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During pregnancy, the mammary gland (MG) undergoes remodeling, which involves alveolar differentiation of mammary epithelial cells (MECs), which is essential for breast milk production and secretion. development or MEC differentiation. and lipid synthesizing markers. using the HC11 cells as a model. Relative to control, 10μM THC and 10μM CBD reduced mRNA levels of milk proteins (CSN2 and WAP), lipid

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the fine-tuning of Gi/o signaling "Aims: Cardiac contractility, essential to maintaining protein signaling (RGS) 2 and 5, separately, was shown to cause G protein dysregulation, contributing to modest Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is Read more at the source #DrGPCR #GPCR #IndustryNews

activation of G protein-coupled receptors (GPCRs) is of paramount importance to the field of cardiovascular medicine Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation and revealing unexpected mechanisms. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Interface from Molecular Dynamics Simulations and Quantum Chemical Calculations "Allosteric modulators specific receptor modulation. The allosteric cavities are detectable in various membrane compositions. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent We tested if this is true for the glucagon receptor (GCGR), which mediates physiological regulation of hepatic glucose metabolism via cAMP signaling. and transit via EEA1-marked endosomes shown previously to be sites of GPCR/Gs-stimulated production Read more at the source #DrGPCR #GPCR #IndustryNews

Much of the understanding of psychedelic pharmacology is derived from rodent models, but most of this preclinical research has only focused on male mice. potential - in male and female mice. DOI elicited more HTR in female as compared to male C57BL/6J mice, a sex-specific exacerbated behavior C57BL/6J mice.

Due to its irreversible activation mechanism, some agonists that rapidly desensitized PAR2 have been of MAPKs, but in a delayed and sustained manner compared to the rapid and transient signals induced by GB83, which may be the reason why GB83 is recognized as an antagonist of PAR2. Our results revealed that GB83 is a bona fide agonist of PAR2 that uniquely modulates PAR2-mediated cellular Read more at the source #DrGPCR #GPCR #IndustryNews

In this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor 5 (mGlu5) were performed. The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system modulators. Chemical libraries containing fragment- (1.6 million molecules) and lead-like (4.6 million molecules)

involved in epithelial malignancies. motifs. It effectively attenuates PAR2&4-Akt/PKB associations; PAR4 instigated Matrigel invasion and migration EGFR/erbB is among the most prominent cancer targets. Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Ligands must first partition into the surrounding membrane and take lipid paths to these sites. Remarkably, a significant part of the bound ligands appears exposed to the membrane lipids. Using classical and enhanced molecular dynamics simulations, we show that membrane lipids are critical Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Lysosomes coordinate cellular metabolism and growth upon sensing of essential nutrients transmembrane protein that enables cholesterol-dependent activation of the master growth regulator, the protein kinase mechanistic target of rapamycin complex 1 (mTORC1). mTORC1 activation. Read more at the source #DrGPCR #GPCR #IndustryNews

In a recent issue of Molecular Cell, Fonseca et al. identified a previously overlooked desensitization mechanism. Eliminating β2AR S-nitrosylation by mutation of C265 augments β2AR protein kinase A signaling, enables β2AR nitric oxide (NO) signaling, renders mice resistant to bronchoconstriction, and protects mice from Read more at the source #DrGPCR #GPCR #IndustryNews

designed from the intracellular loops of G protein-coupled receptors (GPCRs) that act in an allosteric manner to modulate the activity of GPCRs. Over the past 2 decades, pepducins have progressed initially from pharmacologic tools used to manipulate GPCR activity in an orthosteric site-independent manner to compounds with therapeutic potential that Read more at the source #DrGPCR #GPCR #IndustryNews

Matthew E. on Friday, October 7th at 1 PM ET. Don't miss the chance to listen to his latest research on the field. It's a great opportunity to get warmed up for the upcoming Summit starting the next Monday.

understanding and translational potential of psychedelic drugs such as lysergic acid diethylamide (LSD), mescaline , and psilocybin: the desire for additional approaches to mental health care, incremental progress in such applications, however, is a clearer understanding of how these drugs exert their effects at the molecular Here we review the current knowledge regarding the molecular details of psychedelic drug actions and Read more at the source #DrGPCR #GPCR #IndustryNews

In the prospect of a psychedelic drug becoming again an approved treatment, much of these efforts have been oriented toward exploring the relationship between the actual psychedelic effects and those manifestations Here we discuss some of the most recent findings in human studies and contextualize them considering previous preclinical models studying phenomena related to synaptic plasticity. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis "β-Arrestins are ubiquitously expressed intracellular proteins with many functions which interact directly and indirectly with a wide number of cellular partners and mediate downstream Originally, β-arrestins were identified for their contribution to GPCR desensitization to agonist-mediated Read more at the source #DrGPCR #GPCR #IndustryNews

Systematic modification of 1 was performed to produce compounds with improved potency and ADME properties agonist potency (Ca2+EC50 = 24 nM, cAMPi EC50 = 6.5 nM) and pharmacokinetic properties (clearance ∼20 mL /min/kg in rats) was identified. Read more at the source #DrGPCR #GPCR #IndustryNews

Background and purpose: Vascular tone is regulated by the relative contractile state of vascular smooth muscle Several integrins directly modulate VSMC contraction by regulating calcium influx through L-type voltage-gated Read more at the source #DrGPCR #GPCR #IndustryNews

Here, we reveal that the Smog GPCR transduces Fog signal to regulate Rho kinase accumulation and myosin activation in the medioapical region of cells to control apical constriction during SG invagination. Our data support a model wherein Smog regulates distinct myosin pools and actin cytoskeleton in a ligand-dependent manner during epithelial tube formation." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in the central nervous system, which mediates the functional response to endocannabinoids and Cannabis compounds understanding of CB1 ligand interactions, selectivity, receptor activation and allosteric modulation In this review, we describe the structural determinants for modulation of CB1 receptors by different Proteins (BJP 75th Anniversary). " Read more at the source #DrGPCR #GPCR #IndustryNews

Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends on different molecular mechanisms triggered by conserved amino acid residues. Although studies have focused on the G-protein signaling state, the mechanism for β-arrestin signaling Studies have indicated that transmembrane helix 7 (TMH7) and the highly conserved NPXXY motif can be mechanism to trigger β-arrestin recruitment. " Read more at the source #DrGPCR #GPCR #IndustryNews

accumulation in the cell as a secondary messenger. On the other hand, they showed the ability to couple with Gαq/11 protein and make Ca2+ mobilization at Studies about the Gα protein coupling bias of mutant AVPR2s may broaden our understanding of the relationship shed light on the development of more effective new therapeutics." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology, We now summarize important pharmacological, molecular, and cellular studies relevant to D1-mediated β-arrestin-related toward or against D1-mediated β-arrestin either can improve or impair functional outcomes. We discuss the importance of understanding the translatability of cell and animal models to have more Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function. The scope of our review is to present the most important of the aforementioned ligands, highlight their properties and exhibit the current state-of-the-art pallet of promising drug candidates or useful molecular Read more at the source #DrGPCR #GPCR #IndustryNews

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