Next on the Dr. GPCR Podcast, we have Dr. Pina Cardarelli, CSO of GPCR Therapeutics. ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr#drgpcr #podcast

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in D2 dopamine receptors. The D1 receptor (D1R) is a Gαs/olf-coupled GPCR which activates a cAMP/PKA/DARPP-32 signalling cascade findings identify the BET protein family, and Brd4 in particular, as novel regulators of basal and D1R-dependent transcription in rat striatal neurons, and delineate complex bi-directional effects of bromodomain inhibitors

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine This increase is at least partially due to a significant decrease in agonist-promoted phosphorylation Interestingly, there were also significant differences in receptor degradation, with S339fs5 having a very high basal level of degradation compared to that of R334X and wild type CXCR4. the CXCR4 antagonist TE-14016, this had no effect on the degradation of the WHIM mutants.

Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes: Impact of Ligand discovery aimed at identification of chemical tools and drug leads is aided by molecular docking and 68 cross docking simulations). to self-docking. cross-docking, respectively.

Intracellular calcium ([Ca2+]i) signaling is a critical regulator of chondrogenesis, chondrocyte differentiation , and cartilage development. One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs , proliferation, and protein deposition in 2D ATDC5 cultures. , increased cell proliferation, and enhanced matrix production in a CNO dose- and frequency-dependent

Recent studies have revealed that PGs play pivotal roles in embryo development, ciliogenesis, and organ During development, PGE2 signaling regulates embryogenesis, hepatocyte differentiation, hematopoiesis advances in understanding the functions and mechanisms of prostaglandin signaling in ciliogenesis, embryo development

In recent years, pharmaceutical companies have begun to utilize cryo-EM for structure-based drug design Structural analysis of integral membrane proteins, which comprise a large proportion of druggable targets pose particular challenges for X-ray crystallography, by cryo-EM has enabled insights into important drug In this review, we discuss recent instructive examples of impacts from cryo-EM in therapeutics design for future development of the technique.

December 2022 Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop Novel Therapeutic Antibodies against GPCR Targets " Collaboration aims to combine Twist’s GPCR targets Tokyo, Japan and Cambridge, UK, 16 December 2021 – Sosei Group Corporation (“the Company ”; TSE: 4565), the world leader in GPCR-focused structure-based drug design (SBDD) and development, and using its silicon platform, announced a strategic collaboration to discover therapeutic antibodies

November 2021 Dr. Kevin Pfleger and Dr. Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day of the 2022 Diabetes Research Grants at yesterday's annual World Diabetes Day Breakfast! is linked to type 2 diabetes." Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 "So proud and grateful to receive honorary doctorate yesterday from Karolinska Institute Read more at the source #DrGPCR #GPCR #IndustryNews

but Omass Therapeutics Ltd.’s new structure-based technology has passed a key test, in enabling the discovery of orally available small molecules aimed at intractable and poorly drugged membrane and complex-bound intracellular protein complexes and solute carriers, are relevant to immunology indications and rare diseases Read more at the source #DrGPCR #GPCR #IndustryNews

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

Below is your Classified GPCR News at a glance for December 5 to December 11th, 2022. GPCR Activation and Signaling Targeting GRK2 and GRK5 for treating chronic degenerative diseases: Advances GPCR Binders, Drugs, and more LP2, a cyclic angiotensin-(1-7) analog extended with an N-terminal D-lysine Deadline February 12, 2023. Explore Dr. GPCR Ecosystem

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma Here, we identified a total 216 full-length GPCR genes in the marine water flea Diaphanosoma celebensis genome, which were classified into five distinct classes (A, B, C, F, and other). Phylogenetic comparison of GPCRs in D. celebensis to those in humans (Homo sapiens), fruitfly (Drosophila Our findings suggest sporadic evolutionary processes within the GPCR gene families identified in D. celebensis

D., & Collins, B. M. (2019). Sustained cyclic AMP production by parathyroid hormone receptor endocytosis. J., & Calebiro, D. (2016). , D., Huang, B., Wedegaertner, P. J., & Calebiro, D. (2017).

(NASDAQ: KRTX), a clinical-stage biopharmaceutical company driven to create and deliver transformative The trial met its primary endpoint, with KarXT demonstrating a statistically significant and clinically PANSS) total score compared to placebo (-21.2 KarXT vs. -11.6 placebo, p<0.0001) at Week 5 (Cohen’s d KarXT also demonstrated an early and sustained statistically significant reduction of symptoms, as assessed Read more at the source #DrGPCR #GPCR #IndustryNews

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can be employed in GPCR research and drug discovery. Rational Drug Design One immediate application of this research lies in rational drug design . This distinction is essential for designing drugs that selectively target these residues to achieve desired For example, orthosteric drug design —in which drugs bind to the receptor’s primary active site—can now Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery. Dr. GPCR Ecosystem; Dr.

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Dear GPCR Enthusiasts! Get ready to save the dates! Dr. Before the new semester kicks off, dive into our premium on-demand courses! Kenakin and Hoare on '   Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR Discount for Dr. GPCRs and mRNA antigens enable drug discovery and development Mapping GPCR-RAMP complexes with MolBoolean

Unlock a 25% exclusive discount on these courses with Dr. Don’t miss out—secure your spot today! Registrations for the public will be on Monday! Hurry! Contact us at Hello@DrGPCR.com   to learn more. Your participation is eagerly awaited!   ONE-GO: Direct detection of context-dependent GPCR activity Multiplexed mapping of the interactome of breathe new life into schizophrenia pipeline GPCR Dynamics Reveal Mechanisms for Drug Discovery DMS:

G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play critical roles in the regulation of tissue development of the C-terminal Go protein is essential for Go's efficient engagement with the active GPR97, the detailed Hence, we performed extensive large-scale molecular dynamics (MD) simulations of the GPR97-Go complex design of aGPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews

2022 Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of depression ), a classic prescription of traditional Chinese Medicine (TCM), is widely used in the treatment of depression Moreover, molecular docking was applied to valid the important interactions between the ingredients and KEGG pathway analysis highlighted the most significant pathways associated with depression treatment, Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor In a recent issue of Molecular Cell, Fonseca et al. identified a previously overlooked desensitization adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor to internalize and desensitize Read more at the source #DrGPCR #GPCR #IndustryNews

is one of the critical acaricides/insecticides for effective control of pest infestation of Varroa destructor mite, a devastating parasite of Apis mellifera, because of its low toxicity to honeybees. Here, molecular dynamics simulations are employed to explore the implied mechanism of the enhanced sensitivity Read more at the source #DrGPCR #GPCR #IndustryNews

fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases , but few therapies have been directed against GPCRs in the field of cancer, partly because of the lack the gene expression of a panel of GPCRs in tumor and stromal cells, identifying specific gene sets defining for GPCR characterization through imaging, and as possible new tools used for target validation in drug Read more at the source #DrGPCR #GPCR #IndustryNews

Intriguingly, the two ligands have distinct signaling and physiological properties: PTH evokes prolonged The distinct molecular actions are ascribed to the differences in ligand recognition and dissociation A comparison of the PTH-bound and PTHrP-bound structures reveals distinct ligand-receptor interactions into the unique and complex process of ligand dissociation from the receptor and shed light on the distinct durations of signaling induced by PTH and PTHrP" Read more at the source #DrGPCR #GPCR #IndustryNews