Unlocking the Future of Medicine: Advancements in GPCR Research

📰 GPCR Weekly News, July 15 to 21, 2024

Hey everyone! Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just for you!

This week's highlight includes congrats to

• Omolade Otun, Chris de Graaf, Cherine Bechara, et al. for their work on Conformational dynamics underlying atypical chemokine receptor 3 activation 
  

• Michael Trogdon, J Silvio Gutkind, Edward C Stites, et al., for their study on Systems modeling of oncogenic G-protein and GPCR signaling reveals unexpected differences in downstream pathway activation
  

• Chiara D Mancinelli, Joshua Levitz, David Eliezer, et al. for their research on Control of G protein-coupled receptor function via membrane-interacting intrinsically disordered C-terminal domains

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Dr. GPCR University

Exciting news! We are pleased to announce the scheduled dates for our highly anticipated courses led by Dr. Terry Kenakin. As of July 31st, early-bird registration for our premium Ecosystem members will begin, allowing you to benefit from this exclusive discount. Be sure to mark your calendars and secure your spot for this extraordinary learning opportunity!

Course Schedule and Details

Every Thursday at 10 am EST

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

Dates: September 5th to 26th, 2024

Registrants will learn:

• Essentials of measuring pharmacologic activity of ligands (affinity, efficacy, co-operativity).

• Application of this knowledge to determine the mechanism of action of new GPCR ligands.

• The required elements of a comprehensive and effective GPCR Discovery.

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

Dates: October 3rd to 31st, 2024

Registrants will learn:

• The powerful applications of new cellular assays to determine GPCR ligand behavior in different functional systems.

• Understanding real-time kinetics to predict activity and in vivo target coverage.

• New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and signaling, location bias, signaling bias).

GPCR Event Highlight

Get ready for the 11th Adhesion GPCR Workshop!

Hosted by the Adhesion GPCR Consortium, this exciting event will occur in lively and culturally rich Mexico City from October 23 to 25, 2024. It is an opportunity to connect with like-minded scientists and researchers and gain valuable insights into the latest developments in adhesion GPCR biology.

Take advantage of the chance to showcase your creativity by participating in the Logo Contest. Submit your design by August 15, 2024, and stand a chance to have your creation represent this prestigious event.

Are you interested in becoming a sponsor?

Take advantage of the sponsorship opportunities and elevate your brand's presence at this crucial scientific gathering. Feel free to reach out to us at Hello@DrGPCR.com.

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 Let’s dive into the Classified GPCR News from July 15th to 21st, 2024

GPCR Activation and Signaling

• Conformational dynamics underlying atypical chemokine receptor 3 activation

• RhoA-mediated G12-G13 signaling maintains muscle stem cell quiescence and prevents stem cell loss

• Activation of Polycystin-1 Signaling by Binding of Stalk-derived Peptide Agonists

GPCR Binders, Drugs, and more

• In silico exploration of 4(α-l-rhamnosyloxy)-benzyl isothiocyanate: A promising phytochemical-based drug discovery approach for combating multi-drug resistant Staphylococcus aureus

• Isolation, Structure Elucidation, and Biological Activity of the Selective TACR2 Antagonist Tumonolide and its Aldehyde from a Marine Cyanobacterium

• Fluorophore-Labeled Pyrrolones Targeting the Intracellular Allosteric Binding Site of the Chemokine Receptor CCR1

GPCRs in Cardiology, Endocrinology, and Taste

• GPCR-mediated regulation of beige adipocyte formation: Implications for obesity and metabolic health

GPCRs in Neuroscience

• Chronic modulation of cAMP signaling elicits synaptic scaling irrespective of activity

• Neuronal GPCR NMUR-1 regulates energy homeostasis in response to pathogen infection

GPCRs in Oncology and Immunology

• Systems modeling of oncogenic G-protein and GPCR signaling reveals unexpected differences in downstream pathway activation

Methods & Updates in GPCR Research

• A combination treatment based on drug repurposing demonstrates mutation-agnostic efficacy in pre-clinical retinopathy models

Reviews, GPCRs, and more

• Lessons from the physiological role of guanosine in neurodegeneration and cancer: Toward a multimodal mechanism of action?

Structural and Molecular Insights into GPCR Function

• Entropy drives the ligand recognition in G-protein-coupled receptor subtypes

• Structural insights into ligand recognition, selectivity, and activation of bombesin receptor subtype-3

• Control of G protein-coupled receptor function via membrane-interacting intrinsically disordered C-terminal domains

Industry News

• Novartis continues to deliver strong sales growth and core margin expansion in Q2; raises FY 2024 bottom-line guidance 

• Crinetics Pharmaceuticals to Report Second Quarter 2024 Financial Results on August 8, 2024

• Dynamic nature of G-protein coupled receptors

• Septerna Secures $150 Million in Series B Financing to Advance Pipeline of Novel GPCR-targeted Medicines
  

GPCR Events, Meetings, and Webinars

• NEW November 5 - 7, 2024 | 16th Annual PEGS Europe 

• 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

GPCR Jobs

• NEW Senior or Lead Researcher 

• NEW Senior Scientist, Cryo-Electron Microscopy 

• Postdoctoral Research Associate

• Senior Scientist - Discovery Biotherapeutics

• Post-Doctoral Fellow/Trainee

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

Join the Dr. GPCR Ecosystem