Gunnar Schulte Gunnar Schulte is a Professor in receptor pharmacology and research group leader for the section Receptor Biology and Signaling at the Department of Physiology and Pharmacology. University, Melbourne Australia, GPCR pharmacology; 2006) before starting his independent research team "Receptor Most importantly my research team tries to understand underlying mechanisms of WNT-receptor interaction , the relevance of receptor dynamics, and receptor complex composition for signal initiation and specification

contributed to multiple projects exploring the underlying mechanisms of biased signaling at chemokine receptor signaling profile of CXCR3’s three endogenous biased ligands, elucidating the role of site-specific receptor biased agonists, and demonstrating the ligand specificity behind GRK recruitment to endosomes upon receptor identifying the non-canonical signaling effectors involved in the activation of Atypical Chemokine Receptor 3 (ACKR3), a receptor which does not couple to G protein and has been shown to maintain its activation

< GPCR News < GPCRs in Oncology and Immunology Leukotriene B4 receptor 2 governs macrophage migration Although leukotriene B4 receptor 2 (BLT2) has been characterized as a low affinity receptor to several Kierstin Webster , Sarah A Tersey , Ryan M Anderson , Raghavendra G Mirmira Tags G-protein coupled receptor

< 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

< 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 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.

Paul Clarck , where she studied opioid receptors. AstraZeneca as a postdoctoral trainee, where she studied animal models of pain and sensory neuron sensitive-receptor Brigitte Kieffer , where she studied ligand-directed signaling at the delta-opioid receptor. Amynah studied how arrestins regulate ligand-directed signaling at delta-opioid receptors, and it is Andrew Charles that who specialized in animal models of migraine and delta-opioid receptors as a therapeutic

Published date May 13, 2023 Abstract "The adipokine chemerin is the endogenous ligand of the chemokine-like receptor 1 (CMKLR1), a member of the family of G protein-coupled receptors (GPCR). Stable receptor-ligand interactions are highly relevant for its different physiological effects, e. g Using receptor chimera of G protein-coupled receptor 1 (GPR1) and CMKLR1, we were able to identify the Tags double mutant cycle analysis , protein expression , protein-protein interaction , receptor binding

< GPCR News < GPCRs in Oncology and Immunology G protein-coupled receptors: A target for microbial metabolites demonstrated that small-molecules from gut microbiota act as ligands for specific human G protein-coupled receptors permeability of the small-molecules we elucidated their molecular interactions with specific human cell receptors Authors Gajender Aleti , Emily A Troyer , Suzi Hong Tags G protein-coupled receptors , Gut microbiota

< GPCR News < GPCRs in Oncology and Immunology Ovarian cancer G protein-coupled receptor 1 (OGR1) deficiency Published date July 11, 2023 Abstract "OGR1 (Gpr68) and GPR4 (Gpr4) are proton-activated G protein-coupled receptors These receptors have various physiological and pathophysiological roles in renal acid-base physiology Pellegrini , Nicole Joller , Carsten A Wagner , Pedro Henrique Imenez Silva Tags G-protein-coupled receptors

< GPCR News < GPCRs in Oncology and Immunology Identification of a G-protein coupled receptor-related G protein-coupled receptors (GPCRs, the largest family of human cell surface receptors) are associated Shaohan Ma, Ruyue Li, Guangqi Li, Meng Wei, Bowei Li, Yongmei Li, Chunfang Ha Tags G protein-coupled receptor

< 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.

generally, by identifying its importance in β-arrestin recruitment, β-arrestin dependent agonist-induced receptor internalisation, and receptor recycling." A Chetwynd, Richard J Ward, Graeme Milligan, Heidi C E Welch Tags C5aR1 , CXCR4 , G protein-coupled receptor (GPCR) , GPCR trafficking , Ncdn , Neurochondrin , P-Rex1 , agonist-induced internalisation , receptor desensitization , receptor endocytosis , receptor recycling , β-arrestin Source Contribute to the GPCR

< GPCR News < GPCRs in Oncology and Immunology Aberrant hormone receptors regulate a wide spectrum of endocrine tumors Published date September 23, 2024 Abstract "Aberrant G-protein coupled receptor (GPCR somatotroph tumours; AVPR2, D2DR, and SSTR5 in pituitary corticotroph tumours; GLP1R, GIPR, and somatostatin receptors

That summer, he used radioligand binding methods to dissect receptor function from the adenylyl cyclase From that point on, Paul was hooked and has since studied receptor function in human physiology, receptor Today, Paul and his team focus on previously unrecognized receptors with the hopes to use these as novel

Gloriam About this episode David Gloriam is a Professor in Computational Receptor Biology at the University University in Sweden where he worked on the bioinformatic identification of 24 novel human G protein-coupled receptors He later identified physiological hormones of such under characterized ‘orphan’ receptors and functional probes for a range of receptors. Gloriam on the web LinkedIn ResearchGate Twitter Google Scholar Computation Receptor Biology- Gloriam

