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based on RNA-seq Published date August 8, 2023 Abstract "Background: About one-third of patients with estrogen receptor alpha (ERα)-positive breast cancer have tumors which are progesterone receptor (PR) negative seven significantly enriched biological processes affected by PR and associated with G protein-coupled receptor Stefan Aebi , Rolf Jaggi Tags Breast cancer cell pools , progesterone response , RNA-seq , CRISPR/Cas9 , estrogen receptor alpha , gene expression , Progesterone receptor.

< GPCR News < GPCRs in Oncology and Immunology G protein-coupled estrogen receptor (GPER)/GPR30 forms a complex with the β1-adrenergic receptor, a membrane-associated guanylate kinase (MAGUK) scaffold protein 30 (GPR30), also named G protein-coupled estrogen receptor (GPER), and the β1-adrenergic receptor (β1AR ) are G protein-coupled receptors (GPCR) that are implicated in breast cancer progression. Both receptors contain PSD-95/Discs-large/ZO-1 homology (PDZ) motifs in their C-terminal tails through

< GPCR News < GPCRs in Oncology and Immunology Pharmacological inhibition of neuropeptide Y receptors NPY) is an abundant neurohormone in human breast carcinomas that acts on a class of G-protein coupled receptors that NPY1R and NPY5R mRNA abundance is increased by hypoxia inducible factors, which sensitizes these receptors The estrogen receptor positive MCF7 cells were significantly less invasive in 3D spheres when NPY5R was

< GPCRs in Oncology and Immunology The Effect of Cancer-Associated Mutations on Ligand Binding and Receptor Function - A Case for the 5-HT2C Receptor Published date October 29, 2024 Abstract "The serotonin 5- HT2C receptor is a G protein-coupled receptor (GPCR) mainly expressed in the central nervous system. In this study, we aimed to investigate the effects of cancer patient-derived 5-HT2C receptor mutations on ligand binding and receptor functionality.

Sponsors GPCR Retreat Program < Back to schedule Atypical Structure and Function of Typical Chemokine Receptors of the principal efforts of our laboratory is to understand the physiological consequences of NMDA receptor The NMDA receptor is a subtype of glutamate neurotransmitter receptor that regulates the formation and Our laboratory is interested in the role of NMDA receptors not only on neurons, but also on other cells Our laboratory has a long-standing interest in the way that NMDA receptors contribute to the symptoms

< GPCR News < GPCRs in Oncology and Immunology Chemoattractant receptor signaling in humoral immunity on orchestrated migration of B cells within lymphoid organs, which is governed by G protein-coupled receptors ligand binding, GPCRs are phosphorylated by different GPCR kinases (GRKs) at distinct sites on the receptor C termini, which dictates functional outcomes of β-arrestin-mediated signaling, ranging from receptor In this review, we summarize the current understanding of chemoattractant receptor signaling in the context

< GPCR News < GPCRs in Oncology and Immunology Olfactory Receptors and Tumorigenesis: Implications for Diagnosis and Targeted Therapy Published date October 4, 2024 Abstract "Olfactory receptors (ORs) are a class of G protein-coupled receptors (GPCR) widely distributed in olfactory sensory neurons and various Increasing evidence reveals the heightened expression of olfactory receptors in tumorous tissues and Authors Yi Tang, Ye Tian, Chun-Xia Zhang, Guo-Tai Wang Tags G Protein-coupled receptors , Olfactory receptors

, GPCR , Group 2 innate lymphoid cell , HES , High-affinity Fc receptor for IgE , Hypereosinophilic alpha P , Interleukin-13 receptor , Interleukin-13 receptor alpha 1/2 , Interleukin-31 receptor , Interleukin -31 receptor A , Interleukin-33 receptor , Interleukin-4 receptor alpha , Interleukin-5 receptor alpha 11 , Mas-related family of G protein-coupled receptor X1 , Mas-related family of G-protein-coupled receptor , Transient receptor potential , Transient receptor potential ankyrin 1 , Transient receptor potential

< GPCR News < GPCRs in Oncology and Immunology Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal cancer Published date June ) receptor inhibited the growth of GAL2 receptor-expressing patient-derived xenografts (PDX) of pancreatic with high GAL2 receptor expression. for GAL2 receptor agonists.

