain, which contains the hormone-binding site and is linked to the transmembrane domain by the hinge

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agonist potency (Ca2+EC50 = 24 nM, cAMPi EC50 = 6.5 nM) and pharmacokinetic properties (clearance ∼20 mL/min

dynamin-dependent endocytosis in HEK293 and Huh-7-Lunet cells after activation by glucagon within 5 min

properties of DOI differed among sexes - brain and plasma concentrations of DOI were lower 30 and 60 min

sustained phase of endothelin-1 and angiotensin-II-stimulated Akt phosphorylation, whilst the peak (5 min

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Nature communications, 8(1), 443. https://doi.org/10.1038/s41467-017-00357-2 Jong, Y.

., Hong, J.

associate with the active parathyroid hormone 1 receptor (PTH1R) in different complex configurations ("hanging

The drugs also target relatively low-hanging fruit: like cytokines or tyrosine kinase receptors.

interaction follows a common pattern which is generally described by the classic “two-site” model (Crump, Gong

A rational drug discovery campaign hinges on a deep understanding of how distinct molecules interact

epithelial cells proliferation via activation by β-ionone which initiates prostate cancer cell cycle arrest (Jones non-small-cell lung cancer OR2J3 activation induced apoptosis and inhibited cell proliferation and migration in long-term

GSnP-6 displays nanomolar affinity and promising potential for blocking PSGL-1/P-selectin interaction (Wong sulfated mCCR2 peptides can outcompete available chemokines, decreasing retinal degradation in mice (Jung

recognized for inhibiting G protein signaling, they also influence specific pathways such as MAPK signaling (Song states: methods and implications The formation of functional complexes involving GPCRs and β-arrestins hinges , as well as MAPK cascade kinases which can be activated through specific β-arrestin conformations (Song

However, the receptors that these medicines target have been described as the ‘low-hanging’ fruit, and This leads to strikingly long in vitro receptor occupancy durations (at least seven days), meaning that