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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 Direct line to the Dr. GPCR community members Join the GPCR fan club and geek out with fellows!

January 2022 "G-protein-coupled receptors’ star has been on the rise in biotech in recent years as researchers have discovered the vast potential for GPCR-targeting drugs in treating a range of health conditions, from cancer and genetic disorders to inflammation and metabolic imbalances. Among those hitching their wagons to that star are Verily and Sosei Heptares, which have struck a research agreement to discover new GPCR targets that’ll fuel the development of potential drug candidates. The financial details of the strategic collaboration weren’t released, but Sosei Heptares’ past two team-ups in GPCR-based drug discovery have clocked in at $1 billion—with Genentech—and, just last November, $2.6 billion in a partnership with Neurocrine." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 ADGRL3 genomic variation implicated in neurogenesis and ADHD links functional effects to found that nsSNPs rs35106420, rs61747658, and rs734644, previously reported to be associated and in linkage GIP has been linked to the pathogenesis of diabetes mellitus, and our analyses suggest a potential link

September 2022 High GPER expression in triple-negative breast cancer is linked to pro-metastatic pathways Besides, high GPER expression was significantly linked to the worse survival in patients with lymph node Transcriptome-based bioinformatics analysis revealed that GPER was linked to pro-metastatic pathways

June 2022 "June 15, 2022 06:30 AM EDT - In 2016, Abbie Celniker was promoted to partner at Third Rock Ventures as the firm raised just over $600 million for its fourth fund. Since then, Celniker has helped usher in an additional fund and headed a few startups as interim CEO. Coming on its 15th year, Third Rock Ventures announced its sixth fund today — and largest one by far — at a whopping $1.1 billion. Adding it all up, Third Rock has raised $3.8 billion since its inception. That money has gone to some 60 biotechs, much of it as early funding." Read more at the source #DrGPCR #GPCR #IndustryNews

and chemistry pulled him into the world of GLP-1R, pancreatic β-cells, and the biological questions David The call from David — the glowing islet — created a pivot the team couldn’t ignore. He learned tissue complexity from David; David picked up the quirks of acetonitrile. David Hodson

episode, JB pulls the curtain back on the mindset and tactics he’s used for years—including the exact line The One-Line Icebreaker That Makes Asking Better Questions in Science Easy At conferences, most early-career JB short-circuits that anxiety with a single line he’s used for years: “Hi, I’m JB. In his collaboration with David Hodson, every major leap—from early ligand design to GPCR visualization David Hodson

David Hodson needed molecules that were only one synthetic step beyond what JB was already making. When David later shared early data — including a moment where he realized he could image an entire islet David brought deep experience in islet biology, calcium imaging, and tissue physiology. David picked up unexpected chemistry insights — including a well-loved lesson involving acetonitrile David Hodson

This week's highlight includes congrats to: David A Cooper, David Minh, et al., for their research on Classified GPCR News from April 1st to 7th, 2024 GPCR Activation and Signaling GPRASP1 loss-of-function links

localization, ligand access, and intracellular signaling can look different in actual tissues vs. cell lines GPCR–islet signaling links extended beyond classical ligand models.Collaboration and long-term persistence David Hodson

David Hodson walks through how his team uses fluorescence tools and chemically engineered ligands to Fluorescent ligand engineering clarifies receptor behavior that cell lines can’t reveal. Listen to the episode ➤ Quick Links Assess GPCR Biased Signaling of Agonist How GPCR Collaboration Built

Watch Episode #177 The Experiment That Was Never Meant to Succeed When David Hodson’s lab teamed up with David Hodson

Nguyen ,  Ziaurrehman Tanoli ,  Saad Hassan , Umut Onur Özcan ,   Jimmy Caroli ,   Albert J Kooistra ,   David Taracena Herrera , Søren N Andreassen ,   Jimmy Caroli ,   Albert J Kooistra , Gáspár Pándy-Szekeres ,   David Direct line to the Dr.

David Gloriam and his team present GproteinDb in 2024 Are you looking to hire? adhesion GPCR dissociation GPCR Activation and Signaling GPR101: Modeling a constitutively active receptor linked to X-linked acrogigantism The mechanism of Gαq regulation of PLCβ3-catalyzed PIP2 hydrolysis GPCR Binders

David Gloriam and Dr. Albert Kooistra.

They think in functional groups, fluorophores, linkers, and binding pockets. The signaling didn’t line up. The knockout behaved differently than expected. David Hodson

However, Trinquet’s team, in collaboration with Professor David Parker from Durham University, cracked with other HTRF assays for multi-pathway mapping—G protein, arrestin, internalization—on the same cell line

pushed pHSense toward rapid commercialization—pivoting it from a research probe into a full product line It’s the product of layered collaborations—with Durham University chemist David Parker on the probe chemistry

David Gloriam , Dr.

David Parker spent years designing rare-earth europium probes. And for those on the front lines of GPCR science, it’s a new lens to see what’s always been there—just

This week’s edition links ligand mechanism to the decisions that shape affinity, efficacy, selectivity Working closely with Professor David Parker of Durham University, Trinquet’s group cracked the scaffold

reveals unexpected differences in downstream pathway activation Chiara D Mancinelli, Joshua Levitz, David Novartis continues to deliver strong sales growth and core margin expansion in Q2; raises FY 2024 bottom-line

Maria Majellaro, Johannes Broichhagen, and David Hodson discuss GLP-1 receptor probes, fluorescence-based

José Labandeira-García , Rafael Franco Endomembrane GPCR signaling: 15 years on, the quest continues Davide Direct line to the Dr.

spatial, temporal and ligand bias of G protein-coupled receptors Antonios Drakopoulos, Peter Gmeiner, Davide

Lukas Grätz, David Gloriam, and Gunnar Schulte’s research on Unveiling pathway selectivity in Frizzleds

Burger , Arthur Christopoulos , David M.

Heterodimerization when Expressed Heterologously in Saccharomyces cerevisiae The beta 2 adrenergic receptor cross-linked dendritic cells Methods & Updates in GPCR Research Generation of CRISPR/Cas9 modified human iPSC line

Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the that orchestrate P-gp expression and highlight unappreciated connections between multiple pathways linked

pharmacophore with the desired affinity and/or functional activity, that is modified to introduce a linked A3 adenosine receptor fluorescent antagonist (CELT-327) was added to HCT116 cells (colon cancer cell line The combination of the correct linker and dye can offer better photostability, maintaining signal integrity Our proprietary conjugation technology also facilitates the synthesis of different linker sizes and types The dashed line represents the frontier between both cell types.