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Highlights: Celebrating Excellence: Hyoungjun Ham , Yamina Berchiche , Thomas Sakmar , Vladimir Katanaev , Helen Su , et al. for their fantastic work on Germline mutations in a G protein identify signaling cross-talk Mark your calendars and make sure to enroll before the deadline! agonist ZT-003 shows promising results for metabolic disorders INDIGO Biosciences, INC as a Preferred Supplier 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered autocatalytic cleavage upstream of the agonistic peptide sequence, an event necessary for NTF displacement and subsequent mediate stronger signaling in mouse versus human GPR116 and recapitulate these findings in a model supporting

August 2022 GPR3 expression in retinal ganglion cells contributes to neuron survival and accelerates The axonal degeneration that occurs before retinal ganglion neuronal loss is suggested to be involved Our earlier reports suggested that GPR3 enhances both neurite outgrowth and neuronal survival. Surprisingly, RGCs in GPR3 knockout mice were vulnerable to neural death during aging without affecting These results suggest that GPR3 expression in RGCs helps maintain neuronal survival and accelerates axonal

Orthosteric sites are zero-sum: highest affinity or concentration wins. mechanisms helps refine therapeutic index calculations, prioritize safer leads, and avoid late-stage surprises orthosteric vs. allosteric isn’t just a mechanistic detail; it’s a decision that shapes your pipeline’s success discovery 🌍 Flexible, on-demand lessons for busy scientists 💡 Influence the curriculum with your topic suggestions Subscribe to The Kenakin Brief  today ➤

Breakthroughs this week: Novo Nordisk cuts Ozempic® cost; Nxera launches obesity pipeline; Superluminal–Lilly cardiometabolic partnership; New GPCR allosteric sites; GPCR signaling potentiation by ATP and sugars Are your promising in vitro results failing to translate into real-world clinical success? Dr. Manuscript summary deadline: 24 September 2025 . Final submissions: 12 January 2026 . Submit your paper today to secure your work in Volume II ➤ Why Dr.

Glycosylation and sulfation – N-terminal PTMs on chemokine receptors The interaction of chemokine receptors N-terminal PTMs include sulfation and glycosylation which contribute to the overall negative charge of tool for tyrosine sulfation sites (Monigatti F et al. 2002), suggest that CC chemokine receptors have Tyrosine sulfation consists in the transfer of a sulfate group from the adenosine 3’-phosphate 5’-phosphosulfate There are few examples of the applicability of the sulfo-glyco barcode in drug discovery.

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October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter

October 2022 Successful prednisolone or calcimimetic treatment of acquired hypocalciuric hypercalcemia This emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate fluctuating Ca levels from approximately normal to near fatally high ranges, (e) acute exacerbations could be successfully

October 2022 Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and This study unveiled a new antifibrotic cGAS/STING signaling pathway that suppresses pathological angiogenesis We showed that cGAS expression was induced in fibrotic liver and kidney, but suppressed in endothelial Together, our data support that activation of cGAS/STING signaling mitigates organ fibrosis and suppresses

August 2022 TAS2R supports odontoblastic differentiation of human dental pulp stem cells in the inflammatory

August 2022 In vitro assays for the functional characterization of (psychedelic) substances at the serotonin receptor 5-HT2A R "Serotonergic psychedelics are substances that induce alterations in mood, perception Besides their appearance on the (illicit) drug market, e.g. as new psychoactive substances, their potential This group of substances demonstrates a broad structural variety, leading to insufficiently described

is, besides classical ligands, a great number of bivalent ligands (i. e. aiming on two distinct OR subtypes

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👥We have many surprises in reserve for you at the next Dr. GPCR Summit 2022 held between October 10th and 16th. Dr. GPCR Summit is FREE for all Ecosystem site members! Become a member today, it's also free!

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September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing Herein we generated CaSR-GABAB1 and CaSR-GABAB2 chimeras subject to GABAB -dependent endoplasmic reticulum sorting to traffic mutant heterodimers to the cell surface. domain, however, corresponding to heterozygous familial hypocalciuric hypercalcemia type-1 (FHH-1), supported We consider how receptor asymmetry may support the underlying mechanisms. © 2022 The Authors.

September 2022 Fly casting with ligand sliding and orientational selection supporting complex formation

Despite similar subunit composition, close amino acid identity, and identical posttranslational farnesylation of their Gγ subunits, rods and cones rely on unique Gγ1 (Gngt1) and Gγc (Gngt2) isoforms, respectively The only other farnesylated G-protein γ-subunit, Gγ11 (Gng11), is expressed in multiple tissues but not Thus, while farnesylated Gγ subunits are functionally active and largely interchangeable in supporting

September 2022 Identification and functional characterization of the sulfakinin and sulfakinin receptor in the Chinese white pine beetle Dendroctonus armandi "The sulfakinin (SK) is an important signal molecule

Subacute SCI is mainly characterized by neuronal apoptosis, axonal demyelination, Wallerian degeneration It has been discovered in recent years that inflammatory responses are particularly important in subacute

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therapeutics to treat a wide range of chronic diseases, today introduced Basecamp Bio, a wholly owned subsidiary

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March 2022 Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment discovery of medicines targeting G-protein coupled receptors (GPCRs), today announced that the first subjects The Phase 1 study will assess the safety, tolerability and pharmacokinetics of CFTX-1554 in healthy subjects

February 2022 Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner Jiangsu Nhwa Pharmaceutical "Submission supported by data from a Phase 3 bridging study of oliceridine injection compared to IV morphine, conducted in China by Nhwa Trevena is eligible to receive future success disorders, today announced that China’s National Medical Products Administration (NMPA) has accepted submission The NDA was submitted by Trevena’s partner, Jiangsu Nhwa Pharmaceutical, and follows completion by Nhwa

October 2022 "Lysosomes coordinate cellular metabolism and growth upon sensing of essential nutrients, including cholesterol. Through bioinformatic analysis of lysosomal proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annotated as G protein-coupled receptor 155), a multidomain transmembrane protein that enables cholesterol-dependent activation of the master growth regulator, the protein kinase mechanistic target of rapamycin complex 1 (mTORC1). Cholesterol bound to the amino-terminal permease-like region of LYCHOS, and mutating this site impaired mTORC1 activation. At high cholesterol concentrations, LYCHOS bound to the GATOR1 complex, a guanosine triphosphatase (GTPase)-activating protein for the Rag GTPases, through a conserved cytoplasm-facing loop. By sequestering GATOR1, LYCHOS promotes cholesterol- and Rag-dependent recruitment of mTORC1 to lysosomes. Thus, LYCHOS functions in a lysosomal pathway for cholesterol sensing and couples cholesterol concentrations to mTORC1-dependent anabolic signaling." Read more at the source #DrGPCR #GPCR #IndustryNews