📰 GPCR Weekly News, May 29 to June 4, 2023

Hello GPCR friends👋, Stay informed with the latest developments in GPCR research and industry news! Happy reading📚!

This week, we would like to highlight two new publications:

• Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics.

• Tagged for arrest: 'Barcode' determines receptor's fate.

Our next Dr. GPCR Symposium is coming up on July 21st on Structural and Molecular Insights on GPCR Activation. We are looking for speakers and poster presenters! If you'd like to showcase your work, please email us at Hello@DrGPCR.com. For more information, follow the Dr. GPCR News by subscribing to our monthly newsletter.

We look forward to seeing you in a few days at the Molecular Pharmacology GRC and the associated Molecular Pharmacology GRS in Switzerland. We would also like to take a moment to thank the organizers for inviting Dr. Yamina Berchiche, our founder.

Below is your Classified GPCR News at a glance for May 29th to June 4th, 2023.

GPCR Activation and Signaling

• Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief.

• Molecular mechanism of fatty acid activation of FFAR1.

• Conformational flexibility of β-arrestins - How these scaffolding proteins guide and transform the functionality of GPCRs.

• Gβγ signaling regulates microtubule-dependent control of Golgi integrity.

• Ligand-dependent intracellular trafficking of the G protein-coupled P2Y6 receptor.

GPCR Binders, Drugs, and more

• ACE2 Activation by Tripeptide IRW (Ile-Arg-Trp) Depends on the G Protein-Coupled Receptor 30 Signaling Cascade.

• Molecular insights into peptide agonist engagement with the PTH receptor.

• An Atomic Level Investigation of Sodium Ions Regulating Agonist and Antagonist Binding in the Active Site of a Novel Target 5HT2BR Against Drug-Resistant Epilepsy.

GPCRs in Cardiology, Endocrinology, and Taste

• GPR97 deficiency ameliorates renal interstitial fibrosis in mouse hypertensive nephropathy.

• Bitter Odorants and Odorous Bitters: Toxicity and Human TAS2R Targets.

GPCRs in Neuroscience

• DRD1 signaling modulates TrkB turnover and BDNF sensitivity in direct pathway striatal medium spiny neurons.

• The contribution of endocytosis to sensitization of nociceptors and synaptic transmission in nociceptive circuits.

• The crosstalk between 5-HT2AR and mGluR2 in schizophrenia.

GPCRs in Oncology and Immunology

• A2aR on lung adenocarcinoma cells: A novel target for cancer therapy via recruiting and regulating tumor-associated macrophages.

• Coronavirus Porcine Epidemic Diarrhea Virus Utilizes Chemokine Interleukin-8 to Facilitate Viral Replication by Regulating Ca2+ Flux.

• CircFKBP5 Suppresses Apoptosis and Inflammation and Promotes Osteogenic Differentiation.

• Transcriptomic analysis of human cytomegalovirus to survey the indirect effects on renal transplant recipients.

• Pharmacological inhibition of neuropeptide Y receptors Y1 and Y5 reduces hypoxic breast cancer migration, proliferation, and signaling.

Methods & Updates in GPCR Research

• Illuminating the brain-genetically encoded single wavelength fluorescent biosensors to unravel neurotransmitter dynamics.

• Activity Models of Key GPCR Families in the Central Nervous System: A Tool for Many Purposes.

• Structure-based pharmacophore modeling 1. Automated random pharmacophore model generation.

• NMR applications to GPCR recognition by peptide ligands.

• How can we improve the measurement of receptor signaling bias?

Reviews, GPCRs, and more

• Advancements in G protein-coupled receptor biosensors to study GPCR-G protein coupling.

• Application of computational methods for class A GPCR Ligand discovery.

• New paradigms in purinergic receptor ligand discovery.

• Targeting biased signaling by PAR1: function and molecular mechanism of parmodulins.

• Lysophosphatidic acid, a simple phospholipid with myriad functions.

Structural and Molecular Insights into GPCR Function

• Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics.

• The role of G protein conformation in receptor-G protein selectivity.

• Components of TOR and MAP kinase signaling control chemotropism and pathogenicity in the fungal pathogen Verticillium dahliae.

• New insights into GPCR coupling and dimerisation from cryo-EM structures.

• Computational insights into ligand-induced G protein and β-arrestin signaling of the dopamine D1 receptor.

• Understanding the Rhodopsin Worldview Through Atomic Force Microscopy (AFM): Structure, Stability, and Activity Studies.

• Scribble scrambles parathyroid hormone receptor interactions to regulate phosphate and vitamin D homeostasis.

Industry News

• Structure Therapeutics Announces Poster Presentations of its Oral GLP-1 Receptor Agonist GSBR-1290 at the American Diabetes Association 83rd Scientific Sessions

• Domain Therapeutics' Nomination of DT-9045: A Groundbreaking NAM for Immunooncology

• Structure Therapeutics to Present at Jefferies Healthcare Conference

• Tagged for arrest: “Barcode” determines receptor’s fate.

GPCR Events, Meetings, and Webinars

• FREE Symposium - IPI Surfacing (June 15, 2023)

• GPCRs in drug discovery: challenges & solutions (June 19 - 23, 2023)

• Training School on “Cell-based assays to study Adhesion GPCR function". (June 28 - 30, 2023)

• FREE 11th Adrenoceptor Symposium: Adrenoceptors and GPCR Signalling (June 30 - July 1, 2023)

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

• 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023)

• GPCR Retreat (November 2 - 4, 2023)

GPCR Jobs

• NEW Senior Vice President of Global Medical Affairs

• NEW Postdoctoral Position on Gliovascular Unit of Glioblastoma

• Associate Director / Director, Clinical Operations

• Postdoctoral Research Associate

• Lab Manager

• Vice President, Medical Affairs

Explore Dr. GPCR Ecosystem