signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery Nicola J Smith, Lauren T May, and Natasha L Grimsey for their work on Highlights and hot topics in GPCR research from 'Down Under' Dr.

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

., Yoo, L., Gao, Z. G., Irwin, J. J., Shoichet, B. K., & Jacobson, K. A. (2010). D., Muñoz, L. L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A., & May, L.

Neil Grimsey About Dr. Neil Grimsey " During my postdoctoral studies at USCD, I discovered a novel GPCR-dependent atypical kinase Neil Grimsey on the web LinkedIn University of Georgia Google Scholar X (Twitter) Dr.

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

Papadourakis, Konstantinos Tsianakas, Robert P Millar, Ross C Anderson, Georgios A Spyroulias, Claire L