2022 Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR simulation was conducted to elucidate binding mechanisms of a middle-sized flexible molecule, bosentan, to a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "Class A (rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid scrambling is not detectable in the resting plasma membrane of mammalian cells that is replete with GPCRs considered whether cholesterol, a prominent component of the plasma membrane, limits the ability of GPCRs This mechanism may explain the inability of GPCRs to scramble lipids at the plasma membrane." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient to specify recruitment of STAM1 to βarr1 for other GPCRs. Read more at the source #DrGPCR #GPCR #IndustryNews

2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR programs in key therapeutic areas Kallyope, pioneers in drug discovery involving the gut-brain axis, the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR . " Read more at the source #DrGPCR #GPCR #IndustryNews

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August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated reveal an interaction between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin Read more at the source #DrGPCR #GPCR #IndustryNews

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling pathways over time, and in response to drug treatments in freely-moving adult rats. After several weeks to allow biosensor expression, fiber photometry is used in order to record drug responses spectrum of neuroscience research, ranging from the study of neural circuits and behavior, to preclinical drug 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

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

GPCR Binders, Drugs, and more Persistent challenges in the development of an mGlu7 PAM in vivo tool compound 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. GPCR Ecosystem

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

Binders, Drugs, and more LP2, a cyclic angiotensin-(1-7) analog extended with an N-terminal D-lysine Papers GPCRs: Signal Transduction. 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 Binders, Drugs, and more Engineered Human Antibody with Improved Endothelin Receptor Type A Binding 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. GPCR Ecosystem

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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

undrugged peptidergic GPCRs. His presentations will describe Orion’s drug discovery platform, one of the fastest drug discovery solutions in the industry for targeting peptidergic GPCRs. drug candidates." Read more at the source #DrGPCR #GPCR #IndustryNews

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December 2021 "Drug development is rarely trivial. Drugs that do make it to clinical trials have major hurdles to clear—not the least of which is safety It is necessary for drugs to evaluated for potential toxicities and side effects, and these key factors must be deemed tolerable before investigators can assess drug potency. Read more at the source #DrGPCR #GPCR #IndustryNews

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

July 2022 "Orion Biotechnology and Peptilogics are pursuing AI-driven drug discovery to explore new functional and precision-engineer therapeutics with enhanced potency and tailored signaling against an undrugged GPCR #ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews

GPCRs have also been identified within the mitochondria. Therefore, it is essential to design tagging strategies that minimize interference with GPCR function 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.

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

the regulation of mTORC1 by upstream stimuli, with a specific focus on G-protein coupled receptor (GPCR

September 2022 "G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases A central question of GPCR drug discovery is to understand what determines the agonism or antagonism small changes to the ligands that invert their pharmacological activity and thus helps to guide the drug This approach can be readily applied to any drug target." Read more at the source #DrGPCR #GPCR #IndustryNews