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

Sakmar, Debbie L. Hay, Lukas Grätz, and more. Check out some of the latest GPCR discoveries below!

., 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.

Here, we show that the gut IEL GLP-1 receptor (GLP-1R) is not required for enteroendocrine L cell GLP These data reposition key roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R

., Hunyady, L., Luttrell, L. M., & Lefkowitz, R. J. (2003). L. (2017). doi.org/10.1007/s11064-016-2026-6 Mendizabal-Zubiaga, J., Melser, S., Bénard, G., Ramos, A., Reguero, L. Z., Wilderman, A., Katakia, T., McCann, T., Yokouchi, H., Zhang, L., Corriden, R., Liu, D., Feigin, M

L., Dohlman, H. G., Frielle, T., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. C., Lundin, L. G., & Schiöth, H. B. (2003). B., Panova, O., Hilger, D., Casiraghi, M., He, F., Maul, L., Gmeiner, P., Kobilka, B.

Several integrins directly modulate VSMC contraction by regulating calcium influx through L-type voltage-gated

electron-electron resonance (DEER) spectroscopy for high-resolution conformational state determination (Wingler, L. A., et al. 1997, Bohn, L. M. et al. 1999), while dual knockout is lethal (Schmid, C. L., & Bohn, L. conformational changes for the binding to the same GPCR to mediate differential regulatory effects (Haider

transporters and their AlphaFold2 predicted water-soluble QTY variants and uncovering the natural mutations of L- >Q, I->T, F->Y and Q->L, T->I and Y->F Industry News Sosei Heptares Doses First Subject in Phase 1 Trial

Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the range of μg/L In nematodes, exposure to PS-NPs (1-100 μg/L) significantly altered transcriptional expressions of some

., Hunyady, L., Luttrell, L. M., & Lefkowitz, R. J. (2003).

A study published in Scientific Data by Arne Hansen et a l has introduced a sensitive method for detecting

mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system, L-glutamate

mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system, L-glutamate

Ji, et al. 2020; L. Wan, 2020). when mGluR2 dimers are inactive, switching to an interface mainly at TM6 when the receptor is active (L.

Point mutations are in the C-tail of PAR4 PH-binding domain; F347 L and D349A, but not E346A, abrogate

and dopamine D2 receptor is required for selective potentiation of dopamine D2 receptor function by L- disease-associated LPA6 missense mutants and a potential pharmacoperone therapy for autosomal recessive woolly hair

cilium initiate SMOOTHENED-PKA signaling in the Hedgehog cascade Allatotropin (AT) related peptides L-ATRP

Bryan L Roth study on Illuminating the understudied GPCR-ome Save the dates: February 8 - 29: Dr.

Structural and Molecular Insights into GPCR Function Endogenous l- to d-amino acid residue isomerization

kinases – a potential pathway for GPCR-targeted drug discovery Nicola J Smith, Lauren T May, and Natasha L

Zhang, and L. Ma. 2008.

Binding of Stalk-derived Peptide Agonists GPCR Binders, Drugs, and more In silico exploration of 4(α-l-rhamnosyloxy

HDAC3 inhibition to activate autophagy in head kidney macrophages from turbot (Scophthalmus maximus L.

Endogenous l- to d-amino acid residue isomerization modulates selectivity between distinct neuropeptide

Katharina Grotsch, Bryan L Roth, Valery V Fokin  et al. for their research on Virtual Screening of a

L., & Garcia, K. C. (2015). Structural biology.

November 2021 "Nov. 15, 2021 LONDON – There’s not yet proof of the pudding, 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 protein targets. The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute carriers, are relevant to immunology indications and rare diseases with high unmet need." Read more at the source #DrGPCR #GPCR #IndustryNews