< GPCR News < GPCRs in Oncology and Immunology From odor to oncology: non-canonical odorant receptors in cancer Published date December 12, 2023 Abstract "Odorant receptors, traditionally associated with Alongside the canonical GPCR odorant receptors, dysregulation of non-canonical odorant receptors such as trace amine-associated receptors (TAARs), formyl peptide receptors (FPRs), and membrane-spanning The roles of these non-canonical chemoreceptors in cancer are complex, with some receptors promoting

Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Interrogating Multiscale Receptors for Beta-arrestin signaling in the brain in vivo and has established its importance in D2 dopamine receptors These receptors belong to the super-family of G-protein coupled receptors (GPCR), the major molecular (e.g. lithium) used for bipolar disorder therapy target signaling mechanisms regulated by dopamine receptors

< GPCR News < GPCRs in Oncology and Immunology The path of GPR87: from a P2Y-like receptor to its role first described as an orphan receptor in 2001. Despite its high structural homology to several extracellular nucleotide-activated P2Y receptors and data are preliminary and inconsistent, and IUPHAR is currently considering GPR87 as an orphan receptor Authors Katrin Sak Tags Carcinogenesis , GPR87 , LPA receptor , Metastasis , Orphan GPCR , P2Y receptor

< GPCR News < GPCRs in Oncology and Immunology Signaling by Neutrophil G Protein-Coupled Receptors that Neutrophils, which express many receptors that are members of the large family of G protein-coupled receptors (FPRs) and free fatty acids recognized by free fatty acid receptors (FFARs) regulate neutrophil functions The activation profiles of these receptors include the release of reactive oxygen species (ROS) generated The receptors have signaling and functional similarities, although there are also important differences

Committee Sponsors GPCR Retreat Program < Back to schedule Regulation and role of mitochondria delta opioid receptors pharmacology and has published seminal papers where he used various approaches to describe the role of opioid receptors anagesia as well as to study the mechanisms involved in the cellular trafficking of the delta opioid receptor

< GPCR News < GPCRs in Oncology and Immunology Interplay between G protein-coupled receptors and nanotechnology Published date July 28, 2023 Abstract "G protein-coupled receptors (GPCRs), as the largest family of membrane receptors, actively modulate plasma membrane and endosomal signalling. , GPCR ligands can endow nanoparticles with active targeting capacity for specific cells via ligand-receptor binding and mediate receptor-dependent endocytosis of nanoparticles.

< GPCR News < GPCRs in Oncology and Immunology G protein coupled receptor transcripts in human immune cells and platelets Published date September 27, 2024 Abstract "G-protein coupled receptors (GPCRs) On average, the white cells studied expressed 160 receptor mRNAs (range, 123-206). Some, but far from all, of the receptors we found have been detected earlier. We believe our data should stimulate studies of receptor function and contribute to drug development.

< GPCR News < GPCRs in Oncology and Immunology C5aR2 receptor: The genomic twin of the flamboyant C5aR1 C5a is established to interact with a set of genomically related transmembrane receptors, like C5aR1 The C5aR1 is a classical G-protein-coupled receptor (GPCR), whereas C5aR2 is a nonclassical GPCR that Authors Aurosikha Das, Pulkit K Gupta, Soumendra Rana Tags C5a; C5aR2/C5L2 receptor; lipid bilayer; molecular

< GPCR News < GPCRs in Oncology and Immunology The β2-adrenergic receptor associates with CXCR4 multimers Published date April 2, 2024 Abstract "While the existence and functional role of class C G-protein-coupled receptors of consensus is largely due to the inherent challenges of demonstrating the presence of multimeric receptor The C-X-C motif chemokine receptor 4 (CXCR4) is a class A GPCR that is a promising target of anticancer Using a bimolecular fluorescence complementation (BiFC) assay, we identified the β2 adrenergic receptor

