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...

Descripción completa

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
_version_ 1783230670744584192
author Mikula, Hannes
Stapleton, Shawn
Kohler, Rainer H.
Vinegoni, Claudio
Weissleder, Ralph
author_facet Mikula, Hannes
Stapleton, Shawn
Kohler, Rainer H.
Vinegoni, Claudio
Weissleder, Ralph
author_sort Mikula, Hannes
collection PubMed
description 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.
format Online
Article
Text
id pubmed-5399591
institution National Center for Biotechnology Information
language English
publishDate 2017
publisher Ivyspring International Publisher
record_format MEDLINE/PubMed
spelling pubmed-53995912017-04-21 Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging Mikula, Hannes Stapleton, Shawn Kohler, Rainer H. Vinegoni, Claudio Weissleder, Ralph Theranostics Research Paper 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. Ivyspring International Publisher 2017-03-06 /pmc/articles/PMC5399591/ /pubmed/28435463 http://dx.doi.org/10.7150/thno.18238 Text en © Ivyspring International Publisher This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) license (https://creativecommons.org/licenses/by-nc/4.0/). See http://ivyspring.com/terms for full terms and conditions.
spellingShingle Research Paper
Mikula, Hannes
Stapleton, Shawn
Kohler, Rainer H.
Vinegoni, Claudio
Weissleder, Ralph
Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
title Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
title_full Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
title_fullStr Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
title_full_unstemmed Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
title_short Design and Development of Fluorescent Vemurafenib Analogs for In Vivo Imaging
title_sort design and development of fluorescent vemurafenib analogs for in vivo imaging
topic Research Paper
url 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
work_keys_str_mv AT mikulahannes designanddevelopmentoffluorescentvemurafenibanalogsforinvivoimaging
AT stapletonshawn designanddevelopmentoffluorescentvemurafenibanalogsforinvivoimaging
AT kohlerrainerh designanddevelopmentoffluorescentvemurafenibanalogsforinvivoimaging
AT vinegoniclaudio designanddevelopmentoffluorescentvemurafenibanalogsforinvivoimaging
AT weisslederralph designanddevelopmentoffluorescentvemurafenibanalogsforinvivoimaging

Ejemplares similares