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August 2022 Dopamine D 1 receptor-mediated β-arrestin signaling: Insight from pharmacology, biology,

precursors and 48 putative neuropeptide G protein-coupled receptor (GPCR) genes were identified in D. research provides more knowledge on neuropeptide systems and sets the groundwork for the creation of novel D.

Alterations in the expression and/or activity of brain G-protein-coupled receptors (GPCRs) such as dopamine D1R, D2LR, D3R, and D4R, vasopressin V1AR, and serotonin 5-HT1AR are noted in various neurodegenerative diseases (NDDs). Since studies have indicated that flavonoids can target brain GPCRs and provide neuroprotection via inhibition of monoamine oxidases (hMAOs), our study explored the functional role of kurarinone, an abundant lavandulated flavonoid in Sophora flavescens, on dopamine receptor subtypes, V1AR, 5-HT1AR, and hMAOs. Radioligand binding assays revealed considerable binding of kurarinone on D1R, D2LR, and D4R. Functional GPCR assays unfolded the compound's antagonist behavior on D1R (IC50 42.1 ± 0.35 μM) and agonist effect on D2LR and D4R (EC50 22.4 ± 3.46 and 71.3 ± 4.94 μM, respectively). Kurarinone was found to inhibit hMAO isoenzymes in a modest and nonspecific manner. Molecular docking displayed low binding energies during the intermolecular interactions of kurarinone with the key residues of the deep orthosteric binding pocket and the extracellular loops of D1R, D2LR, and D4R, validating substantial binding affinities to these prime targets. With appreciable D2LR and D4R agonism and D1R antagonism, kurarinone might be a potential compound that can alleviate clinical symptoms of Parkinson's disease and other NDDs. Read full article

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR smoothened "The oncogenic G-protein-coupled receptor (GPCR) Smoothened (SMO) is a key transducer of the hedgehog (HH) morphogen, which plays an essential role in the patterning of epithelial structures. Here, we examine how HH controls SMO subcellular localization and activity in a polarized epithelium using the Drosophila wing imaginal disc as a model. We provide evidence that HH promotes the stabilization of SMO by switching its fate after endocytosis toward recycling. This effect involves the sequential and additive action of protein kinase A, casein kinase I, and the Fused (FU) kinase. Moreover, in the presence of very high levels of HH, the second effect of FU leads to the local enrichment of SMO in the most basal domain of the cell membrane. Together, these results link the morphogenetic effects of HH to the apico-basal distribution of SMO and provide a novel mechanism for the regulation of a GPCR." Read more at the source #DrGPCR #GPCR #IndustryNews

JoAnn Trejo!

References   (1) Brown, D. G.; Boström, J. D.; Reid, R.; Robinson, L.; Ashley, G. W.; Santi, D. V.

If you’re in GPCR discovery or biotech R&D, this is a masterclass in turning deep science into scalable For Early-Career Scientists: If you want to work in product R&D, learn this: real innovation happens It reflects decades of foundational R&D—from the fluorescent probes of Cisbio’s early days to the receptor-targeting practical tools to accelerate your research or career. 👥 Build connections. 🧪 Get insights. 🎧 Stay ahead

S.; Wu, Z.; Kendall, D. A. D.; Irizarry, L.; Trecki, J.; Schwartz, M.; Gerona, R. M.; Compton, D. R.; Martin, B. R.; Abood, M. E. P.; Maccarrone, M.; Veprintsev, D. B.; Carreira, E. M.; Grether, U.; Nazaré, M. H.; Lambert, D. M.; Depreux, P.; Hénichart, J.-P.

L., & Fowler, D. M. (2011). Trends in Biotechnology , 29 (9), 435–442. https://doi.org/10.1016/j.tibtech.2011.04.003 Fowler, D. M., Trinidad, D. D., English, J. G., Coyote-Maestas, W., & Aashish Manglik. (2024).

K., Strader, D. J., Benovic, J. L., Dohlman, H. G., Frielle, T., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. E., Mumford, R. A., Slater, E. E., Sigal, I. S., Caron, M. D. (1986). B., Panova, O., Hilger, D., Casiraghi, M., He, F., Maul, L., Gmeiner, P., Kobilka, B.

