Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2

Natalia V. Ortiz Zacarı́as, Jacobus P. D. van Veldhoven, Laura Portner, E. van Spronsen, Salviana Ullo, Margo Veenhuizen, Wijnand J. C. van der Velden, Annelien J.M. Zweemer, Roy M. Kreekel, Kenny Oenema,

Journal of Medicinal Chemistry · 2018 · 43 citations · 42 references

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Abstract

S]GTPγS assay revealed that they act as inverse agonists in CCR1, providing a new manner of pharmacological modulation. Thus, this intracellular binding site enables the design of selective and multitarget inhibitors as a novel therapeutic approach.

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