Hop in the Time Machine with GPCR: Unraveling the Future of Research! ⦿ Nov 24 - Dec 1, 2024

Grab your flux capacitors, GPCR time travelers!

We're zooming back to the future of GPCR discoveries. Buckle up as we time-hop through this week's GPCR escapade!

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This Week’s Highlights:

G protein-coupled receptor (GPCR) pharmacogenomics

Miles D Thompson, David Reiner-Link, Alessandro Berghella, Brinda K Rana, G Enrico Rovati, Valerie Capra, Caroline M Gorvin, Alexander S Hauser

Calcineurin-fusion facilitates cryo-EM structure determination of a Family A GPCR

Jun Xu, Geng Chen, Haoqing Wang, Sheng Cao, Jie Heng, Xavier Deupi, Yang Du, Brian K Kobilka

Red and far-red cleavable fluorescent dyes for self-labelling enzyme protein tagging and interrogation of GPCR co-internalization

Kilian Roßmann, Ramona Birke, Joshua Levitz, Ben Jones, Johannes Broichhagen

Design of allosteric modulators that change GPCR G protein subtype selectivity 

Madelyn N Moore, Kelsey L Person, Abigail Alwin, Campbell Krusemark, Ezequiel Marron Fernandez de Velasco, Steven H Olson, Lauren M Slosky, et. al.

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Classified GPCR News

 Let’s dive into the Classified GPCR News from November 25th to December 1st, 2024

Industry News

• Amgen says obesity drug caused up to 20% weight loss after a year, with no plateau

• INAUGURATION OF AELIS FARMA NEW LABORATORY at Institut Européen de Chimie et Biologie (IECB) in Pessac (Bordeaux)

• AI-Powered Drug Discovery and Antibody Innovation: DeciBio Q&A with Sean McClain, Founder & CEO, and Zach Jonasson, CFO & CBO at Absci

• Octant: A Next Generation Approach to Genetic Disease

• Antiverse, Nxera Pharma Teams to Unleash Machine Learning on Elusive Biological Keys to Medical Therapies

• From Structure to Solution: How Structural Biology Informs the Development of Drugs Targeting G Protein-Coupled Receptors

• ARTICA THERAPEUTICS ANNOUNCES ESTABLISHMENT OF SCIENTIFIC ADVISORY BOARD

GPCR Events, Meetings, and Webinars

• December 10 - 12, 2024 | Pharmacology 2024

• January 13 - 16, 2025 | PepTalk 2025

• January 25 - 29, 2025 | SLAS 2025

• February 15 - 16, 2025 | Structural and Functional Approaches in GPCR Drug Discovery

• February 15 - 19, 2025 | BPS 2025

• February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery

• March 12 - 14, 2025 | NextGen Biomed 2025

• March 25 - 28, 2025 | 10th German Pharm-Tox Summit

• April 1 - 5, 2025 | XXIII GEM Meeting in 2025

• April 3 - 6, 2025 | ASPET 2025

• April 14 - 17, 2025 | 20th Drug Discovery Chemistry

• April 24 - 27, 2025 | American Physiology Summit 2025

• April 25 - 30, 2025 | AACR Annual Meeting 2025

• May 12 - 15, 2025 | PEGS 2025

• May 20 - 22, 2025 | SLAS Europe 2025

• June 16 - 19, 2025 | BIO International Convention 2025

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

GPCR Jobs

• NEW GPCR Molecular Pharmacologist

• Scientist - Biology

• Scientist I Cell Biology - Tectonic Therapeutic

• Senior Principal Scientist, Medicinal Chemistry

• PhD fellowship in GPCR mechanosensing

• Senior Scientist, GPCR Pharmacology

• Research Associate - Professor Graeme Milligan

• Postdoc in Molecular Pharmacology - The Hauser Group

• Postdoctoral Scholar – iPSC in cardiac and endothelial cell function

• Protein Biochemist/Structural Biologist

  
  

GPCR Activation and Signaling

• Exploring Bias in GPCR Signaling and its Implication in Drug Development: A One-Sided Affair

• Agonist activation to open the Gα subunit of the GPCR-G protein precoupled complex defines functional agonist activation of TAS2R5

• Biased activation of the vasopressin V2 receptor probed by molecular dynamics simulations, NMR and pharmacological studies

• High-affinity ELR+ chemokine ligands show G protein bias over β-arrestin recruitment and receptor internalization in CXCR1 signalling

GPCR Binders, Drugs, and more

• G protein-coupled receptor (GPCR) pharmacogenomics

• Antibodies expand the scope of angiotensin receptor pharmacology

• Chimeric antigens displaying GPR65 extracellular loops on a soluble scaffold enabled the discovery of antibodies, which recognized native receptor

• Design of allosteric modulators that change GPCR G protein subtype selectivity

GPCRs in Cardiology, Endocrinology, and Taste

• Integrated bioinformatics analysis reveals that CCBP2 and GPR87 are new GPCR-associated biomarkers for preeclampsia

• Metabolic control of Luteinizing Hormone-responsive ovarian steroidogenesis

• Cardiovascular Complications and Their Association With Short- and Long-Term Outcomes in Patients With Multiple Myeloma and Lymphoma Undergoing Chimeric Antigen Receptor T-Cell Therapy

GPCRs in Neuroscience

• Innervation density governs crosstalk of GPCR-based norepinephrine and dopamine sensors

• Intranasal delivery of liposome encapsulated flavonoids ameliorates l-DOPA induced dyskinesia in hemiparkinsonian mice

• GPR88 impairs the signaling of kappa opioid receptors in a heterologous system and in primary striatal neurons

GPCRs in Oncology and Immunology

• Protease-Activated Receptor-1 IgG Autoantibodies in Patients with COVID-19

• Signaling by neutrophil G protein-coupled receptors that regulate the release of superoxide anions

• SSTR2 positively associates with EGFR and predicts poor prognosis in nasopharyngeal carcinoma

• RNAi library screening reveals Gβ1, Casein Kinase 2 and ICAP-1 as novel regulators of LFA-1-mediated T cell polarity and migration

Methods & Updates in GPCR Research

• Calcineurin-fusion facilitates cryo-EM structure determination of a Family A GPCR

• Red and far-red cleavable fluorescent dyes for self-labelling enzyme protein tagging and interrogation of GPCR co-internalization

• AlloViz: A tool for the calculation and visualisation of protein allosteric communication networks

• GPTrans: A Biological Language Model-Based Approach for Predicting Disease-Associated Mutations in G Protein-Coupled Receptors

Structural and Molecular Insights into GPCR Function

• Inhibitory effect of truncated isoforms on GPCR dimerization predicted by combinatorial computational strategy

• Uncovering conserved networks and global conformational changes in G protein-coupled receptor kinases

• The membrane domains of mammalian adenylyl cyclases are lipid receptors

• Structural insights into endogenous ligand selectivity and activation mechanisms of FFAR1 and FFAR2

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