📰 GPCR Weekly News, May 22 to 28, 2023

Hi GPCR lovers👋, Ready for exciting news in the GPCR world? Read them below!

You can now watch the live talk recordings from the previous symposiums, check them out here.

Also, let's congratulate Lauri Urvas on his first first-author paper! Check out GPCR papers featuring Drs. Bryan Roth, Peter Gmeiner, and Thomas P. Sakmar this week.

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Below is your Classified GPCR News at a glance for May 22 to 28, 2023.

GPCR Activation and Signaling

• The adhesion GPCRs CELSR1-3 and LPHN3 engage G proteins via distinct activation mechanisms.

• Multiple Subthreshold GPCR Signals Combined by the G-Proteins Gαq and Gαs Activate the Caenorhabditis elegans Egg-Laying Muscles.

• Modulating GPCR and 14-3-3 protein interactions: prospects for CNS drug discovery.

GPCR Binders, Drugs, and more

• Design of Drug Efficacy Guided by Free Energy Simulations of the β2 -Adrenoceptor.

• Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells.

• Differential Responses of the GLP-1 and GLP-2 Receptors to N-Terminal Modification of a Dual Agonist.

GPCRs in Cardiology, Endocrinology, and Taste

• Pathophysiology and pharmacology of G protein-coupled receptors in the heart.

GPCRs in Neuroscience

• PACAP key interactions with PAC1, VPAC1, and VPAC2 identified by molecular dynamics simulations.

• Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief.

Structural and Molecular Insights into GPCR Function

• Cholesterol Biases the Conformational Landscape of the Chemokine Receptor CCR3: A MAS SSNMR-Filtered Molecular Dynamics Study.

• The intertwining roles of caveolin, oxytocin receptor, and the associated signalling pathways in prostate cancer progression.

• A key GPCR phosphorylation motif discovered in arrestin2⋅CCR5 phosphopeptide complexes.

• Divergent regulation of α-arrestin ARRDC3 function by ubiquitination.

• Molecular mechanism of fatty acid activation of FFAR1.

• Structural genomics of the human dopamine receptor system

• Structural Insights into Molecular Recognition and Receptor Activation in Chemokine–Chemokine Receptor Complexes

Industry News

• Mavorixafor reduces infection rates among patients with WHIM syndrome

• Bristol Myers Squibb’s Investigational LPA1 Antagonist Reduces the Rate of Lung Function Decline in Patients with Idiopathic Pulmonary Fibrosis

• Exscientia Business Update for First Quarter 2023

• Structure Therapeutics Initiates Phase 2a Study of Oral GLP-1 agonist GSBR-1290 for the Treatment of Type 2 Diabetes and Obesity

• Prof. Andrew Hopkins, Exscientia's CEO, will speak at the University of Chicago's Distinguished Seminar Series on Population and Precision Health next week.

• Your body naturally produces opioids without causing addiction or overdose – studying how this process works could help reduce the side effects of opioid drugs

GPCR Events, Meetings, and Webinars

• The Illuminating the Understudied Druggable Proteome Conference. (June 4 - 8, 2023).

• 2023 Molecular Pharmacology (GRS) Seminar GRC. (June 10 - 11, 2023).

• Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. (June 11 - 16, 2023).

• FREE Symposium - IPI Surfacing (June 15, 2023)

• NEW GPCRs in drug discovery: challenges & solutions (June 19 - 23, 2023)

• Training School on “Cell-based assays to study Adhesion GPCR function". (June 28 - 30, 2023)

• FREE 11th Adrenoceptor Symposium: Adrenoceptors and GPCR Signalling (June 30 - July 1, 2023)

• 19th World Congress of Basic & Clinical Pharmacology 2023. (July 2 - 7, 2023).

• 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023)

• NEW GPCR Retreat (November 2 - 4, 2023)

GPCR Jobs

• NEW Associate Director / Director, Clinical Operations

• Postdoctoral Research Associate

• Lab Manager

• Vice President, Medical Affairs

• Associate Scientist - Technology

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