📰 GPCR Weekly News, January 30 to February 5, 2023

Hello Readers👋,

We're excited to share our weekly newsletter with you. Keep up-to-date with the latest research and advancements in the field with our convenient, weekly news delivered to your inbox. You can always adjust your email preferences in your account settings. For Dr. GPCR News, please subscribe to your monthly newsletter.

Below is your Classified GPCR News at a glance for January 30th to February 5th, 2023.

GPCR Activation and Signaling

• The dual-function chemokine receptor CCR2 drives migration and chemokine scavenging through distinct mechanisms.

• Cannabinoid 1 (CB1 ) receptor arrestin subtype-selectivity and phosphorylation dependence.

• Metabolic depletion of sphingolipids inhibits agonist-induced endocytosis of the serotonin1A receptor.

• Genetic code expansion to enable site-specific bioorthogonal labeling of functional G protein-coupled receptors in live cells.

• Platelet P2Y1 receptor exhibits constitutive G protein signaling and β-arrestin 2 recruitment.

• Multiple Potassium Channel Tetramerization Domain (KCTD) family members interact with Gβγ, with effects on cAMP signaling.

GPCR Binders, Drugs, and more

• Ligands selectively tune the local and global motions of neurotensin receptor 1 (NTS1).

• Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139.

• Valorization of leftover green tea residues through conversion to bioactive peptides using probiotics-aided anaerobic digestion.

• Comparative evaluation of biased agonists Sarcosine1 , d-Alanine8 -Angiotensin (Ang) II (SD Ang II) and Sarcosine1 , Isoleucine8 -Ang II (SI Ang II) and their radioiodinated congeners binding to rat liver membrane AT1 receptors.

GPCRs in Cardiology, Endocrinology, and Taste

• Receptor autoantibodies: Associations with cardiac markers, histology, and function in human non-ischaemic heart failure.

GPCRs in Oncology and Immunology

• LP2, a cyclic angiotensin-(1-7) analog extended with an N-terminal D-lysine, impairs growth of patient-derived xenografts of colorectal carcinoma in mice.

• Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration.

Methods & Updates in GPCR Research

• Deep-Learning-Enhanced Diffusion Imaging Assay for Resolving Local-Density Effects on Membrane Receptors.

• Computational investigation of functional water molecules in GPCRs bound to G protein or arrestin.

• Functional expression of oxytocin receptors in pulp-dentin complex.

Reviews, GPCRs, and more

• Understanding Neuropeptide Transmission in the Brain by Optical Uncaging and Release.

• Patching holes in the mechanism of opioid tolerance.

• Non-canonical Golgi-compartmentalized Gβγ signaling: mechanisms, functions, and therapeutic targets.

• β-arrestins and G protein-coupled receptor kinases in viral entry: A graphical review.

• Development and challenges in the discovery of 5-HT1A and 5-HT7 receptor ligands.

• Involvement of SAP97 anchored multiprotein complexes in regulating cardiorenal signaling and trafficking networks.

• The chemokines CXCL8 and CXCL12: molecular and functional properties, role in disease and efforts towards pharmacological intervention.

• The Memory Orchestra: Contribution of Astrocytes.

Structural and Molecular Insights into GPCR Function

• Structural view of G protein-coupled receptor signaling in the retinal rod outer segment.

• Cryo-EM structure of orphan G protein-coupled receptor GPR21.

Industry News

• Exscientia Announces First-in-Human Study for Bristol Myers Squibb In-Licensed PKC Theta Inhibitor, EXS4318

• GPCR Therapeutics Announces Launch of US Phase 2 Trial of GPC-100 in Multiple Myeloma

• Behind Friday's $161M IPO: A star scientist, GPCR drug discovery and a plan to challenge pharma in diabetes

• TGA’s approval of MDMA and Psilocybin for medical use is a result of ‘renewed interest’

• Addex Strategic Partner Completes Enrollment In Adx71149 Epilepsy Phase 2 Study Part 1

• Domain Therapeutics to Participate in Upcoming Investor and Industry Conferences

• International Day of Women and Girls in Science

• Orion Biotechnology Publishes Whitepaper Highlighting the Importance and Challenges in Unlocking “Undruggable” GPCRs

• Endocrine Society Awards Baxter Prize to Innovator in Endocrine Drug Discovery

• Upstream Bio Announces the Appointment of Marcella Ruddy, M.D., to the Board of Directors

Call for GPCR Papers

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

GPCR Events, Meetings, and Webinars

• 2nd GPCR-Targeted Drug Discovery Summit, (February 21 - 23, 2023), Boston.

• SLAS2023 International Conference and Exhibition (February 25 - March 1, 2023).

• 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 B

• uilding 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

• 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)

• Post-Doctoral Research Assistant

• Research Fellow - School of Physics and Astronomy

• Postdoctoral Research Associate (Fixed Term)

Explore Dr. GPCR Ecosystem