📰 GPCR Weekly News, May 27 to June 2, 2024

Hello everyone!

Take a moment to browse our latest coverage of GPCRs this week, featuring 24 insightful research papers and industry updates. Stay informed with the most recent developments in GPCR research and industry news.

This week's highlight includes congrats to:

• Inês Pinheiro, for her Dr. GPCR contributor article Canonical chemokine receptors as scavenging “decoys”
  

• Shivani Sachdev, Brendan Creemer, Thomas Gardella, and Ross Cheloha for their work on Highly biased agonism for GPCR ligands via nanobody tethering
  

• Elk Kossatz, Michel Bouvier, Jana Selent, et al. for their study on G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related effects and memory deficits

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Dr. GPCR University

We are excited to announce that Dr. Terry Kenakin will return for two consecutive courses in September and October 2024. More details will be shared soon, and registration will open in July 2024.

Dr. GPCR Podcast

Episode 154 of the Dr. GPCR Podcast on Self-Learning, Collaboration, and Delegation in Science with Dr. Badr Sokrat is live! You can now watch podcast episodes in video format on our website. Catch up on missed episodes and enjoy the visual experience!

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GPCR Event Highlight

We are excited to announce our first in-person event in collaboration with the Adhesion GPCR Consortium: The 11th Adhesion GPCR Workshop will take place in vibrant Mexico City from October 23 to 25, 2024.

Join the global GPCR community to share your research—submit your abstract using this form.

We are also offering sponsorship opportunities for this exciting event, which unites scientists worldwide to explore all aspects of adhesion GPCR biology. Interested in sponsoring? Please email us at Hello@DrGPCR.com.

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Let’s dive into the Classified GPCR News from May 27th to June 2nd, 2024.

GPCR Activation and Signaling

• Highly biased agonism for GPCR ligands via nanobody tethering

• Mechanistic insights into G-protein activation via phosphorylation mediated non-canonical pathway

• GPCR Screening Reveals that the Metabolite Receptor HCAR3 Regulates Epithelial Proliferation, Migration, and Cellular Respiration

• G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related effects and memory deficits

GPCRs in Cardiology, Endocrinology, and Taste

• The full-length TSH receptor is stabilized by TSH ligand

• Cardiomyocyte-specific overexpression of GPR22 ameliorates cardiac injury in mice with acute myocardial infarction

GPCRs in Neuroscience

• Voltage tunes mGlu5 receptor function, impacting synaptic transmission

• Orphan receptor GPR88 as a potential therapeutic target for CNS disorders - an in silico approach

• GRN knockdown regulates the expression and alternative splicing of genes associated with aphasia-related diseases in PC12 cells

• 17-β-estradiol potentiates the neurotrophic and neuroprotective effects mediated by the dopamine D3/acetylcholine nicotinic receptor heteromer in dopaminergic neurons

• A new GRAB sensor reveals differences in the dynamics and molecular regulation between neuropeptide and neurotransmitter release

GPCRs in Oncology and Immunology

• Neurotoxicity and accumulation of CPPD quinone at environmentally relevant concentrations in Caenorhabditis elegans

• Comparison of infectious complications with BCMA-directed therapies in multiple myeloma

• Glucose and HODEs regulate Aspergillus ochraceus quorum sensing through the GprC-AcyA pathway

• Deciphering the genetic landscape of lumpy skin disease: Unraveling variable virulence through comprehensive genome sequence analysis in India

Methods & Updates in GPCR Research

• Engineering G protein-coupled receptors for stabilization

• Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism

• Chemogenetic Signaling in Space and Time: Considerations for Designing Neuroscience Experiments Using DREADDs

Reviews, GPCRs, and more

• ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

• Why classical receptor theory, which ignores allostery, can effectively measure the strength of an allosteric effect as agonist's efficacy

• Single transmembrane GPCR modulating proteins: neither single nor simple

Structural and Molecular Insights into GPCR Function

• Insights on the G protein-coupled receptor helix 8 solution structure and orientation using a neurotensin receptor 1 peptide

• Illuminating the neuropeptide Y4 receptor and its ligand pancreatic polypeptide from a structural, functional, and therapeutic perspective

• Structural basis for selectivity and antagonism in extracellular GPCR-nanobodies

Industry News

• Structure Therapeutics Reports Positive Topline Data from its Phase 2a Obesity Study and Capsule to Tablet PK Study for its Oral Non-Peptide Small Molecule GLP-1 Receptor Agonist GSBR-1290

• Crinetics Pharmaceuticals Appoints Robert M. Cuddihy, M.D., as Senior Vice President of Medical Affairs

• Septerna to Participate in the Jefferies Global Healthcare Conference

• Crinetics Announces Positive Initial Findings At Endo 2024 For Atumelnant In Two Ongoing, Open-Label Studies For The Treatment Of Congenital Adrenal Hyperplasia (CAH) And Acth-Dependent Cushing’s Syndrome (ADCS)

• Nxera Pharma to Receive $4.6 Million in Milestone Payments from Centessa Pharmaceuticals
  

• CB1 receptor inverse agonist improves lung functioning in preclinical asthma
  

GPCR Events, Meetings, and Webinars

• June 2 - 7, 2024 | Chemotactic Cytokines

• June 4, 2024 | Live Webinar ‘It All Starts With a Protein – Protein Sciences as a Key to Success in Drug Discovery’ 

• June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling Networks

• June 25 - 29, 2024 | FENS Forum 2024

• October 2024 | Biologics US 2024 

• October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry

• October 23 - 25, 2024 | 11th Adhesion GPCR Workshop

• July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026

GPCR Jobs

• HIGHLIGHT Principal Scientist, In vitro pharmacology 

• Senior Scientist - Receptor Pharmacology

• PostDoctoral Scientist

• Senior Research Associate/Associate Scientist, Protein Science

• Post-Doctoral Fellow—Pharmacology/Cell Biology/Biochemistry

• Post Doctoral Fellow

• Postdoc Position

Join Dr. GPCR Ecosystem