October 2022 Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination report the finding of two copy number variants (CNVs) in a 12-year-old boy presenting both with autism spectrum

diversity of location, effectors, and signaling of GPCRs, and how these could interact to generate specific spatiotemporal patterns of GPCR signaling in cells."

September 2022 "Background Spinal cord injury (SCI) is a common trauma in clinical practices.

Nuclear magnetic resonance (NMR) spectroscopy allows the determination of atomic-level information on In particular, we focus on the application of on-cell NMR spectroscopy to characterize ligand interactions

András D Tóth , Gábor Turu , and László Hunyady  for their research on Functional consequences of spatial Don’t miss out—secure your spot today! Sponsorship Opportunities :   Boost your brand’s visibility at this scientific event. : dialing up and down neurotransmitter responses by G-protein regulators Functional consequences of spatial

As Chief Matchmaker, I recently had the pleasure of speaking with Beth Fleck, Director of In Vitro Pharmacology

Lipid molecules, such as phosphoinositides, can bind to specific domains of β-arrestins, promoting their binds to the plasma membrane by inserting the C-edge into the lipid bilayer, allowing it to explore space Stimulated condition in the presence of a stimulated receptor: Spontaneous insertion into the plasma The increase in active β-arrestin molecules and the time they spend diffusing on the plasma membrane Diversity and specificity in the regulated endocytic membrane trafficking of G-protein-coupled receptors

Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors (GPCRs) can form biologically active homodimers or heterodimers which drive specific signaling pathways A more in-depth analysis of the functional specificity of transmembrane peptides will provide a better

October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent animals both exhibited skin dysbiosis, with reduced microbial diversity and expansion of Staphylococcus species

The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine receptor CXCR4 specifies However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient to specify In conclusion, this study provides evidence that distal C-tail phosphorylation sites specify GRK-βarrestin-mediated

Modulating a single function of a specific aGPCR isoform while affecting no other function and no other engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3, and specifically In cellular-adhesion assays, LK30 specifically broke the trans-cellular interaction of ADGRL3 with teneurin Our work provides proof of concept for the modulation of isoform- and ligand specific aGPCR functions

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on

February 2022 Septerna emerges with $100M to spark 'second golden age' of prolific drug target GPCR with pioneer as co-founder "J an 27, 2022 07:00am Septerna wants to spark a second golden age in G-protein-coupled Better known as GPCR, the fruitful research space has led to more than 700 approved drugs over previous

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer

Besides, ligand-specific subtle differences in the conformations assumed by intracellular loop 2 and

VIB spin-off Confo Therapeutics today announced that it has entered into a collaborative agreement with

October 2022 "Neisseria meningitidis is a Gram-negative opportunistic pathogen that is responsible for causing human diseases with high mortality, such as septicemia and meningitis. The molecular mechanisms N. meningitidis employ to manipulate the immune system, translocate the mucosal and blood-brain barriers, and exert virulence are largely unknown. Human-associated bacteria encode a variety of bioactive small molecules with growing evidence for N-acyl amides as being important signaling molecules. However, only a small fraction of these metabolites has been identified from the human microbiota thus far. Here, we heterologously expressed an N-acyltransferase encoded in the obligate human pathogen N. meningitidis and identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor (GPCR) S1PR4. During this process, we also characterized two mammalian N-acyl amides derived from the bovine medium. Both groups of metabolites suppress anti-inflammatory interleukin-10 signaling in human macrophage cell types, but they also suppress the pro-inflammatory interleukin-17A+ population in TH 17-differentiated CD4+ T cells." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Melanocortin 3 receptor (MC3R) is a G-protein coupled receptor (GPCR) that is defined as a regulator of appetite/hunger balance mechanisms mostly up to date. In addition to its function about weight gain and appetite control mechanisms of MC3R, recent studies showed that MC3R controls growth, puberty, and circadian rhythms as well. Despite the drastic effects of the MC3R deficiency in humans and other mammals, its cellular mechanisms are still under investigation. In this review paper, we aimed to point out the importance of the MC3R regulations in three main concepts: 1) its impact on weight and appetite control, 2) the control of growth, puberty, and circadian rhythm, and, 3) its protein-protein interactions and cellular mechanisms." Read more at the source #DrGPCR #GPCR #IndustryNews

Consistent with the multilumen phenotype, mitotic spindles are incorrectly oriented during cystogenesis

have exploited gene capture as part of their strategy to escape immune surveillance, promote virus spreading

October 2022 "Enzymatic and cellular signalling biosensors are used to decipher the activities of complex biological systems. Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in the human body, are plentiful and vary in utility, form and function. Their applications have continually expanded our understanding of this important protein class. Here, we briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric signalling complexes." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE

August 2022 "A confluence of factors has renewed interest in the scientific 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 basic and clinical research, and the reconsideration and relaxation of existing drug policies. With the United States Food and Drug Administration's designation of psilocybin as a "Breakthrough Therapy" for treatment-resistant depression, a new path has been forged for the conveyance of psychedelics to the clinic. Essential to the further development of such applications, however, is a clearer understanding of how these drugs exert their effects at the molecular level. Here we review the current knowledge regarding the molecular details of psychedelic drug actions and suggest that these discoveries can facilitate new insights into their hallucinogenic and therapeutic mechanisms." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). FSHR is involved in reproductive processes such as gonadal development and maturation. 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. How this HR is involved in hormone binding and signal transduction is still an open question. We combined in vitro and in situ chemical crosslinking, disulfide pattern analysis, and mutation data with molecular modeling to generate experimentally driven full-length models. These models provide insights into the interface, important side-chain interactions, and activation mechanism. The interface indicates a strong involvement of the connecting loop. A major rearrangement of the HR seems implausible due to the tight arrangement and fixation by disulfide bonds. The models are expected to allow for testable hypotheses about signal transduction and drug development for GPHRs." Read more at the source #DrGPCR #GPCR #IndustryNews

sensitivity of G-protein coupled receptors: Unraveling molecular mechanisms and physiological implications Sphingosine Preparations of Manduca sexta and Identification of the Receptor-Associated G Proteins in Two Lepidopteran Species

is a powerful method for studying the functional consequences of various genetic variants within a specific Instead, a collection of titratable residues spans from the extracellular surface to the transmembrane Specifically, the study revealed that the protonation of key residues surrounding an extracellular facing By evaluating a broad spectrum of mutations, DMS can help predict which patient subpopulations will respond Moreover, DMS requires considerable resources, including time, financial investment, and specialised

Get your space suits on, GPCR cadets! Adriano Marchese , et al. for their excellent work on Receptor determinants for ß-arrestin functional specificity regulates male reproduction in teleosts: an in vitro study in Channa punctata GPCRs in Neuroscience Neuron specific Receptor Function - A Case for the 5-HT2C Receptor Reviews, GPCRs, and more Functional consequences of spatial chronic pain and neurological diseases Structural and Molecular Insights into GPCR Function Native mass spectrometry

The presentations and discussions sparked new ideas and collaborations, shaping the future of the field October 21st to 27th, 2024 Industry News UNC School of Medicine to Receive $3-Million Award from ARPA-H’s Sprint Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Activated by GPRCs in Olfactory Neuronal Precursor Cells Derived from Patients Diagnosed with Schizophrenia Sphingosine GPCRs in Oncology and Immunology Characterization, expressional and evolutionary analysis of five fish-specific

understanding of class B1 GPCR biology but also opens new avenues for developing therapeutic agents that target specific