They are G-protein-coupled receptors and bind as ligand retinal, which is bound covalently to a lysine Therefore, we wondered: Do opsins exists that have lost this lysine during evolution? To find such opsins, we built an automatic pipeline for reconstructing a large-scale opsin phylogeny. Thus, we call them gluopsins. However, what their particular function is, remains to be seen."

October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. Employing GRK knockout cells and β-arrestins lacking the finger-loop-region, we show that the two isoforms Moreover, we assess β-arrestin conformational changes that are induced specifically by proximal and distal Here, we show differences between conformational changes that are induced by P-R* or R* receptor states

Here, we introduce azodopa, a novel photoswitchable ligand that enables reversible spatiotemporal control We demonstrate that azodopa activates D1-like receptors in vitro in a light-dependent manner. Azodopa is the first photoswitchable dopamine agonist with demonstrated efficacy in wild-type animals and opens the way to remotely controlling dopaminergic neurotransmission for fundamental and therapeutic

October 2022 Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism Whether and how RH affects responses within metabolically important peripheral organs to counterregulatory liver, white adipose tissue and skeletal muscle. Methods: Using a widely adopted rodent model of 3-day recurrent hypoglycemia, we first checked expression Additionally, we measured circulating FFA and glycerol to check lipolysis.

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September 2022 "In the Wnt-β-catenin pathway, Wnt binding to Frizzled (Fzd) and LRP5 or LRP6 (LRP5/6) Using purified Fzd proteins reconstituted in lipid nanodiscs, we investigated the factors that promote We found that the affinity of Fzd for Dvl was not affected by Wnt ligands, in contrast to other members by Dvl-associated lipid kinases in response to Wnt and which is required for LRP5/6 phosphorylation. Our findings suggest a positive feedback loop in which Wnt-stimulated local PI(4,5)P2 production enhances

February 2022 "Switzerland Today, InterAx Biotech is pleased to announce that Carola Weiss has joined Carola Weiss is a Senior Executive with more than 20 years of international experience in the biopharmaceutical Carola Weiss ’ professional career brings deep expertise in business development, marketing & sales,

of the Royal Society of Chemistry and Founder of (and ongoing consultant to) OMass Therapeutics , which This is a highly prestigious international award – exemplified by the fact that other winners this year

., a clinical-stage global biopharmaceutical company developing novel oral therapeutics to treat a wide range of chronic diseases, today introduced Basecamp Bio, a wholly owned subsidiary dedicated to fueling

Instituut Biotechnologie , at the Vrije Universiteit Brusle, Brussels, Belgium, has been named the winner Jan Steyaert will be presented with the Gabbay Award at Brandeis University on October 27 when he will give a public lecture on his work, followed by a ceremony.

August 2022 "We are happy to announce you our 2nd IRN i-GPCRnet meeting that will be held at the University of Wurzburg (Germany) from september 30th to october 1rst."

The Boston biotech revealed Wednesday afternoon that it would downsize its research to focus on its lead The move comes less than three weeks after X4 pulled together a $55 million PIPE and amended a loan facility

June 2022 "We’re delighted to welcome Dr Ed Brennan as our new Vice President, Head of Clinical Development He has led teams that have filed more than 10 Investigational New Drug Applications (IND), as well as In 2007 he formed IndiPharm which was a full-service Contract Research Organization whose operational headquarters were in Mumbai, India. He went on to study medicine at the Royal College of Surgeons in Ireland before receiving his Medical

April 2022 John Streicher talks about his work on terpenes found in cannabis as these may be a novel way to treat pain without the negative side effects " Many people are familiar with cannabis, but John These compounds may be a novel way to treat pain without the negative side effects of cannabinoids or

January 2022 "We are an experienced, innovative, global team on a bold mission to improve health by creating and developing life-changing medicines for people around the world."

receptor CXCR4 WHIM syndrome is a rare immunodeficiency disorder that is characterized by warts, hypogammaglobulinemia Here, we report on a new WHIM syndrome mutation that results in a frame shift within the codon for Ser339 (S339fs5) and compare the properties of S339fs5 with wild type CXCR4 and a previously identified WHIM In contrast to wild type CXCR4, both R334X and S339fs5 were largely insensitive to CXCL12-promoted degradation Moreover, while basal and agonist-promoted degradation of wild type CXCR4 was effectively inhibited by

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea are considered to have originated from early evolution of eukaryotic species, therefore, the genome-wide 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). purinergic and chemokine receptors were highly differentiated in humans.

Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day " Congratulations to Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of the 2022 Diabetes Research Grants at yesterday's annual World Diabetes Day Breakfast! This $60,000 grant from Diabetes Research WA will assist the Perkins' Molecular Endocrinology and Pharmacology Laboratory team who are investigating new ways to tackle the disease-inducing chronic inflammation that

March 2022 "Congratulations to Richard J. Law , our newly named Chief Business Officer. Richard is the architect behind nearly all of Exscientia's partnerships and collaborations across pharma and #biotech⁠ and is an advocate for the role of #AI in drug discovery." Read more at the source #DrGPCR #GPCR #IndustryNews

Transporting Protein-coupled receptors (GPCRs) to the synapse, where they are involved in neurotransmission vesicle-associated-membrane-protein-2-is-a-cargo-selective-v-snare-for-a-subset-of-gpcrs #GPCR #DrGPCR#Ecosystem Crilly, S.E., W. Weinberg, and M.A. Puthenveedu. 2021. Wang, F., X. Chen, X. Zhang, and L. Ma. 2008. Wickner, W., and R. Schekman. 2008. Membrane fusion. Nat. Struct. Mol. Biol. 15:658–664.

November 2021 "Target class-specific libraries mean you need to screen less to identify high-quality antibodies. Aaron Sato , Chief Scientific Officer at Twist Bioscience , elaborates. Antibody developers are increasingly utilising antibody libraries to derive high-quality, drug-like biologics. However, only a few general-purpose libraries have been commercially available for drug discovery. As a result, most approved library-derived antibodies originate from just three libraries. The drugs also target relatively low-hanging fruit: like cytokines or tyrosine kinase receptors. To target hard-to-drug targets like G protein-coupled receptors (GPCRs), more libraries, including better and more targeted libraries, are needed." Read more at the source #DrGPCR #GPCR #IndustryNews

Nbs typically consist of a single polypeptide chain which contains the antigen-binding site and the effector H., Pautsch, A., Steyaert, J., Weis, W. I., & Kobilka, B. K. (2011). C., Gmeiner, P., Steyaert, J., Weis, W. I., Garcia, K. C., Wess, J., & Kobilka, B. K. (2013). N., Angelini, A., Waghray, D., Dror, R. O., Ploegh, H. L., & Garcia, K. C. (2015). D., Tworak, A., Watanabe, K., Pardon, E., Steyaert, J., Kandori, H., Katayama, K., Kiser, P.

impacted quality of life during treatment coupled with brain tumour recurrence; thus, new treatments are desperately In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets. date, the most promising targets are the chemokine, cannabinoid, and dopamine receptors, but future work

receptor activation, make this receptor an intriguing target for treating schizophrenia, a disease where novel interventions that move beyond dopamine receptor antagonists are desperately needed. While more work is needed to further elucidate the translational value of selectively targeting CB2 receptors below could suggest that CB2 receptors are anatomically located in schizophrenia-relevant circuits, where

The highest affinity compounds (15 to 24 nM) were identified from AF2 docking. One significant concern is the reliance on data quality and quantity, where inaccuracies or biases in Moreover, advanced AI models like AlphaFold3, which can predict complex protein-molecule interactions design is set to spark innovation in automated screening and large-scale data analysis, paving the way Nature 630, 493–500 (2024). https://doi.org/10.1038/s41586-024-07487-w

Subacute SCI is mainly characterized by neuronal apoptosis, axonal demyelination, Wallerian degeneration Methods The gene expression profiles of GSE20907 , GSE45006 , and GSE45550 were downloaded from the The models of the three gene expression profiles were all for SCI to the thoracic segment of the rat. The differentially expressed genes (DEGs) and weighted correlation network analysis (WGCNA) were performed using R software, and functional enrichment analysis and protein–protein interaction (PPI) network were

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