📰 GPCR Weekly News, June 17 to 23, 2024

Greetings to all!

This Thursday, explore the latest content on GPCRs, which includes 29 informative research papers and industry news. Stay informed about the most recent developments in GPCR research and industry updates.

This week's highlight includes congrats to:

• Ya-Tzu Li for her contributor article titled Do You Believe AI Could Accelerate Drug Discovery?
  

• Shane Wright, Michel Bouvier, et al., for their work on Conformation- and activation-based BRET sensors differentially report on GPCR-G protein coupling
  

• Samuel Liu, Preston Anderson, Sudarshan Rajagopal, Robert Lefkowitz, Howard Rockman for their review G Protein-Coupled Receptors: A Century of Research and Discovery

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Dr. GPCR University

We are excited to announce that Dr. Terry Kenakin will conduct two back-to-back courses this fall. Save the September and October 2024 dates, and look for registration details in July. The two back-to-back courses are new and specially tailored to the Dr. GPCR Ecosystem and our community. The classes will be online Thursdays from 10 am EST.

Save the dates from September 5th to 26th, 2024, to learn about Strategies for Successful Lead Optimization of Candidate Molecules.

Save the dates from October 3rd to 31st, 2024, to learn more about the Advanced Methods for the Optimization of Candidate Selection.

GPCR Event Highlight

Join us for a special in-person event in collaboration with the Adhesion GPCR Consortium: The 11th Adhesion GPCR Workshop. This exciting event will occur in lively Mexico City from October 23 to 25, 2024, and will be a cornerstone for discussions in adhesion GPCR Biology.

• NEW DEADLINE July 22, 2024: Submit your abstract today!
  

• Logo Contest: Unleash your creativity by designing the event logo! Submit your entries by August 15th, 2024.
  

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

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  Let’s dive into the Classified GPCR News from June 17th to 23rd, 2024.

GPCR Activation and Signaling

• GPCR-dependent and -independent arrestin signaling

• Direct GPCR-EGFR interaction enables synergistic membrane-to-nucleus information transfer

• TMC6 functions as a GPCR-like receptor to sense noxious heat via Gαq signaling

• Exploring the Activation Mechanism of the GPR183 Receptor

GPCR Binders, Drugs, and more

• Target-based discovery of antagonists of the tick (Rhipicephalus microplus) kinin receptor identifies small molecules that inhibit midgut contractions

• Ligand-based analysis of the antifungal potential of phytosterols and triterpenes isolated from Cryptostegia grandiflora against Candida auris FKBP12

• Development and therapeutic perspectives of CXCR4 antagonists for disease therapy

GPCRs in Cardiology, Endocrinology, and Taste

• Transcriptomic profiling highlights cell proliferation in the progression of experimental pulmonary hypertension in rats

• Latrophilin-2 mediates fluid shear stress mechanotransduction at endothelial junctions

GPCRs in Neuroscience

• Male-specific behavioral and transcriptomic changes in aging C. elegans neurons

• Activation of Gs Signaling in Cortical Astrocytes Does Not Influence Formation of a Persistent Contextual Memory Engram

• β-arrestins are scaffolding proteins required for Shh-mediated axon guidance

GPCRs in Oncology and Immunology

• Regulator of G protein signaling 16 restrains apoptosis in colorectal cancer through disrupting TRAF6-TAB2-TAK1-JNK/p38 MAPK signaling

• Metallo-protease Peptidase M84 from Bacillusaltitudinis induces ROS-dependent apoptosis in ovarian cancer cells by targeting PAR-1

• G protein-coupled receptors related to autoimmunity in postural orthostatic tachycardia syndrome

• The binding mechanism of an anti-multiple myeloma antibody to the human GPRC5D homodimer

• Identification of a G-protein coupled receptor-related gene signature through bioinformatics analysis to construct a risk model for ovarian cancer prognosis

• GprC of the nematode-trapping fungus Arthrobotrys flagrans activates mitochondria and reprograms fungal cells for nematode hunting

• Role and recent progress of P2Y12 receptor in cancer development

• Mutation Patterns Predict Drug Sensitivity in Acute Myeloid Leukemia

Methods & Updates in GPCR Research

• The ufmylation cascade controls COPII recruitment, anterograde transport, and sorting of nascent GPCRs at ER

• Optical Control of TRPV1 Channels In Vitro with Tethered Photopharmacology

• Deuteration as a General Strategy to Enhance Azobenzene-Based Photopharmacology

• Optical Control of Cell-Surface and Endomembrane-Exclusive β-Adrenergic Receptor Signaling

• Conformation- and activation-based BRET sensors differentially report on GPCR-G protein coupling

Reviews, GPCRs, and more

• Proteome-wide analysis reveals G protein-coupled receptor-like proteins in rice (Oryza sativa)

• G Protein-Coupled Receptors: A Century of Research and Discovery

• Challenges and opportunities in cancer immunotherapy: a Society for Immunotherapy of Cancer (SITC) strategic vision

Structural and Molecular Insights into GPCR Function

• Structure and dynamics of the pyroglutamylated RF-amide peptide QRFP receptor GPR103

Industry News

• EY Announces Scott Struthers, Ph.D., CEO and Founder of Crinetics Pharmaceuticals, as an Entrepreneur Of The Year® 2024 Pacific Southwest Award Winner

• Monlunabant by Inversago Pharma for Metabolic Syndrome: Likelihood of Approval

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

• Addex Pharma unveils new mGlu7 receptor negative allosteric modulators

• Trevena Announces Preclinical TRV045 Data Providing Insight Into Novel Mechanism of Analgesic Effect in Chronic Neuropathic Pain Model and Demonstrating Statistically Significant Anti-Seizure Activity in Epilepsy Models

• Biophysicists decipher functionality of adrenaline-binding receptor

• Tectonic plates more than $130m in new funding and goes public

GPCR Events, Meetings, and Webinars

• NEW June 27, 2024 | FREE GPCR Forum ECI Zoominar

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

• June 25 - 29, 2024 | FENS Forum 2024

• NEW 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

• HIGHLIGHT Principal Scientist, In vitro pharmacology 

• NEW Post-Doctoral Scientist- Molecular Pharmacology (FDE)

• NEW Research Assistant 

• Senior Scientist - Receptor Pharmacology

• Postdoctoral Scientist

• Senior Research Associate/Associate Scientist, Protein Science

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

Join Dr. GPCR Ecosystem