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Main objectives: - Learning how to perform advanced GPCR pharmacology data analysis in support of drug

September 2022 "The diamondback moth (Plutella xylostella) is one of the most destructive lepidopteran pests of cruciferous vegetables, and insights into regulation of its physiological processes contribute towards the development of new pesticides against it. Thus, we investigated the regulatory functions of its β-adrenergic-like octopamine receptor (PxOctβ3). The open reading frame (ORF) of PxOctβ3 was phylogenetically analyzed, and the levels of expression of the receptor mRNA were determined. This ORF was also cloned and expressed in HEK-293 cells. A series of octopamine receptor agonists and antagonists were tested against PxOctβ3. We showed that the receptor is a member of the Octβ3 protein family, and an analysis using quantitative PCR showed that it was expressed at all developmental stages of P. xylostella. Octopamine activated PxOctβ3, resulting in increased levels of intracellular cAMP. Furthermore, the agonists naphazoline, clonidine, 2-phenethylamine, and amitraz activated the PxOctβ3 receptor, and naphazoline was the most effective. Only metoclopramide and mianserin had significant antagonistic effects on PxOctβ3, whereas yohimbine, phentolamine, and chlorpromazine lacked obvious antagonistic effects. The injection of double-stranded RNA in an RNA interference assay indicated that PxOctβ3 regulates development in P. xylostella. This study demonstrated the pharmacological properties and functions of PxOctβ3 in P. xylostella, thus, providing a theoretical basis for the design of pesticides that target octopamine receptors." Read more at the source #DrGPCR #GPCR #IndustryNews

Principles of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate Binding of Stalk-derived Peptide Agonists GPCR Binders, Drugs, and more In silico exploration of 4(α-l-rhamnosyloxy Dynamic nature of G-protein coupled receptors Septerna Secures $150 Million in Series B Financing to Advance

September 2022 "Background G protein-coupled receptor (GPCR) is the most targeted protein family by the FDA-approved drugs. GPCR-kinase 3 (GRK3) is critical for GPCR signaling. Our genomic analysis showed that GRK3 expression correlated with poor prognosis of gastric adenocarcinoma (GAC) patients. However, GRK3’s functions and clinical utility in GAC progression and metastases are unknown. Methods We studied GRK3 expression in normal, primary, and metastatic GAC tissues. We identified a novel GRK3 inhibitor, LD2, through a chemical-library screen. Through genetic and pharmacologic modulations of GRK3, a series of functional and molecular studies were performed in vitro and in vivo. Impact of GRK3 on YAP1 and its targets was determined." Read more at the source #DrGPCR #GPCR #IndustryNews

Contest Committee Sponsors GPCR Retreat Program < Back to schedule Cannabinoid compounds to augment L-DOPA

Daniel Kahne and Suzanne Walker studying the structure and function of the essential human enzyme, O-GlcNAc Olympiad Journey John shared his experiences in high school, where he developed a keen interest in advanced Journey John shared his experience with the Chemistry Olympiad program, highlighting its rigorousness and advanced Scientific Journey and Lab Collaboration John discussed his scientific journey, starting with a project in Suzanne He then moved to Dan's lab where he met Suzanne and her project.

forms, specifically the short and long forms of the stimulatory G protein, Galpha-s(s) and Galpha-s(l) We demonstrated that Galpha-s(l), but not Galpha-s(s), regulates extracellularly regulated kinases (ERK We speculate that these aberrations in Galpha-s(l), specifically, may be involved in other pathologies