GPCRs in Oncology and Immunology [1,2,4]Triazolo[1,5-c]pyrimidines as Tools to Investigate A3 Adenosine Receptors in Cancer Cell Lines Published date September 7, 2023 Abstract "A3 adenosine receptor is an interesting [1,2,4]triazolo[1,5-c]pyrimidines has been carried out, obtaining potent and selective A3 adenosine receptor and A1 and A2A adenosine receptors. Compound 20 has been tested on both A3 adenosine receptor positive cancer cell lines (CHO-A3AR transfected

< GPCR News < GPCRs in Oncology and Immunology Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration Published date February 1 , 2023 Abstract "C-X-C chemokine receptor 4 (CXCR4) is widely overexpressed in various types of cancer The roles of histamine and histamine receptor H1 (HRH1) in cancer pathogenesis remain controversial.

< GPCR News < GPCRs in Oncology and Immunology Orphan receptor GPR50 attenuates inflammation and insulin G protein-coupled receptors (GPCRs) are involved in endocrine and metabolic processes as well as many GPR50 (G protein-coupled receptor 50) is an orphan GPCR that shares the highest sequence homology with melatonin receptors. deficiency increased inflammation in 3T3-L1 cells and induced the phosphorylation of AKT and insulin receptor

Immunology Identification of Small-Molecule Antagonists Targeting the Growth Hormone Releasing Hormone Receptor (GHRHR) Published date August 29, 2024 Abstract "The growth hormone-releasing hormone receptor (GHRHR ) belongs to Class B1 of G protein-coupled receptors (GPCRs). model, where first the C-terminal region of the peptide interacts with the extracellular domain of the receptor and, subsequently, the N-terminus interacts with the seven transmembrane domain of the receptor, resulting

< GPCR News < GPCRs in Oncology and Immunology Role and recent progress of P2Y12 receptor in cancer development Published date June 14, 2024 Abstract "P2Y12 receptor (P2Y12R) is an adenosine-activated G protein-coupled receptor (GPCR) that plays a central role in platelet function, hemostasis, and thrombosis.

Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Complex Allosteric Cannabinoid Receptor

GPCR News < GPCRs in Oncology and Immunology Expression prevalence and dynamics of GPCR somatostatin receptors NET: a paired immunohistochemistry approach Published date November 27, 2023 Abstract "Somatostatin receptors Among the five somatostatin receptors, SST2 and SST3 are associated with apoptosis and cell cycle arrest , making these receptor subtypes better differentiated targets in precision oncology. The expression prevalence of both receptors tends to decline with tumor progression.

structural and pharmacological bases for hormone-mediated activation of G proteins by G protein-coupled receptors These approaches were invaluable to resolve the crystal structure of the beta2-adrenergic receptor (beta2AR We continue to utilize these data to better understand the basis for receptor-G protein specificity and This is an important perspective in the pursuit of receptor subtype-specific ligands, a major aspect Again, our intention is to target specific receptor subtypes.

< GPCR News < GPCRs in Oncology and Immunology G protein-coupled receptors related to autoimmunity in an increased rate of autoimmune comorbidities as evidenced by the finding of several types of neural receptor In particular, the association of the disease with several types of anti-G protein-coupled receptor ( Authors Yoko Sunami, Keizo Sugaya, Kazushi Takahashi Tags G protein-coupled receptors , Autoimmunity

< GPCR News < GPCRs in Oncology and Immunology G Protein-coupled Receptor-mediated Membrane Targeting Published date April 11, 2023 Abstract " The current dogma is that chemoattractants G protein-coupled receptors (GPCRs) activate β phospholipase C (PLCβ) while receptor tyrosine kinases (RTKs) activate γ phospholipase Tags G protein-coupled receptor (GPCR) , calcium-promoted Ras inactivator (CAPRI) , chemotaxis , neutrophils