📰 GPCR Weekly News, October 30 to November 4, 2023

Good day, GPCR folks! Take advantage of our GPCR highlights of the week.

• Dr. Hannes Schihada and his lab team developed fluorescent analogues for real-time binding studies of orphan GPCR GPR3:

Save the dates:

• November 17: Join our final Dr. GPCR Symposium for the year on GPCRs in Immunology and Oncology! A panel of top experts will discuss in a roundtable starting at 10 AM EST. Find speaker details on the Live Talks page and mark your calendar HERE.

You don't want to miss out on our monthly Dr. GPCR Newsletter for exclusive content, check out our latest video featuring Dr. Kathleen Caron.

Check out the weekly Classified GPCR News from October 30 to November 4, 2023.

GPCR Activation and Signaling

• The G protein alpha chaperone and guanine-nucleotide exchange factor RIC-8 regulates cilia morphogenesis in Caenorhabditis elegans sensory neurons

• CaSR links endocytic and secretory pathways via MADD, a Rab11A effector that activates Rab27B

• Targeting of insulin receptor endocytosis as a treatment to insulin resistance

• Stepwise phosphorylation of BLT1 defines complex assemblies with β-arrestin serving distinct functions

• Phosphorylation motif dictates GPCR C-terminal domain conformation and arrestin interaction

• Ready for the sheet: β-strand folding of phosphorylation clusters guides GPCR binding to arrestin

• Dietary dibutyryl cAMP supplementation regulates the fat deposition in adipose tissues of finishing pigs via cAMP/PKA pathway

GPCR Binders, Drugs, and more

• Cloning and deorphanization of three inotocin (insect oxytocin/vasopressin-like) receptors and their ligand from the tick Ixodes scapularis

• Evidence that pyrophosphate acts as an extracellular signalling molecule to exert direct functional effects in primary cultures of osteoblasts and osteoclasts

• Development of Fluorescent AF64394 Analogues Enables Real-Time Binding Studies for the Orphan Class A GPCR GPR3

• Antimalarial and Plasmodium falciparum serpentine receptor 12 targeting effect of FDA approved purinergic receptor antagonist

GPCRs in Cardiology, Endocrinology, and Taste

• Palmitoylation-Dependent Regulation of Cardiomyocyte Rac1 Signaling Activity and Minor Effects on Cardiac Hypertrophy

• Single cell G-protein coupled receptor profiling of activated kidney fibroblasts expressing transcription factor 21

GPCRs in Neuroscience

• Pregabalin inhibits purinergic P2Y2 receptor and TRPV4 to suppress astrocyte activation and to relieve neuropathic pain

GPCRs in Oncology and Immunology

• Systems Pharmacodynamic Model of Combination Gemcitabine and Trabectedin in Pancreatic Cancer Cells. Part II: Cell Cycle, DNA Damage Response, and Apoptosis Pathways

• Spliceosome mutations are associated with clinical response in a phase 1b/2 study of the PLK1 inhibitor onvansertib in combination with decitabine in relapsed or refractory acute myeloid leukemia

Methods & Updates in GPCR Research

• Mining the ZINC database of natural products for specific, testosterone-like, OXER1 antagonists

• A 19F-qNMR-Guided Mathematical Model for G Protein-Coupled Receptor Signaling

• Optical Approaches for Investigating Neuromodulation and G Protein-Coupled Receptor Signaling

• Protocol for identifying physiologically relevant binding proteins of G-protein-coupled receptors

Reviews, GPCRs, and more

• RGS proteins and cardiovascular Angiotensin II Signaling: Novel opportunities for therapeutic targeting

• Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

• Ligand selectivity hotspots in serotonin GPCRs

• Study of G protein-coupled receptors dimerization: From bivalent ligands to drug-like small molecules

Structural and Molecular Insights into GPCR Function

• Hydrophobic interaction between the TM1 and H8 is essential for rhodopsin trafficking to vertebrate photoreceptor outer segments

Industry News

• Sosei Heptares Will Receive US$3.75 Million Payment in Multi-Target Partnership

• Sosei Heptares Announces Submission of New Drug Application in Japan for Daridorexant (ACT-541468), a Dual Orexin Receptor Antagonist for the Treatment of Insomnia

• OMass Therapeutics Releases First Protein Structures in PDB, Advances Lupus Therapy Research

• Structure Therapeutics Receives R&D Achievement of the Year Award for GPCR Research

• Bryan Roth, Natural Products, and the John Daly Legacy

• Sosei Heptares’ Partner, Pfizer, Progresses Its GLP-1 Receptor Agonist PF-06954522 into a Phase 1 Trial

• Andrew Hopkins Inducted into RSC BMCS Hall of Fame and Receives Associated Medal in 2023

• 'This field is in its infancy': Amgen noncommittal on oral obesity med until phase 1 data arrive

• Form and Function - Consequences of subcellular cAMP signaling revealed

• AI Predicts How GPCRs Respond to Drug-Like Molecules

• Accurately predicting GPCR P2Y1 membrane protein ligand binding with Free Energy Perturbation

GPCR Events, Meetings, and Webinars

• November 10, 2023 | Sosei Heptares Zoom Webinar

• November 15 - 17, 2023 | MPGPCR Conference

• November 20 - 23, 2023 | ASCEPT Annual Scientific Meeting

• February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition

• March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar

• March 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference

• April 5 - 10, 2024 | AACR Annual Meeting

• May 13 - 17, 2024 | 20th Annual PEGS Boston Summit

• May 16 - 19, 2024 | ASPET 2024

• May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition

• June 2 - 7, 2024 | Chemotactic Cytokines

GPCR Jobs

• NEW Research Scientist/Postdoctoral Associate in Computational Chemistry/Biophysics

• NEW Post-Doctoral Associate

• NEW Team Leader Antibody Discovery

• Staff Scientist (AC-TAP) in Database Development at Department of Drug Design and Pharmacology Faculty of Health and Medical Sciences

• Octant Apprentice

• Head of Human Resource Business Partners

• Senior Scientist, In vitro pharmacology - Crinetics Pharmaceuticals

• Senior Director, In vitro pharmacology - Crinetics Pharmaceuticals

Explore Dr. GPCR Ecosystem