📰 GPCR Weekly News

Hello Readers👋,

We are working on bringing your the latest GPCR News more frequently directly in your inbox and in the Ecosystem. Below is your Classified GPCR News at a glance for November 28 to December 4th, 2022.

Adhesion GPCRs

• GPR56 C-terminal fragment mediates signal received by N-terminal fragment of another adhesion GPCR Latrophilin1 in neurons.

GPCR Activation and Signaling

• Biased Activation Mechanism Induced by GPCR Heterodimerization: Observations from μOR/δOR Dimers.

• FFAR4 improves the senescence of tubular epithelial cells by AMPK/SirT3 signaling in acute kidney injury.

• Distal extracellular teneurin region (teneurin C-terminal associated peptide; TCAP) possesses independent intracellular calcium regulating actions, in vitro: A potential antagonist of corticotropin-releasing factor (CRF).

• Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity.

• Mechanisms underlying divergent relationships between Ca2+ and YAP/TAZ signaling.

• Virtual screening yields refined GPCR agonists.

GPCR Binders, Drugs, and more

• Altered signaling at the PTH receptor via modified agonist contacts with the extracellular domain provides a path to prolonged agonism in vivo.

GPCRs in Cardiology, Endocrinology, and Taste

• Pathogenic variants of the GNAS gene introduce an abnormal amino acid sequence in the β6 strand/α5 helix of Gsα, causing pseudohypoparathyroidism type 1A and pseudopseudohypoparathyroidism in two unrelated Japanese families.

• Quantification of changes in human islet G protein-coupled receptor mRNA expression in obesity.

• Alterations in mouse visceral adipose tissue mRNA expression of islet G-protein-coupled receptor ligands in obesity.

• The Ca2+/CaM, Src kinase and/or PI3K-dependent EGFR transactivation via 5-HT2A and 5-HT1B receptor subtypes mediates 5-HT-induced vasoconstriction.

GPCRs in Neuroscience

• CGRP physiology, pharmacology, and therapeutic targets: Migraine and beyond.

• Emerging approaches for decoding neuropeptide transmission.

• Exploring pharmacological inhibition of Gq/11 as an analgesic strategy.

• Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of depression.

• Superconserved receptors expressed in the brain: Expression, function, motifs and evolution of an orphan receptor family.

GPCRs in Oncology and Immunology

• Germinal Center-Related G Protein-Coupled Receptors in Antibody-Mediated Autoimmune Skin Diseases: from Basic Research to Clinical Trials.

• Oncogenic signaling of the free-fatty acid receptors FFA1 and FFA4 in human breast carcinoma cells.

• Targeted inhibition of the GRK2/HIF-1α pathway is an effective strategy to alleviate synovial hypoxia and inflammation.

Methods & Updates in GPCR Research

• CPGL: Prediction of Compound-Protein Interaction by Integrating Graph Attention Network With Long Short-Term Memory Neural Network.

• Establishment of a CaCC-based Cell Model and Method for High-throughput Screening of M3 Receptor Drugs.

• High-performance optical control of GPCR signaling by bistable animal opsins MosOpn3 and LamPP in a molecular property-dependent manner.

• A quantitative systems pharmacology model for simulating OFF-Time in augmentation trials for Parkinson's disease: application to preladenant.

• Genetically encoded tools for in vivo G-protein-coupled receptor agonist detection at cellular resolution.

Reviews, GPCRs, and more

• The diversity of invertebrate visual opsins spanning Protostomia, Deuterostomia, and Cnidaria.

Structural and Molecular Insights into GPCR Function

• Computational investigation of functional water molecules in GPCRs bound to G protein or arrestin.

• Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its interactions with antagonist and agonist ligands.

• Cryo-EM structure of G-protein-coupled receptor GPR17 in complex with inhibitory G protein.

• Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to the Serotonin1A Receptor.

• Molecular insights into the mechanism of sugar-modified enkephalin binding to opioid receptors.

• Oligomerization of the heteromeric γ-aminobutyric acid receptor GABAB in a eukaryotic cell-free system.

Call for GPCR Papers

• GPCRs: Signal Transduction

• Advances in Computational and Chemical Methods to study GPCR Signal Transduction.

• Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology.

GPCR Events, Meetings, and Webinars

• 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston.

• 2nd ERNEST Training School – February 20th to March 3rd.

• GEM2023 (14-17 March 2023).

• 8th and final ERNEST Meeting May 3-7, 2023 in Crete.

• The Illuminating the Understudied Druggable Proteome Conference. June 4-8,2023.

• 2023 Molecular Pharmacology (GRS) Seminar GRC. June 10 - 11.

• Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. June 11-16, 2023.

• 19th World Congress of Basic & Clinical Pharmacology 2023. July 2 - 7.

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