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

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 (IC(50) < 1 nM) TRKA/B/C inhibitor. Pz-1 potently inhibited proliferation of human cancer cells carrying either RET- or TRKA oncoproteins (IC(50)...

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Detalles Bibliográficos
Autores principales: Moccia, Marialuisa, Yang, Donglin, Lakkaniga, Naga Rajiv, Frett, Brendan, McConnell, Nicholas, Zhang, Lingtian, Brescia, Annalisa, Federico, Giorgia, Zhang, Lingzhi, Salerno, Paolo, Santoro, Massimo, Li, Hong-yu, Carlomagno, Francesca
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8352932/
https://www.ncbi.nlm.nih.gov/pubmed/34373541
http://dx.doi.org/10.1038/s41598-021-95612-4