Read fast, apply faster, and stay ahead in GPCR drug discovery with evidence-based insights—no hype, busy scientists 💡 Influence the curriculum with your topic suggestions 🆕 Weekly new releases to stay ahead   👉 Explore Trailers & Join Today Inside Revvity's R&D: How pHSense Was Born The day your data surprises And perhaps that’s the deeper story: Revvity’s R&D team didn’t just invent another tool. . 👉 Go behind the scenes with Revvity’s R&D team ➤ Celtarys Research – Advantages of Fluorescent Ligands

T., Rosenbaum, D. M., Thian, F. S., Kobilka, T. S., Schnapp, A., Konetzki, I., Sunahara, R. N., Angelini, A., Waghray, D., Dror, R. O., Ploegh, H. L., & Garcia, K. C. (2015). Science (New York, N.Y.), 347(6226), 1113–1117. https://doi.org/10.1126/science.aaa5026 Wu, A., Salom, D. D., Tworak, A., Watanabe, K., Pardon, E., Steyaert, J., Kandori, H., Katayama, K., Kiser, P. D., & Palczewski, K. (2023).

Johannes Broichhagen - aka JB  — which, amusingly, began when Hodson opened the door wearing cleaning one sustained curiosity thread involved a protein released by alpha cells in the pancreas: Vitamin D agonists reshaping diabetes and obesity care, the biggest questions — and opportunities — are still ahead

Build the R in R&D.

D., & Collins, B. M. (2019). J., & Calebiro, D. (2016). Endocrinology, 157(4), 1613–1621. https://doi.org/10.1210/en.2015-1945 Irannejad, R., Pessino, V., Mika, D. J., & Calebiro, D. (2017). Z., Wilderman, A., Katakia, T., McCann, T., Yokouchi, H., Zhang, L., Corriden, R., Liu, D., Feigin, M

Fowler, D. M., & Fields, S. (2014). Deep mutational scanning: a new style of protein science. C., Sykes, D. A., Viray, A. E., Vitale, R. M., Tomašević, N., ... & Carreira, E. M. (2024). D., Muñoz, L. L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A., & May, L.

We have cloned and characterized SK and SKR genes in the D. armandi and carried out bioinformatics predictions parallel, injection of SK caused a significant reduction in body weight and increase in mortality of D.

from more than 60 ORs in the testis and only a few ORs in the liver (Flegel C. et al. 2013; Maßberg D. ORs, although there are highly increased in prostate tissue, especially in prostate cancer (Maßberg D. sandalore-activated receptor OR2AT4 shown to promote human keratinocyte proliferation and migration (Busse D. olfactory-specific chaperones to be correctly targeted to the surface of heterologous cells (Maßberg D.

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

Improving Hematopoietic Stem Cell Mobilization Using Propranolol with GPC-100 Sosei Heptares to Host R&D Day Highlighting its Innovative R&D and Late-Stage Development Progress Parker Moss to Join Exscientia

Innovation in the pharmaceutical industry: New estimates of R&D costs. Lu S, He X, Ni D, Zhang J. Persechino M, Hedderich JB, Kolb P, Hilger D. Dave K, Gelman H, Thu CT, Guin D, Gruebele M. Rößler P, Mayer D, Tsai CJ, Veprintsev DB, Schertler GFX, Gossert AD.

Schelshorn, D., et al., Lateral allosterism in the glucagon receptor family: glucagon-like peptide 1 Wootten, D., et al., Allostery and Biased Agonism at Class B G Protein-Coupled Receptors.  

Multi-target Collaboration and License Agreement in Diabetes and Metabolic Diseases Sosei Heptares Enters R&D Treating Type 2 Diabetes and Obesity Special report 2022: Meet 20 women blazing trails in biopharma R&D

Medel-Lacruz, B., Baidya, M., Makarova, M., Mistry, R., Goulding, J., Drube, J., Hoffmann, C., Owen, D. J., & Calebiro, D. (2023). 2255.e20. https://doi.org/10.1016/j.cell.2023.04.018 Janetzko, J., Kise, R., Barsi-Rhyne, B., Siepe, D.

Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor D However, involvement of the human Mas-related G-protein coupled receptor D (MRGPRD) in the regulation

. -11.6 placebo, p<0.0001) at Week 5 (Cohen’s d effect size of 0.61).

Highlights: • The Foundry Arrives : R&D meets biotech with real-world acceleration, strategic consulting drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead

Matt Barnes appointed President of Heptares Therapeutics Ltd., and Head of UK R&D Tokyo, Japan and Cambridge

elderly (74-87 years at diagnosis), (b) male, (c) unexpectedly showed no other autoimmune diseases, (d)

Allosteric Modulator. α1-adrenoceptor ligands inhibit chemokine receptor heteromerization partners of α1B/D-adrenoceptors Endogenous l- to d-amino acid residue isomerization modulates selectivity between distinct neuropeptide