GPCR Weekly Whirlwind: Top Receptor Highlights from Sep 30 - Oct 6, 2024!

Hey there, GPCR Enthusiasts!

Are you geared up for your GPCR fix of the day? Get ready to dive into some discoveries and mind-blowing breakthroughs with us!

This Week’s Highlights:

Congrats to:

• Our contributor, Cam Sinh Lu, who has just released an incredible article on our site and a GPCR Paper with his team:

  • Targeted Drug Design through GPCR Mutagenesis: Insights from β2AR

    
    

• China M Payne, Cam Sinh Lu, Karen Gregory, Lauren May, Andrea Vernall, et al. for their fantastic paper on Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor

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

• Sabrina Rahman, Arthur Christopoulos, Christopher Langmead, et al. for their outstanding work on Ligand-directed biased agonism at human histamine H3 receptor isoforms across Gαi/o- and β-arrestin2-mediated pathways

  
  

---

Get ready for the Second class of Principles of Pharmacology I

We are diving into the second class of our Principles of Pharmacology I course with enthusiasm and determination!

If you missed out on enrolling in this one, worry not – a spot is reserved just for you in Principles of Pharmacology II.

Secure your spot now for our next course. Seize this opportunity to enhance your expertise and proficiency in pharmacology! We close registrations in 2 weeks!!

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).

Modules:

• October 31st: The Eyes to See- The Importance of Pharmacologic Assays.

• November 7th: Drug Disposition in Physiological Tissues as a Therapeutic Variable.

• November 14th: The Application of GPCR Ligand Kinetics to Candidate Design.

• November 21st: Unconventional GPCR Ligands as Drugs.

• December 5th: Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit.

*Lessons are every Thursday at 10 AM EST.

---

📌 Reasons to Consider Enrolling Now:

Cost-effective and Unique Educational Opportunities

• Our courses offer affordability without compromising on quality.

Adaptable Learning Environment

• Benefit from the flexibility of accessing recorded sessions to deepen your comprehension.

Positive Feedback from Our Esteemed Students

• Past students highly recommend our programs, lauding the course content and the exceptional faculty members who adeptly simplify the intricacies of GPCR pharmacology for practical application in both academic and industrial research settings.

Save Your Spot Today!

---

Exclusive Deal for Scientists in Developing Nations

If you reside and work in a developing country, complete this form for free access to Dr. Kenakin's upcoming course. We aim to make education accessible to all!

Take action immediately to join our esteemed learning community!

---

GPCR Event Spotlight

11th Adhesion GPCR Workshop  

📍 Mexico City

📅 October 23 - 25, 2024

Hurry, there are only a couple of weeks left!

Act now to secure your spot, prepare to spark your passion, and interact with your exceptional peers to explore the latest advancements in adhesion GPCR biology!

🌟 Get ready - the full agenda is now available; check it HERE!

Are you ready to significantly boost your brand? Contact Hello@DrGPCR.com for exciting sponsorship opportunities. Let's elevate your brand together!

---

Classified GPCR News

 Let’s dive into the Classified GPCR News from September 30th to October 6th, 2024

Industry News

• Nxera Pharma appoints experienced commercial R&D executive Makoto Sugita as Chief Medical Officer and President of Nxera Pharma Japan

• Septerna files for IPO on strength of preclinical data, vision for expanding GPCR landscape

• The Royal Swedish Academy of Sciences has decided to award the Nobel Prize in Chemistry 2024

• Septerna Announces Initiation of Phase 1 Clinical Trial with SEP-786, a Novel Oral Small Molecule PTH1R Agonist for the Treatment of Hypoparathyroidism

• World first: Australian scientists uncover “plant-like” behavior in important human cell regulator, opening up a new drug target for cancer, other diseases

  
  

Call for GPCR Papers

• Deadline: Nov 1, 2024. Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology

GPCR Events, Meetings, and Webinars

• October 17, 2024 | Unprecedented fragment-based screening using Spectral Shift for GPCRs

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

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

• November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference

• November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe

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

GPCR Jobs

• HIGHLIGHT Research Associate - Professor Graeme Milligan

• HIGHLIGHT Postdoc in Molecular Pharmacology - The Hauser Group

• Postdoctoral Scholar – iPSC in cardiac and endothelial cell function

• Protein Biochemist/Structural Biologist

• Senior Scientist/Staff Scientist, Computational Chemistry

• Postdoc in GPCR mechanosensing 

• Postdoctoral Position

• Postdoctoral research position

GPCR Activation and Signaling

• Preassembly of specific Gβγ subunits at GABAB receptors through auxiliary KCTD proteins accelerates channel gating

• Ligand-directed biased agonism at human histamine H3 receptor isoforms across Gαi/o- and β-arrestin2-mediated pathways

• Postsynaptic Density Proteins and Their Role in the Trafficking of Group I Metabotropic Glutamate Receptors

• Dual regulation of IP3 receptors by IP3 and PIP2 controls the transition from local to global Ca2+ signals

• Coordinated cellular behavior regulated by epinephrine neurotransmitters in the nerveless placozoa

• Selective ligand recognition and activation of somatostatin receptors SSTR1 and SSTR3

• SPMs exert anti-inflammatory and pro-resolving effects through positive allosteric modulation of the prostaglandin EP4 receptor

GPCR Binders, Drugs, and more

• Molecular glues as potential GPCR therapeutics

• N-acyl glycines produced by commensal bacteria potentiate GLP-1 secretion as GPCR ligands

• Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor

GPCRs in Cardiology, Endocrinology, and Taste

• Ciliary localization of GPR75 promotes fat accumulation in mice

GPCRs in Neuroscience

• Diverse signaling mechanisms and heterogeneity of astrocyte reactivity in Alzheimer's disease

• Identification of immune-related hub genes in spinal cord injury
  

GPCRs in Oncology and Immunology

• Biochemical pharmacology of adenylyl cyclases in cancer

• Olfactory Receptors and Tumorigenesis: Implications for Diagnosis and Targeted Therapy

Methods & Updates in GPCR Research

• Protocol for detecting endogenous GPCR activity in primary cell cultures using ONE-GO biosensors

• Quantitation of F-actin in cytoskeletal reorganization: Context, methodology and implications

Structural and Molecular Insights into GPCR Function

• LYCHOS is a human hybrid of a plant-like PIN transporter and a GPCR

• Biochemical characterization of Prokineticin 2 binding to Prokineticin receptor 1 in zebrafish

• Coupling and Activation of the β1 Adrenergic Receptor - The Role of the Third Intracellular Loop

Become a Premium Member!

Get your 5-day free trial TODAY!