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用于成像的荧光维莫非尼类似物的设计与开发。

Design and Development of Fluorescent Vemurafenib Analogs for Imaging.

作者信息

Mikula Hannes, Stapleton Shawn, Kohler Rainer H, Vinegoni Claudio, Weissleder Ralph

机构信息

Center for Systems Biology, Massachusetts General Hospital, 185 Cambridge Street, CPZN 5206, Boston, MA, 02114, USA.

Department of Systems Biology, Harvard Medical School, 200 Longwood Ave, Boston, MA, 02115, USA.

出版信息

Theranostics. 2017 Mar 6;7(5):1257-1265. doi: 10.7150/thno.18238. eCollection 2017.

DOI:10.7150/thno.18238
PMID:28435463
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5399591/
Abstract

Herein we describe fluorescent derivatives of vemurafenib to probe therapeutic BRAF inhibition in live cells and . 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 non-resistant and resistant melanoma tumors.

摘要

在此，我们描述了维罗非尼的荧光衍生物，用于在活细胞中探究治疗性BRAF抑制作用。通过测定靶点结合、对突变型BRAF黑色素瘤细胞系的抑制作用以及活细胞成像，对这些化合物进行了评估和比较。我们表明，维罗非尼-硼二吡咯是一种卓越的成像药物，可在活细胞以及非耐药和耐药黑色素瘤肿瘤中可视化维罗非尼的靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/0ecadddf65d9/thnov07p1257g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/392b189a0a51/thnov07p1257g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/fd9ab727c474/thnov07p1257g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/c344c2ed1b1d/thnov07p1257g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/0ecadddf65d9/thnov07p1257g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/392b189a0a51/thnov07p1257g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/fd9ab727c474/thnov07p1257g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/c344c2ed1b1d/thnov07p1257g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a8ed/5399591/0ecadddf65d9/thnov07p1257g004.jpg

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