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Melanoma adapts to RAF/MEK inhibitors through FOXD3-mediated upregulation of ERBB3
Journal article   Open access   Peer reviewed

Melanoma adapts to RAF/MEK inhibitors through FOXD3-mediated upregulation of ERBB3

Ethan V. Abel, Kevin J. Basile, Curtis H. Kugel, Agnieszka K. Witkiewicz, Kaitlyn Le, Ravi K. Amaravadi, Giorgos C. Karakousis, Xiaowei Xu, Wei Xu, Lynn M. Schuchter, …
The Journal of clinical investigation, v 123(5), pp 2155-2168
01 May 2013
PMID: 23543055
url
https://doi.org/10.1172/jci65780View
Published, Version of Record (VoR)Maybe Open Access (Publisher Bronze) Open

Abstract

Life Sciences & Biomedicine Medicine, Research & Experimental Research & Experimental Medicine Science & Technology
The mechanisms underlying adaptive resistance of melanoma to targeted therapies remain unclear. By combining ChIP sequencing with microarray-based gene profiling, we determined that ERBB3 is upregulated by FOXD3, a transcription factor that promotes resistance to RAF inhibitors in melanoma. Enhanced ERBB3 signaling promoted resistance to RAF pathway inhibitors in cultured melanoma cell lines and in mouse xenograft models. ERBB3 signaling was dependent on ERBB2; targeting ERBB2 with lapatinib in combination with the RAF inhibitor PLX4720 reduced tumor burden and extended latency of tumor regrowth in vivo versus PLX4720 alone. These results suggest that enhanced ERBB3 signaling may serve as a mechanism of adaptive resistance to RAF and MEK inhibitors in melanoma and that cotargeting this pathway may enhance the clinical efficacy and extend the therapeutic duration of RAF inhibitors.

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210 citations in Scopus

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Collaboration types
Domestic collaboration
Web of Science research areas
Medicine, Research & Experimental
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