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Step into the world of drug discovery with Dr. In this foundational-level  lesson, Terry unpacks the real-life process behind discovering new drugs, You’ll explore: What makes a “discovery team” tick (and why teamwork is non-negotiable) The difference between Me Too  and First in Class  projects—and why both are essential Why target-based  discovery Don’t miss your chance to learn from one of the best: Unlock “Introduction to Drug Discovery" now

🧠Do you want to share your #GPCR knowledge? Come to Dr. GPCR Ecosystem and create a course on your favorite #GPCR research, technique and more… Available for GPCR Ecosystem paid memberships ➡️https://bit.ly/3R8ZZbo #gpcr #drgpcr

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular Modulating a single function of a specific aGPCR isoform while affecting no other function and no other Here, we engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3 Our work provides proof of concept for the modulation of isoform- and ligand specific aGPCR functions therapeutics" Read more at the source #DrGPCR #GPCR #IndustryNews

We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach for GPCR drug development by modulating GPCR/14-3-3 signals temporally." Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators The grant should help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates . " Read more at the source #DrGPCR #GPCR #IndustryNews

What if the way we've been studying GPCRs—arguably the most important drug targets in pharmacology—has Terry Kenakin invites us to challenge outdated assumptions and step into a new era of drug discovery. Here’s the surprising truth: up to 80% of GPCR-targeted drugs fail—not because of poor chemistry, but Join Terry’s Corner and stay updated on the latest in GPCR research—delivered in a format that’s as approachable

He has led teams that have filed more than 10 Investigational New Drug Applications (IND), as well as multiple New Drug (NDA) and Supplemental New Drug Applications (SNDA). #biotech #lifesciences #appointment #GPCR #Oncology" Read more at the source #DrGPCR #GPCR #IndustryNews

Traditionally, GPCR signaling was believed to primarily occur at the plasma membrane. GPCRs have also been identified within the mitochondria. Compartmentalized GPCR Signaling from Intracellular Membranes. Drug discovery today, 24(11), 2192–2201. https://doi.org/10.1016/j.drudis.2019.09.003 Ferrandon, S., Functional selectivity of GPCR-directed drug action through location bias.

GPCR Binders, Drugs, and more Persistent challenges in the development of an mGlu7 PAM in vivo tool compound : The discovery of VU6046980. GPCR Industry News Septerna Announces the Formation of a Cross-Functional Scientific and Drug Discovery GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

Watch Episode 167 Some GPCR-targeting antibodies don’t inhibit receptors. They activate them. GPCRs, are likely targets for antibody-based immune responses. This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology , GPCR diagnostics , Dr. GPCR ecosystem , multiplex assays

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE

GPCR Binders, Drugs, and more Engineered Human Antibody with Improved Endothelin Receptor Type A Binding A robust antibody discovery platform for difficult-to-express G protein-coupled receptors. Identification of a potential structure-based GPCR drug for interstitial cystitis/bladder pain syndrome GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential.

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Binders, Drugs, and more LP2, a cyclic angiotensin-(1-7) analog extended with an N-terminal D-lysine Addex and Indivior Extend Research Term Of Substance Use Disorder Gabab Positive Allosteric Modulator Discovery GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Ecosystem

GPCR event of the year is the 3rd edition of the Summit. Come join us from October 10 to 16 to hear about exciting #GPCR research from amazing speakers. GPCR Ecosystem site member to attend the Summit, it’s free! ➡️ https://bit.ly/3SUkB8D #gpcr #drgpcr

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

Hi GPCR Enthusiasts (and Arrestin Aficionados!)   This week at Dr. of GPCR-RAMP discovery. GPCR Updates   Advanced Methods for the Optimization of Candidate Selection  – Master GPCR behavior beyond modules reveal how location bias, intracellular signaling, and ligand kinetics can be leveraged to expand drug discovery horizons and fine-tune candidate selection.  

GPCR Binders, Drugs, and more Altered signaling at the PTH receptor via modified agonist contacts with Establishment of a CaCC-based Cell Model and Method for High-throughput Screening of M3 Receptor Drugs GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Ecosystem

October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties Read more at the source #DrGPCR #GPCR #IndustryNews

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Welcome to the 4th official Adhesion GPCR Consortium newsletter! de Investigación y de Estudios Avanzados del IPN (Cinvestav) How did you become involved in adhesion GPCR AB: I became aware of the existence of adhesion GPCRs while completing my graduate studies. The family of adhesion GPCRs called the Latrophilins or ADGRLs first captured my attention due to their For my postdoctoral training, I joined one of the labs that participated in Latrophilins’ discovery,

'unproductive coupling'[1] and a fascinating phenomenon known as GPCR priming [2]. The enhanced signalling observed in GPCR priming is attributed to the formation of temporal non-cognate-GPCR GPCR priming opens new avenues for understanding the nuanced regulatory mechanisms governing GPCR signalling This has significant implications for drug development, as targeting these non-cognate interactions could lead to novel therapeutic strategies for modulating GPCR activity.

Think a drug just "locks into" a receptor and does its job? Think again. The Importance of Binding in Drug Action In pharmacology, binding must happen before any drug effect crucial for drug efficacy. Implications for Drug Development As drug developers, understanding these nuances can significantly impact The dynamic interplay of chemical forces shapes drug effectiveness.

Examples of HTRF donor/acceptor pairs Expanding Time-Resolved Fluorescence Applications in Drug Discovery In a recent study , we contributed to the development of a robust HTRF assay for the discovery of new A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. HTRF: A technology tailored for drug discovery - a review of theoretical aspects and recent applications

For drug discovery teams navigating safety margins, biased signaling, and combination therapy design, The Mechanistic Edge Behind Smarter Drug Discovery One of the most powerful aspects of this session is In drug discovery, orthosteric vs. allosteric isn’t just a mechanistic detail; it’s a decision that shapes Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters Your membership gives you:   📚 Proven frameworks for real-world discovery 🌍 Flexible, on-demand lessons

cooperative interaction between G βγ subunits and GIRK channels determines both the amplitude and kinetics of GPCR-dependent Read more at the source #DrGPCR #GPCR #IndustryNews

Discovery? Robert Lefkowitz, Howard Rockman for their review G Protein-Coupled Receptors: A Century of Research and Discovery Binders, Drugs, and more Target-based discovery of antagonists of the tick (Rhipicephalus microplus) proteins in rice (Oryza sativa) G Protein-Coupled Receptors: A Century of Research and Discovery Challenges cell-based assays in drug discovery October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs

Get ready for an expedition, GPCR explorers! Welcome back to your weekly GPCR quest! Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in Olfactory