📰 GPCR Weekly News, July 1 to 7, 2024

Hello everyone! 

Check out our latest collection of 25 cutting-edge research papers on GPCRs and exciting updates on industry news related to GPCRs!

This week's highlight includes congrats to

• Edda Matthees, Drs. Evi Kostenis, Carsten Hoffmann, et al., for their work on GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism
  

• Dr. Gunnar Schulte for his study on the International Union of Basic and Clinical Pharmacology. CXV: The Class F of G Protein-Coupled Receptors
  

• Yusman Manchanda, Dr. Alejandra Tomas, et al. for their research on Engineered mini-G proteins block the internalization of cognate GPCRs and disrupt downstream intracellular signaling
  

• Mónica Navarro-Sánchez, Drs. Ross Bathgate, Francisco Olucha-Bordonau, et al.  for their investigation on Modulation of contextual fear acquisition and extinction by acute and chronic relaxin-3 receptor (RXFP3) activation in the rat retrosplenial cortex
  

• Sarah Bernhard, Drs. Jianming Han, Tao Che for their analysis of GPCR-G protein selectivity revealed by structural pharmacology
  

• Yao Lu, Drs Christopher Langmead,  Gregory Stewart, et al. for their study on Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia

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Dr. GPCR University

The wait is finally over! We're thrilled to announce the dates for our upcoming courses led by the renowned Dr. Terry Kenakin. Mark your calendars because registration opens on July 18, 2024!

These engaging online courses will take place every Thursday at 10 am EST. Here’s a sneak peek at what you can expect:

Principles of Pharmacology in Drug Discovery I - Techniques for Effective Lead Optimization of Candidate Molecules

• Dates: September 5th to 26th, 2024

• Overview: GPCRs have been and arguably still are the most prolific and fertile therapeutic drug targets; this course describes the essential pharmacologic techniques and knowledge required to create a GPCR Target Program to discover new Drugs.

Principles of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate Selection

• Dates: October 3rd to 31st, 2024

• Overview: This course continues with the basics learned in Course 1 and extends the ideas to apply GPCR utilization in drug therapy. Specifically, the ideas discussed cover the complex pleiotropic behaviors of GPCRs and how these may be exploited for new drug discovery.

GPCR Event Highlight

Immerse yourself in the cutting-edge world of adhesion GPCR research at the highly anticipated 11th Adhesion GPCR Workshop, hosted by the Adhesion GPCR Consortium. Taking place in the vibrant setting of Mexico City, this face-to-face gathering scheduled for October 23 to 25, 2024, is poised to be a crucial meeting for scientists and researchers dedicated to the study of adhesion GPCR biology.

Important Deadlines:

• Abstract Submission: July 22, 2024. Submit your abstract today; you have less than two weeks!
  

• 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 July 1 to 7, 2024

GPCR Activation and Signaling

• GPCR-MAPK signaling pathways underpin fitness trade-offs in whitefly

• G protein-coupled receptor kinases in hypertension: physiology, pathogenesis, and therapeutic targets

• GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism

• The roles of RGS proteins in cardiometabolic disease

GPCR Binders, Drugs, and more

• Engineered mini-G proteins block the internalization of cognate GPCRs and disrupt downstream intracellular signaling

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

GPCRs in Cardiology, Endocrinology, and Taste

• Geosmin, a Food- and Water-Deteriorating Sesquiterpenoid and Ambivalent Semiochemical, Activates Evolutionary Conserved Receptor OR11A1

• Tongue-on-a-Chip: Parallel Recording of Sweet and Bitter Receptor Responses to Sequential Injections of Pure and Mixed Sweeteners

• GPCRs involved in metabolic diseases: pharmacotherapeutic development updates

• Targeting G protein-coupled receptors for heart failure treatment

• RAMP and MRAP accessory proteins have selective effects on expression and signalling of the CB1, CB2, GPR18 and GPR55 cannabinoid receptors

GPCRs in Neuroscience

• Neuron specific quantitation of Gαolf expression and signaling in murine brain tissue

• Modulation of contextual fear acquisition and extinction by acute and chronic relaxin-3 receptor (RXFP3) activation in the rat retrosplenial cortex

• Unveiling the therapeutic prospects of EGFR inhibition in rotenone-mediated parkinsonism in rats: Modulation of dopamine D3 receptor

• Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia

• Single nucleotide variations encoding missense mutations in G protein-coupled receptors may contribute to autism

GPCRs in Oncology and Immunology

• Emerging GPCR targets for AUD: Insights from preclinical studies

• CB2 stimulation of adipose resident ILC2s orchestrates immune balance and ameliorates type 2 diabetes mellitus

Methods & Updates in GPCR Research

• Computational modelling of dynamic cAMP responses to GPCR agonists for exploration of GLP-1R ligand effects in pancreatic β-cells and neurons

• The application of artificial intelligence to accelerate G protein-coupled receptor drug discovery

• The application of targeted protein degradation technologies to G protein-coupled receptors

• Unravelling G protein-coupled receptor signalling networks using global phosphoproteomics

Reviews, GPCRs, and more

• International Union of Basic and Clinical Pharmacology. CXV: The Class F of G Protein-Coupled Receptors

Structural and Molecular Insights into GPCR Function

• Cryo-EM advances in GPCR structure determination

• GPCR-G protein selectivity revealed by structural pharmacology

Industry News

• Neurocrine Biosciences Announces U.S. FDA Accepts New Drug Applications and Grants Priority Review for Crinecerfont for Pediatric and Adult Patients with CAH 

• adMare BioInnovations Expands with New Wet Laboratory Space in Vancouver 

• ThirtyFiveBio receives grant to continue work on GPR35 blockers 

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

• HIGHLIGHT Principal Scientist, In vitro pharmacology 

• NEW Senior Scientist - Discovery Biotherapeutics

• NEW Post-Doctoral Fellow/Trainee

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

• Director/Sr. Director GPCR Drug Discovery Biologist 

• Post-Doctoral Scientist- Molecular Pharmacology (FDE)

• Research Assistant  

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