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November 2021 Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID offering of high-quality synthetic DNA using its silicon platform, today announced it has launched Revelar Biotherapeutics, Inc., an independently operated, new biotechnology company to develop and commercialize In addition, Revelar will have the ability to leverage the antibody discovery and optimization platform

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor (GPCR) regulation. In a recent issue of Molecular Cell, Fonseca et al. identified a previously overlooked desensitization mechanism. Agonist activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor to internalize and desensitize. Eliminating β2AR S-nitrosylation by mutation of C265 augments β2AR protein kinase A signaling, enables β2AR nitric oxide (NO) signaling, renders mice resistant to bronchoconstriction, and protects mice from allergen-induced asthma." Read more at the source #DrGPCR #GPCR #IndustryNews

The captured structures reveal a dynamic of conformational changes initiated by the binding of an agonist

Applied to HIV-1 envelope glycoproteins gp120, our quantitative analysis revealed agonist-like properties

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

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine

Retrograde trans-synaptic rabies virus tracing revealed that postsynaptic cAMP signaling is required

October 2022 Genome-scale CRISPR screening reveals that C3aR signaling is critical for rapid capture

September 2022 Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of Mutant proteins were assayed to help reveal the basis of ligand specificity, and structural comparison

October 2022 Use of CRISPR/Cas9-edited HEK293 cells reveals that both conventional and novel protein

August 2022 GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin The structures reveal that transmembrane helices TM5 and TM6 alternate lengths as a macro-switch to determine

β-arrestins (βarrs) play multifaceted roles in the function of G protein-coupled receptors (GPCRs). βarrs typically interact with phosphorylated C-terminal tail (C tail) and transmembrane core (TM core) of GPCRs. However, the effects of the C tail- and TM core-mediated interactions on the conformational activation of βarrs have remained elusive. Here, we show the conformational changes for βarr activation upon the C tail- and TM core-mediated interactions with a prototypical GPCR by nuclear magnetic resonance (NMR) spectroscopy. Our NMR analyses demonstrated that while the C tail-mediated interaction alone induces partial activation, in which βarr exists in equilibrium between basal and activated conformations, the TM core- and the C tail-mediated interactions together completely shift the equilibrium toward the activated conformation. The conformation-selective antibody, Fab30, promotes partially activated βarr into the activated-like conformation. This plasticity of βarr conformation in complex with GPCRs engaged in different binding modes may explain the multifunctionality of βarrs. Read full article

This week's highlights: Kudos to our partner, GPCR Therapeutics, for partnering with Bridge Biotherapeutics We'll pause our regular updates during this time and will resume our newsletter in the upcoming year GPCR Activation and Signaling GPCR screening reveals that the metabolite receptor HCAR3 regulates epithelial Updates in GPCR Research Phosphorylation Sites of the Gastric Inhibitory Polypeptide Receptor (GIPR) Revealed meta-dynamics/FMO3 approach Industry News GPCR Therapeutics Announces Out-Licensing Agreement with Bridge Biotherapeutics

at the Citeline Pharma Intelligence Awards Japan 2023 BioMap and Sanofi to co-develop AI modules for biotherapeutic

Senior Scientist, Cryo-Electron Microscopy Postdoctoral Research Associate Senior Scientist - Discovery Biotherapeutics

Clinical Pharmacology 2026 GPCR Jobs NEW Postdoctoral Research Associate Senior Scientist - Discovery Biotherapeutics

., for their study on Systems modeling of oncogenic G-protein and GPCR signaling reveals unexpected differences infection GPCRs in Oncology and Immunology Systems modeling of oncogenic G-protein and GPCR signaling reveals Senior Scientist, Cryo-Electron Microscopy Postdoctoral Research Associate Senior Scientist - Discovery Biotherapeutics

Jianming Han, Tao Che for their analysis of GPCR-G protein selectivity revealed by structural pharmacology Insights into GPCR Function Cryo-EM advances in GPCR structure determination GPCR-G protein selectivity revealed 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology NEW Senior Scientist - Discovery Biotherapeutics

We will be back next week with our regular weekly GPCR news digest.