Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging

Herein we describe fluorescent derivatives of vemurafenib to probe therapeutic BRAF inhibition in live cells and in vivo. The compounds were evaluated and compared by determining target binding, inhibition of mutant BRAF melanoma cell lines and live cell imaging. We show that vemurafenib-BODIPY is a...

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Detalles Bibliográficos
Autores principales: Mikula, Hannes, Stapleton, Shawn, Kohler, Rainer H., Vinegoni, Claudio, Weissleder, Ralph
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Ivyspring International Publisher 2017
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5399591/
https://www.ncbi.nlm.nih.gov/pubmed/28435463
http://dx.doi.org/10.7150/thno.18238
Descripción
Sumario:Herein we describe fluorescent derivatives of vemurafenib to probe therapeutic BRAF inhibition in live cells and in vivo. The compounds were evaluated and compared by determining target binding, inhibition of mutant BRAF melanoma cell lines and live cell imaging. We show that vemurafenib-BODIPY is a superior imaging drug to visualize the targets of vemurafenib in live cells and in vivo in non-resistant and resistant melanoma tumors.

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