January 2022 "G-protein-coupled receptors’ star has been on the rise in biotech in recent years as researchers have discovered the vast potential for GPCR-targeting drugs in treating a range of health conditions, from cancer and genetic disorders to inflammation and metabolic imbalances. Among those hitching their wagons to that star are Verily and Sosei Heptares , which have struck a research agreement to discover new GPCR targets that’ll fuel the development of potential drug candidates. The financial details of the strategic collaboration weren’t released, but Sosei Heptares ’ past two team-ups in GPCR-based drug discovery have clocked in at $1 billion—with Genentech—and, just last November, $2.6 billion in a partnership with Neurocrine." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 ADGRL3 genomic variation implicated in neurogenesis and ADHD links functional effects to GIP has been linked to the pathogenesis of diabetes mellitus, and our analyses suggest a potential link

Structurally, the extensive extracellular domain, which contains the hormone-binding site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors.

September 2022 High GPER expression in triple-negative breast cancer is linked to pro-metastatic pathways heterogeneous disease with few effective targeted therapies and precision therapeutic options over a long Besides, high GPER expression was significantly linked to the worse survival in patients with lymph node Transcriptome-based bioinformatics analysis revealed that GPER was linked to pro-metastatic pathways

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 be an important factor for survival in four other cancers (clear renal cell carcinoma: p < 0.001, lung ; (d) RGS20 was found to be significantly associated with some tumor-related signaling pathways and long

February 2022 Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner by data from a Phase 3 bridging study of oliceridine injection compared to IV morphine, conducted in China success payments upon approval and commercialization milestones, as well as a 10% royalty on net sales in China commercialization of novel medicines for patients with central nervous system (CNS) disorders, today announced that China

June 2022 "June 15, 2022 06:30 AM EDT - In 2016, Abbie Celniker was promoted to partner at Third Rock Ventures as the firm raised just over $600 million for its fourth fund. Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. Coming on its 15th year, Third Rock Ventures announced its sixth fund today — and largest one by far — at a whopping $1.1 billion. Adding it all up, Third Rock has raised $3.8 billion since its inception. That money has gone to some 60 biotechs, much of it as early funding." Read more at the source #DrGPCR #GPCR #IndustryNews

HLGR2 RNAi led to a low pupation rate (45.00%), body malformation, abnormal wing expansion, failed cuticle Conclusion: HLGR2 is essential for the growth and development and wing expansion and maturation in H.

In this study, the expression and signaling of β2-ADR in B cells during collagen-induced arthritis (CIA investigated to provide an explanation of why only B cells from arthritic mice are able to improve CIA stimulation of β2-ADR agonist terbutaline by flow cytometry. β2-ADR-expressing B cells increase during CIA Stimulation of CIA B cells with the β-ADR agonist terbutaline increased pp38 MAPK independent of the

Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the that orchestrate P-gp expression and highlight unappreciated connections between multiple pathways linked

Heterodimerization when Expressed Heterologously in Saccharomyces cerevisiae The beta 2 adrenergic receptor cross-linked intestinal dendritic cells Methods & Updates in GPCR Research Generation of CRISPR/Cas9 modified human iPSC line

In this study, we generated and characterized human embryonic kidney 293A (HEK293A) cell lines devoid Our PKC KO cell lines expand the repertoire of KO HEK293A cell lines available to research GPCR pharmacology pharmacological tools to study PKC isozymes generally lack specificity and/or potency, we present the PKC KO cell lines

modulation of O-glycosylation and tyrosine sulfation on CCR5 and CCR1 function In this study engineered cell lines pharmacology however the reported effects can vary depending on the receptor-ligand pairs and potentially cell line the observed phenotype since many glycosyltransferases and the two TPSTs also carry O-glycosylation (King In addition, tyrosine sulfation is heterogenous between cell lines or even on the same cell (Scurci I

KISS1R signalling and physiological output in the hormone receptor-negative MDA-MB-231 and BT-20 cell lines We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression. stimulate migration or pro-metastatic behaviour, as divergent responses were observed in the two TNBC lines

Such effects are mediated by the suppression of gut IEL effector functions linked to the dampening of These data reposition key roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R

A rational drug discovery campaign hinges on a deep understanding of how distinct molecules interact can provide a comprehensive understanding of how drugs interact with different receptor regions and link

We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with semi-quantitative receptor mapping in living cells and validated the specific expression of A2BAR in CRC cell lines

that one should consider when attempting to compare functional outcomes from different studies, both linked to the specific assay mechanism and linked to its specific execution, as these may heavily impact the

Electroretinography showed restoration of visual function in all three transgenic Gγ1-deficient lines In all dark-adapted transgenic lines, Gαt1 was targeted to the outer segments, reversing its diffuse

Wednesday-Friday, 5th-7th October 2022 Place Evotec Campus Levi-Montalcini, Verona, Italy Downloads and Links

gastropods Unraveling the G protein-coupled receptor superfamily in aphids: Contractions and duplications linked Morgan Healthcare Conference Andrew Hopkins appointed CBE by HM King Charles III Voyager Therapeutics

Graeme Milligan for receiving the Order of British Empire from King Charles III in recognition of his Immunology Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung Graeme Milligan was awarded the Order of British Empire by King Charles III for services to Biochemical

., explored the function of β-arrestin 2 in MOR signaling using the SH-SY5Y cell line that endogenously learning more about the molecular details of this study, you can consult the article at the following link

detected by the Boyden chamber migration assay, performed on macrophages derived from both the THP-1 cell line

LINKED ARTICLES: This article is part of a themed issue on Structure Guided Pharmacology of Membrane

HH controls SMO subcellular localization and activity in a polarized epithelium using the Drosophila wing Together, these results link the morphogenetic effects of HH to the apico-basal distribution of SMO and

an oxysterol ligand and will facilitate the development of therapeutic approaches that target EBI2-linked