< GPCR News < GPCRs in Oncology and Immunology The orphan G protein-coupled receptor 141 expressed in cells functions as an inflammation suppressor Published date April 29, 2024 Abstract "G protein-coupled receptors Here, we demonstrate that GPR141, an orphan GPCR belonging to the class A receptor family, suppresses Authors Atsuya Sawabe, Shogo Okazaki, Akira Nakamura, Ryo Goitsuka, Tomonori Kaifu Tags G protein–coupled receptor

Slosky’s research is focused on understanding how neuropeptide G protein-coupled receptors (GPCRs) regulate motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling addiction-associated behaviors in animal models without the side effects characteristic of balanced receptor Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor

via GPCR-related genes analysis Published date May 15, 2024 Abstract " Background: G protein-coupled receptors (GPCRs), the biggest family of signaling receptors, account for 34 % of all the drug targets approved Results: A GPCR-related risk score containing eight GPCR-related genes (atypical chemokine receptor 3 receptor 8 (GRM8), hydroxycarboxylic acid receptor 1 (HCAR1), 5-hydroxytryptamine receptor 5A (HTR5A ) and nucleotide-binding oligomerization domain-like receptor family pyrin domain containing 6 (NLRP6

< GPCR News < GPCRs in Oncology and Immunology Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells Published date June 29, 2023 Abstract "Proteinase-activated receptors (PARs) are G protein-coupled receptors (GPCRs) activated by limited n-terminal proteolysis.

Analysis of their Conformational Landscapes Published date June 20, 2024 Abstract "The canonical chemokine receptor CXCR4 and atypical receptor ACKR3 both respond to CXCL12 but induce different effector responses to The receptors also have distinct activation requirements. of CXCR4 and ACKR3, we employed single-molecule FRET to track discrete conformational states of the receptors This and the markedly different conformational landscapes of the receptors suggest that activation of

With respect to GPCRs, I'm particularly interested in peptide/small protein receptors and the mechanisms With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor

same university in 2005 by investigating the molecular mechanisms involved in the angiotensin type 2 receptor She identified the molecular mechanisms involved in the opposite regulation of dopamine D1 and D5 receptors She identified the structural determinant controlling biased signaling of melatonin type 2 receptors Award, she investigated biased and compartmentalized G protein signaling by the vasopressin type 2 receptor understanding the role of compartmentalized Gq signaling by the cytomegalovirus-encoded chemokine US28 receptor

signaling axes Published date May 8, 2024 Abstract "We explored the dysregulation of G-protein-coupled receptor We derived an interaction network of receptors with ligands and their biosynthetic enzymes. The expression of both receptor-ligand (or enzymes) partners improved patient stratification, suggesting Remarkably, we identified many such axes across several cancer molecular subtypes, including many involving receptor-biosynthetic from these actionable axes, including, e.g., muscarinic, adenosine, 5-hydroxytryptamine, and chemokine receptors

Symposium II Date & Time Thursday, November 2nd / 3:00 PM - 4:00 PM Title: Linking Proteinase Activated Receptor Medicine and Dentistry, Western University, researching the molecular mechanisms of Proteinase-Activated Receptors GPCR Title: Balancing G Protein Selectivity and Efficacy in the Adenosine A2A Receptor About Louis-Philippe GPCR Title: Antibodies Expand the Scope of Angiotensin Receptor Pharmacology About Meredith Skiba "Meredith pharmacology, and structural biology to study how different types of ligands modulate angiotensin receptor

signaling and cell migration Published date September 25, 2023 Abstract "Background: G protein-coupled receptor CXC chemokine receptor 4 (CXCR4) and its ligand CXCL12, both of which are overexpressed in many cancers Likewise, lysophosphatidic acid receptor 1 (LPA1) is implicated in cancer cell proliferation and migration 4 , Chemotaxis , G protein-coupled receptor , GPCR heteromer , GPCR signaling , Inflammatory disease , Lysophosphatidic acid receptor 1 Source Contribute to the GPCR News Coming soon Become a Contributor

Jean-Philippe Pin Jean-Philippe Pin participated in the discovery of metabotropic glutamate receptors been studying the allosteric modulation and activation mechanism of this family of G protein-coupled receptors His studies led to new concepts in the GPCR field, such as the activation of cell surface receptors by

< GPCR News < GPCRs in Oncology and Immunology Blockade of vasoactive intestinal peptide receptor 2 ( progression in MCF-7 cells Published date March 1, 2024 Abstract "Vasoactive intestinal peptide (VIP) receptor 2 (VIPR2) is a G protein-coupled receptor that binds to Gαs, Gαi, and Gαq proteins to regulate various