GLP-2 receptor selectivity towards more GLP-1 receptor interaction "Background and purpose: To fully elucidate the regulatory role of the GLP-2 system in the gut and the bones, potent and selective GLP -2 receptor (GLP-2R) antagonists are needed. To examine selectivity, COS-7 cells expressing human GLP-1 or GIP receptors were assessed for cAMP accumulation Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that regulates the cardiovascular system as a vasodepressor. The recently determined structures of B2R have provided molecular insights into the functions and regulation In this review, we summarize the structure and function of B2R in relation to drug discovery and discuss future research directions to elucidate the remaining unknown functions of B2R dimerization."

October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, However, until recently, most CB2 ligands were highly lipophilic and as such not optimal for clinical We review the current state of CB2 ligand development and progress in optimising physicochemical properties Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though However, until recently, most CB2 ligands were highly lipophilic and as such, not optimal for clinical We review the current state of CB2 ligand development and progress in optimizing physicochemical properties Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types. H2R blockers are commonly used medications that recently have shown significant side effects. Read more at the source #DrGPCR #GPCR #IndustryNews

(GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations in the PK2 and PKR2 genes are involved this protein is able to enhance the activation of the ERK1/2 (extracellular signal-regulated kinase 1 /2) pathway elicited by PK2 through PKR2. PKR2, seems to be responsible for this effect. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system , emerging evidence points to CB2 playing a key role in regulating neuronal function in the central nervous Recent anatomical studies, combined with electrophysiological studies, indicate that CB2 receptors are effects of CB2 receptor activation, make this receptor an intriguing target for treating schizophrenia

Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β -Arrestin Interaction The β 2-adrenergic receptor ( β 2AR) is a prototypical and extensively studied GPCR that can provide This single point mutation in extracellular loop 2 of the β 2AR is sufficient to intrinsically bias the pocket formed by transmembrane domains 2, 3, and 7 in GPCR regulation that may contribute to biased Our studies reveal that F193 in extracellular loop 2 in the β2-adrenergic receptor mediates interactions

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July 2022 " G.CLIPS biotech is 2 years old today🎂. Looking forward for more 🎊 #team #grateful #biotech #work #birthdaycelebration" Read more at the source

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September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell carcinoma: an emerging prognostic indicator and future therapeutic target " Purpose: Beta 2-Adrenergic Receptor (β2-AR) is significantly overexpressed in various types of malignancies, which is associated However, the role of β2-AR in oral cancer is not well identified. Read more at the source #DrGPCR #GPCR #IndustryNews

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October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte by G protein-coupled receptor (GPCR) signaling. Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is Here we examined how the dual absence of RGS2 and 5 (Rgs2/5 dbKO) affects blood pressure and cardiac

October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. signatures of β-arrestin1 and 2 when bound to active PTH1R (P-R*). specifically by proximal and distal C-terminal phosphorylation and in the absence of GPCR kinases (GRKs) (R* Here, we show differences between conformational changes that are induced by P-R* or R* receptor states

Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron We hypothesized that isoform 2 of rho-kinase (ROCK2), acting as downstream GPCRs, mediates adjustment Small-interfering RNA (siRNA) technology was also used to knockdown either ROCK1 or ROCK2. , and depressed background resting currents via Gαq/ROCK2 signaling. Read full article

September 2022 Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of various processes including neuroendocrine release, cognition, and nerve regeneration. Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts To understand the basis of the ligand preferences of the receptors and to assist structure-based drug Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing It plays a key role in the regulation of human calcium and thus mineral metabolism. -stimulated Ca2+i mobilization using mutations in either the VFT domains and/or HH bundle intraloop-2 for Bone and Mineral Research (ASBMR)." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic reticulum membrane associated with mitochondria. It is classified into two types: Sigma-1 (S1R) and Sigma-2 (S2R) based on their biological functions. 6c resulting in 100% displacement and a Ki of 95.5 nM. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to the Serotonin 1A Receptor "G protein-coupled receptors (GPCRs) constitute the largest class For this, we explored the possible role of the K101 residue in a cholesterol recognition/interaction amino acid consensus (CRAC) motif in transmembrane helix 2 in conferring the thermal stability of the serotonin1A receptor.

August 2022 Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in endpoint, with KarXT demonstrating a statistically significant and clinically meaningful 9.6-point reduction KarXT also demonstrated an early and sustained statistically significant reduction of symptoms, as assessed by PANSS total score, starting at Week 2 and maintained such reduction through all timepoints in the Read more at the source #DrGPCR #GPCR #IndustryNews

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle in enhanced signalling through their cognate G protein-coupled receptors (GPCR). lesions and vascular remodelling. In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs Read full article

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR) signaling GRK2/β-arrestin2 play multiple roles in the pathological mechanisms of a wide range of diseases including This review summarizes the roles of GRK2/β-arrestin2 in immune cell function and focuses on the pathological

April 2022 Addex Therapeutics Completes Patient Enrollment For Dipraglurant Blepharospasm Phase 2 Clinical Dipraglurant selectively targets the metabotropic glutamate receptor subtype 5 (mGlu5) through allosteric Read more at the source #DrGPCR #GPCR #IndustryNews

(PI(4,5)P2) lipids have been shown to stabilize an active conformation of class A G-protein coupled receptors previous molecular dynamics (MD) simulation studies have shown PI(4,5)P2 interacting with the Glucagon receptor We demonstrate how tail composition plays a role in modulating the binding of PI(4,5)P2 lipids to GCGR This suggests differences in the regulatory function of PI(4,5)P2 between class A and class B GPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 Novel Therapies for Cardiometabolic Disease: Recent Findings in Studies with Hormone Peptide-Derived G Protein Coupled Receptor Agonists "The increasing prevalence of obesity and type 2 diabetes (T2DM) Great success has been reached with therapies based on the GLP-1 receptor monoagonism; therefore, a logical The present review describes novel findings regarding the complex biology of the preproglucagon-derived Read more at the source #DrGPCR #GPCR #IndustryNews