Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases

Abstract We have recently described Pz-1, a benzimidazole-based type-2 RET and VEGFR2 inhibitor. Based on a kinome scan, here we show that Pz-1 is also a potent (IC50 < 1 nM) TRKA/B/C inhibitor. Pz-1 potently inhibited proliferation of human cancer cells carrying either RET- or TRKA oncoproteins...

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Auteurs principaux: Marialuisa Moccia, Donglin Yang, Naga Rajiv Lakkaniga, Brendan Frett, Nicholas McConnell, Lingtian Zhang, Annalisa Brescia, Giorgia Federico, Lingzhi Zhang, Paolo Salerno, Massimo Santoro, Hong-yu Li, Francesca Carlomagno
Format: article
Langue:EN
Publié: Nature Portfolio 2021
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Accès en ligne:https://doaj.org/article/eab71864d5a542ee8748ff9464f7f61c
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