📰 GPCR Weekly News, February 20 to 26, 2023

Hello Readers👋,

Thank you for joining us this week. Each week on Thursday, you receive informative and exciting news about GPCRs. And don't forget, for Dr. GPCR news content, make sure to subscribe to our monthly newsletter for Dr. GPCR News.

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Below is your Classified GPCR News at a glance for February 20th to 26th, 2023.

GPCR Activation and Signaling

• Coupling between GPR143 and dopamine D2 receptor is required for selective potentiation of dopamine D2 receptor function by L-3,4-dihydroxyphenylalanine in the dorsal striatum.

• All-Atom Molecular Dynamics Simulations Indicated the Involvement of a Conserved Polar Signaling Channel in the Activation Mechanism of the Type I Cannabinoid Receptor.

• Allosteric modulation of conserved motifs and helices in 5HT2BR: Advances drug discovery and therapeutic approach towards drug resistant epilepsy.

• Molecular basis for differential activation of p101 and p84 complexes of PI3Kγ by Ras and GPCRs.

• Impact of membrane lipid polyunsaturation on dopamine D2 receptor ligand binding and signaling

GPCR Binders, Drugs, and more

• Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.

• Small-molecule targeting of GPCR-independent non-canonical G protein signaling inhibits cancer progression.

• Application of computational methods for class A GPCR Ligand discovery.

• Gαi-derived peptide binds the µ-opioid receptor.

GPCRs in Cardiology, Endocrinology, and Taste

• α1-Adrenergic Receptors: Insights into Potential Therapeutic Opportunities for COVID-19, Heart Failure, and Alzheimer's Disease.

• Gβγ subunits co-localize with RNA polymerase II and regulate transcription in cardiac fibroblasts.

• Slow-rising and fast-falling dopaminergic dynamics jointly adjust negative prediction error in the ventral striatum.

Methods & Updates in GPCR Research

• GPCRLigNet: rapid screening for GPCR active ligands using machine learning.

• A robust approach for MicroED sample preparation of lipidic cubic phase embedded membrane protein crystals.

Reviews, GPCRs, and more

• Cell-trafficking impairment in disease-associated LPA6 missense mutants and a potential pharmacoperone therapy for autosomal recessive woolly hair/hypotrichosis.

Structural and Molecular Insights into GPCR Function

• Structure-based design of novel melanin-concentrating hormone receptor-1 ligands based on saturated nitrogen-containing heterocycles.

Industry News

• Josephine (Pina) Cardarelli from GPCR Therapeutics on Beyond Biotech Podcast

• Crinetics Pharmaceuticals Reports Fourth Quarter And Full Year 2022 Financial Results And Provides Corporate Update

• Alastair Brown from Sosei Heptares, will present at the 18th Annual Biomarkers Congress.

• A growing understanding of the role of muscarinic receptors in the molecular pathology and treatment of schizophrenia

Call for GPCR Papers

• GPCRs: Signal Transduction. Deadline extended to March 31st, 2023.

GPCR Events, Meetings, and Webinars

• 2nd ERNEST Training School. (February 20 - March 3, 2023).

• WEBINAR Using integrative biophysical approaches to understand GPCR regulation by β-arrestins. (March 2, 2023)

• GEM2023. (March 14-17, 2023).

• SLAS 2023 Building Biology in 3D Symposium. (April 20 - 21, 2023)

• SLAS Europe 2023 Conference and Exhibition. (May 22 - 26, 2023)

• 2nd LEAPS Meets Life Sciences Conference. (May 14 - 19, 2023)

• 8th and final ERNEST Meeting in Crete. (May 3 - 7, 2023).

• 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).

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

GPCR Jobs

• PhD Studentship - Integrated Approaches In Pharmacology, Computer Simulations And Machine Learning To Predict Ligand Signaling Pathways Via The Anti-Inflammatory Receptor Gpr84

• PhD Studentship - Insight Into The Neuroprotective Function Of The Prostaglandin Receptor Ep2

• Computational drug design PhD student at the Department of Drug Design and Pharmacology

• Computational drug design postdoc at the Department of Drug Design and Pharmacology

• Software / database development PhD student at Department of Drug Design and Pharmacology

• Software / database development postdoc at the Department of Drug Design and Pharmacology

• Postdoc in Bioinformatics/Data Science at Department of Drug Design and Pharmacology

• Scientist/Senior Scientist (Research Software Engineer)

• Senior Scientist – Native Mass Spectrometry

• Speculative Applications (Protein Biochemistry)

• Speculative Applications (Mass Spectrometry)

• Speculative Applications (Chemistry)

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