Cancer-Associated Mutations Enhance The Sensitivity Of The Trupath GαQ/11 System

Cancer-Associated Mutations Enhance The Sensitivity Of The Trupath GαQ/11 SystemGPCR Target: HEK293T cells overexpressing full-length GIPR or GLP-1R with an N-terminal FLAG tag were purchased from Multispan, IncAuthors: Dewi Safitri,…

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New quinolone derivatives as neuropeptide S receptor antagonists: Design, synthesis, homology modeling, dynamic simulations and modulation of Gq/Gs signaling pathways.

New quinolone derivatives as neuropeptide S receptor antagonists: Design, synthesis, homology modeling, dynamic simulations and modulation of Gq/Gs signaling pathways.GPCR Target: Calcium assay, cAMP assayAuthors: Batran RZ, Gugnani KS, Maher…

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Distinct biological activities of isomers from several families of branched fatty acid esters of hydroxy fatty acids (FAHFAs). 

Distinct biological activities of isomers from several families of branched fatty acid esters of hydroxy fatty acids (FAHFAs). GPCR Target: Calcium assayAuthors: Aryal P, Syed I, Lee J, Patel R, Nelson…

Continue ReadingDistinct biological activities of isomers from several families of branched fatty acid esters of hydroxy fatty acids (FAHFAs). 

Preferential Gs protein coupling of the galanin Gal1 receptor in the µ-opioid-Gal1 receptor heterotetramer

Preferential Gs protein coupling of the galanin Gal1 receptor in the µ-opioid-Gal1 receptor heterotetramerGPCR Target: CHO-K1-Gαqi5 Gal1RAuthors: Paulo A. De Oliveira, Estefanía Moreno, Nil Casajuana-Martin, Verònica Casadó-Anguera, Ning-Sheng Cai, Gisela…

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In vitro pharmacological profile of PHA-022121, a small molecule bradykinin B2 receptor antagonist in clinical development

In vitro pharmacological profile of PHA-022121, a small molecule bradykinin B2 receptor antagonist in clinical developmentGPCR Target: Antagonist potencies of test items at recombinant dog, rabbit, rat and mouse bradykinin B2 receptors…

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A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal models

A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal modelsGPCR Target: The transfected Chinese hamster ovary-K1 (CHO-K1) Gaqi5 cells with stable S1P1 expression, hS1P1-CHO,Authors: Jing Jin, Nina Xue, Yuan…

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Predictive models to identify small molecule activators and inhibitors of opioid receptors

Predictive models to identify small molecule activators and inhibitors of opioid receptorsGPCR Target: The CHO-K1 cells that express full-length human recombinant μ-, κ-, and δ-OPRs (HMOR, HKOR, and HDOR respectively)Authors:…

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A novel luminescence-based β-arrestin recruitment assay for unmodified receptors.

A novel luminescence-based β-arrestin recruitment assay for unmodified receptorsGPCR Target: CHOK1 stable cell lines, the human MOR, KOR, DOR, and NOP were all inserted into the pMEX2 vector from Multispan…

Continue ReadingA novel luminescence-based β-arrestin recruitment assay for unmodified receptors.