📰 GPCR Weekly News, June 26 to July 2, 2023

Hey there, fellow GPCR enthusiasts! Let's gather 'round for our weekly dose of GPCR News.

Congratulations to our Dr. GPCR Partner, Domain Therapeutics, for their nomination of the best-in-class CCR8 antibody candidate, DT-7012.

Mark your calendars for July 21st, as the next Dr. GPCR Symposium on Structural and Molecular Insights on GPCR Activation is fast approaching!

The exciting news is that this Symposium will be a trainee day with a career panel. If you want to present a poster, all you have to do is fill out the submission form and submit a 1-minute abstract video. And don't forget to subscribe to Dr. GPCR Newsletter for updates!

Let's take a quick look at the weekly Classified GPCR News from June 26th to July 2nd, 2023.

Adhesion GPCRs

• A screen of pharmacologically active compounds to identify modulators of the Adgrg6/Gpr126 signalling pathway in zebrafish embryos.

GPCR Activation and Signaling

• Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion and activates G protein-coupled receptors with a different mechanism from the cis isomer.

• Carbon dioxide-induced decrease in extracellular pH enhances the production of extracellular matrix components by upregulating TGF-β1 expression via CREB activation in human dermal fibroblasts.

• Inverse agonism of lysophospholipids with cationic head groups at Gi-coupled receptor GPR82.

• A unique melanocortin-4-receptor signaling profile for obesity-associated constitutively active variants.

GPCRs in Cardiology, Endocrinology, and Taste

• Adipocyte G Protein-Coupled Receptors as Potential Targets for Novel Antidiabetic Drugs.

GPCRs in Neuroscience

• Fine-tuning GPCR-mediated neuromodulation by biasing signaling through different G protein subunits.

• Modulation of GPCR receptors common to gut inflammatory diseases and neuronal disorders, Alzheimer's and Parkinson's diseases as druggable targets through Withania somnifera bioactives: an in silico study.

• Asymmetric activation of dimeric GABAB and metabotropic glutamate receptors.

GPCRs in Oncology and Immunology

• Dynamic Phosphoproteomics of BRS3 Activation Reveals the Hippo Signaling Pathway for Cell Migration.

• High expression of GPR50 promotes the proliferation, migration and autophagy of hepatocellular carcinoma cells in vitro.

• Gi/o GPCRs drive the formation of actin-rich tunneling nanotubes in cancer cells via a Gβγ/PKCα/FARP1/Cdc42 axis.

• Comparative analysis of the occupancy of Histone H3 Lysine 4 methylation in the cells treated with TGFβ and Interferonγ.

• Esophageal and gastric cancer incidence trends in Golestan, Iran: An age-period-cohort analysis 2004 to 2018.

• Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells.

Methods & Updates in GPCR Research

• GPCRana: A web server for quantitative analysis of GPCR structures.

• Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes.

Reviews, GPCRs, and more

• Noncanonical Regulation of cAMP-Dependent Insulin Secretion and Its Implications in Type 2 Diabetes.

• G protein-coupled receptor-targeting antibody-drug conjugates: Current status and future directions.

• History and function of the lactate receptor GPR81/HCAR1 in the brain: a putative therapeutic target for the treatment of cerebral ischemia.

• Comparative analysis of adipokinetic hormones and their receptors in Blattodea reveals novel patterns of gene evolution.

• Internal and external modulation factors of the orexin system (REVIEW).

• G protein-coupled receptors as targets for transformative neuropsychiatric therapeutics.

• Multi-omics integration analysis of GPCRs in pan-cancer to uncover inter-omics relationships and potential driver genes.

Structural and Molecular Insights into GPCR Function

• Identification of a potential structure-based GPCR drug for interstitial cystitis/bladder pain syndrome: in silico protein structure analysis and molecular docking.

• Structure-based pharmacophore modeling 2. Developing a novel framework for structure-based pharmacophore model generation and selection.

Industry News

• Trevena Announces New Topline OLINVYK Data Highlighting Reduced Cost per Admission from ARTEMIS Real-World Outcomes Study.

• Sosei Heptares Doses First Subject in Phase I Trial with HTL0048149, a First-in-Class GPR52 Agonist for Schizophrenia.

• Domain Therapeutics announces nomination of best-in-class CCR8 antibody candidate, DT-7012, further strengthening its unique portfolio of GPCR-targeting immunotherapies.

GPCR Events, Meetings, and Webinars

• NEW ERNEST ECI Zoominar (July 6, 2023)

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

• ONCORNET2.0 Final Symposium (August 31 - September 1, 2023) Registration ends Tomorrow!

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

• GPCR Retreat (November 2 - 4, 2023) Registration is now open!

• Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels, and Transport Proteins (March 24 - 29, 2024)

GPCR Jobs

• NEW Research Scientist/Senior Scientist I - Molecular Pharmacology

• NEW Vice President, Medical Affairs

• NEW Associate Director / Director, Clinical Operations

• Professor in Cardiovascular Pharmacology

• Scientist I / Scientist II DOE (Native Mass Spectrometry)

• Senior Vice President of Global Medical Affairs

• Postdoctoral Research Associate

Explore Dr. GPCR Ecosystem