📰 GPCR Weekly News, June 24 to 30, 2024

Hello everyone! We have gathered 24 new research papers on GPCRs and updates on industry news related to GPCRs.

This week's highlight includes congrats to:

• Drs. Bryan Roth and Brian Krumm for their study on Molecular glues as potential GPCR therapeutics
  

• Drs. András Tóth, László Hunyady, et al. for their work on G protein-coupled receptor endocytosis generates spatiotemporal bias in β-arrestin signaling
  

• Drs. Kawthar Belkacemi, Philippe Rondard, Jean-Philippe Pin, and Laurent Prézeau, for their research on Heterodimers revolutionize the field of metabotropic glutamate receptors
  

• Kara Anazia, Dr. Matthew Eddy, et al. for their investigation on Interaction Networks within Disease-Associated GαS Variants Characterized by an Integrative Biophysical Approach 

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Dr. GPCR University

We're thrilled to announce that Dr. Terry Kenakin will lead two brand-new, back-to-back courses tailored for the Dr. GPCR Ecosystem this fall. Mark your calendars for September and October 2024, and stay tuned for registration details coming this month. These online courses will be held on Thursdays at 10 am EST. Save the dates:

• Course 1: Strategies for Successful Lead Optimization of Candidate Molecules Dates: September 5th to 26th, 2024
  

• Course 2: Advanced Methods for the Optimization of Candidate Selection Dates: October 3rd to 31st, 2024

GPCR Event Highlight

Join us for an in-person event with the Adhesion GPCR Consortium: the 11th Adhesion GPCR Workshop, which will be held in vibrant Mexico City from October 23 to 25, 2024. This key event will delve into adhesion GPCR Biology.

Important Deadlines:

• Abstract Submission: July 22, 2024. Submit your abstract today!
  

• Logo Contest: Unleash your creativity and submit your design by August 15th, 2024
  

Sponsorship Opportunities: Explore sponsorship options for this prestigious event. For more information, contact us at Hello@DrGPCR.com. 

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 Let’s dive into the Classified GPCR News from June 24th to 30th, 2024

Adhesion GPCRs

• Novel Isoforms of Adhesion G Protein-Coupled Receptor B1 (ADGRB1/BAI1) Generated from an Alternative Promoter in Intron 17

• The adhesion-GPCR ADGRF5 fuels breast cancer progression by suppressing the MMP8-mediated antitumorigenic effects

• GPR56: A potential therapeutic target for neurological and psychiatric disorders

GPCR Activation and Signaling

• Molecular basis for the activation of PAF receptor by PAF

• Heterodimers revolutionize the field of metabotropic glutamate receptors

• Molecular Basis of MC1R Activation: Mutation-Induced Alterations in Structural Dynamics

• Structural insights into ligand recognition and activation of the succinate receptor SUCNR1

• G protein-coupled receptor endocytosis generates spatiotemporal bias in β-arrestin signaling

• Interaction Networks within Disease-Associated GαS Variants Characterized by an Integrative Biophysical Approach

• Redox-modulated SNX25 as a novel regulator of GPCR-G protein signaling from endosomes

• Cellular lipids regulate the conformational ensembles of the disordered intracellular loop 3 in β2-adrenergic receptor

• Extensive location bias of the GPCR-dependent translatome via site-selective activation of mTOR

GPCR Binders, Drugs, and more

• Molecular glues as potential GPCR therapeutics

• A high-affinity, cis-on photoswitchable beta blocker to optically control β2-adrenergic receptors in vitro and in vivo

GPCRs in Neuroscience

• Elucidating the activation mechanism of the proton-sensing GPR68 receptor

• Astrocytic GPCR signaling in the anterior cingulate cortex modulates decision making in rats

• Translation-independent association of mRNAs encoding protomers of the 5-HT 2A -mGlu2 receptor complex in living cells

GPCRs in Oncology and Immunology

• Metabolic crosstalk: Extracellular ATP and the tumor microenvironment in cancer progression and therapy

• Agonists of galanin subtype 2 receptor may prevent pancreatic cancer and agonists of angiotensin II type 2 receptor may prevent colorectal cancer

• Distinct Activation Mechanisms of CXCR4 and ACKR3 Revealed by Single-Molecule Analysis of their Conformational Landscapes

Methods & Updates in GPCR Research

• Protocol to visualize and quantify the COPII concentration and anterograde transport of nascent G protein-coupled receptors

• Effects of an external static EF on the conformational transition of 5-HT1A receptor: A molecular dynamics simulation study

• Monitoring norepinephrine release in vivo using next-generation GRABNE sensors

Structural and Molecular Insights into GPCR Function

• Structural basis for hormone recognition and distinctive Gq protein coupling by the kisspeptin receptor

Industry News

• Nxera Pharma Receives US$10 Million from AbbVie as Collaboration Targeting Neurological Diseases Achieves First R&D Milestone

• Tectonic bets on GPCR heart failure drug following reverse merger with Avrobio

• Lilly signs $140M upfront partnership with Radionetics in latest radiopharma play 

GPCR Events, Meetings, and Webinars

• September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery

• 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

• NEW Scientist; Biochemistry, Cellular and Mechanistic Pharmacology; Lead Discovery and Optimization 

• NEW Director/Sr. Director GPCR Drug Discovery Biologist 

• HIGHLIGHT Principal Scientist, In vitro pharmacology 

• Post-Doctoral Scientist- Molecular Pharmacology (FDE)

• Research Assistant 

• Senior Scientist - Receptor Pharmacology

• Postdoctoral Scientist

Join Dr. GPCR Ecosystem