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An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases

Abstract : Methyl 9-anilinothiazolo[5,4-f]quinazoline-2-carbimidates 1 (EHT 5372) and 2 (EHT 1610) are strong inhibitors of DYRK’s family kinases. The crystal structures of the complex revealed a noncanonical binding mode of compounds 1 and 2 in DYRK2, explaining the remarkable selectivity and potency of these inhibitors. The structural data and comparison presented here provide therefore a template for further improvement of this inhibitor class and for the development of novel inhibitors selectively targeting DYRK kinases.
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https://hal-normandie-univ.archives-ouvertes.fr/hal-02046195
Contributor : Madeleine Roux-Merlin <>
Submitted on : Friday, February 22, 2019 - 3:36:22 PM
Last modification on : Thursday, July 2, 2020 - 3:28:58 AM

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A. Chaikuad, J. Diharce, M. Schröder, Alicia Foucourt, B. Leblond, et al.. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. Journal of Medicinal Chemistry, American Chemical Society, 2016, 59 (22), pp.10315-10321. ⟨10.1021/acs.jmedchem.6b01083⟩. ⟨hal-02046195⟩

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