📰 GPCR Weekly News

Hello Readers👋,

Happy New Year! We're excited to be back and share our weekly newsletter! We'll be sending it directly to your inbox every week, so you'll always be the first to know about the latest GPCR news.

Below is your Classified GPCR News at a glance for December 19th to January 1st, 2023.

GPCR Activation and Signaling

• Transactivation of receptor tyrosine kinases by purinergic P2Y and adenosine receptors.

• Ligand recognition and activation of neuromedin U receptor 2.

• Biased agonists differentially modulate the receptor conformation ensembles in Angiotensin II type 1 receptor.

• Unusual phototransduction via cross-motif signaling from Gq to adenylyl cyclase in intrinsically photosensitive retinalganglion cells.

GPCR Binders, Drugs, and more

• Engineered Human Antibody with Improved Endothelin Receptor Type A Binding Affinity, Developability, and Serum Persistence Exhibits Excellent Antitumor Potency.

• Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility disorders.

• Characterization of a novel positive allosteric modulator of the α1A-Adrenergic receptor.

GPCRs in Cardiology, Endocrinology, and Taste

• Metabolic depletion of sphingolipids inhibits agonist-induced endocytosis of the serotonin1A receptor.

GPCRs in Neuroscience

• Role of G-Proteins and GPCR-Mediated Signalling in Neuropathophysiology.

GPCRs in Oncology and Immunology

• Clinical, pathophysiologic, genetic and therapeutic progress in Primary Bilateral Macronodular Adrenal Hyperplasia.

• GPR4 in the pH-dependent migration of melanoma cells in the tumor microenvironment.

• Increased protease-activated receptor 1 autoantibodies are associated with severe COVID-19.

• Functional Assessment of Cancer-Linked Mutations in Sensitive Regions of Regulators of G Protein Signaling Predicted by Three-Dimensional Missense Tolerance Ratio Analysis.

• Deletion of macrophage Gpr101 disrupts their phenotype and function dysregulating host immune responses in sterile and infectious inflammation.

Methods & Updates in GPCR Research

• Quantitation of Plasma Membrane (G Protein-Coupled) Receptor Trafficking in Cultured Cells.

• A robust antibody discovery platform for difficult-to-express G protein-coupled receptors.

Reviews, GPCRs, and more

• Species dependence of A3 adenosine receptor pharmacology and function.

• Transcriptome profiling of male and female Ascaris lumbricoides reproductive tissues.

• Genetic Code Expansion To Enable Site-Specific Bioorthogonal Labeling of Functional G Protein-Coupled Receptors in Live Cells.

• Functional expression of oxytocin receptors in pulp-dentin complex.

• Ghrelin receptor signaling in health and disease: a biased view.

• Identification and expression analysis of G protein-coupled receptors in the cotton aphid, Aphis gossypii Glover.

Structural and Molecular Insights into GPCR Function

• Global insights into the fine tuning of human A2AAR conformational dynamics in a ternary complex with an engineered G protein viewed by NMR.

• Fusarium graminearum Ste3 G-Protein Coupled Receptor: A Mediator of Hyphal Chemotropism and Pathogenesis.

• Middle-Down Mass Spectrometry Reveals Activity-Modifying Phosphorylation Barcode in a Class C G Protein-Coupled Receptor.

• New insights into the structure and function of class B1 GPCRs.

• Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P2 Lipids.

• Tracking N- and C-termini of C. elegans polycystin-1 reveals their distinct targeting requirements and functions in cilia and extracellular vesicles.

• Identification of a potential structure-based GPCR drug for interstitial cystitis/bladder pain syndrome: in silico protein structure analysis and molecular docking.

• Non-ionic cholesterol-based additives for the stabilization of membrane proteins.

• "Structural Clarity is Brought to Adhesion G protein Coupled Receptor Tethered Agonism".

• Surveying nonvisual arrestins reveals allosteric interactions between functional sites.

• Evaluating GPCR modeling and docking strategies in the era of deep learning-based protein structure prediction.

Industry News

• Sosei Heptares and Neurocrine Biosciences won Out-Licensing Deal of the Year from Locust Walk

• Omass Therapeutics 2022 Review

• Sosei hooks millions from Eli Lilly alliance

• Septerna was selected as one of the Top Life Sciences Startups to Watch in 2023 by BioSpace

• Sosei Heptares Notes its Partner Tempero Bio has Received FDA Clearance to Advance Clinical Development of TMP-301 for Treatment of Alcohol and Substance Use Disorders

• AbbVie recruits a GPCR team in Oxford, buying out a fledgling biotech for $255M+

• Domain Therapeutics announces first patient dosed with DT-9081 in phase I clinical study in patients with advanced, recurrent or metastatic solid tumors: the EPRAD study

Call for GPCR Papers

• GPCRs: Signal Transduction. Deadline February 12, 2023

• Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology. Deadline January 30, 2023.

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.

Explore Dr. GPCR Ecosystem