Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

Inhibition of activated BRAF has been ineffective in colon cancers with the mutation; here, this is shown to be due to the feedback activation of the epidermal growth factor receptor (EGFR) in response to BRAF inhibition. Inhibition of the BRAF(V600E) oncoprotein by the small-molecule drug PLX4032 (...

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Bibliographic Details
Published in:	Nature (London) Vol. 483; no. 7387; pp. 100 - 103
Main Authors:	Prahallad, Anirudh, Sun, Chong, Huang, Sidong, Di Nicolantonio, Federica, Salazar, Ramon, Zecchin, Davide, Beijersbergen, Roderick L., Bardelli, Alberto, Bernards, René
Format:	Journal Article
Language:	English
Published:	London Nature Publishing Group UK 01.03.2012 Nature Publishing Group
Subjects:	631/208/737 692/699/67/1504/1885/1393 692/700/565/1436 692/700/565/1436/1437 Animals Antibodies, Monoclonal - pharmacology Antibodies, Monoclonal, Humanized Antineoplastic agents Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Apoptosis - drug effects Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects Cetuximab Chemotherapy Colorectal Neoplasms - drug therapy Colorectal Neoplasms - enzymology Colorectal Neoplasms - genetics Colorectal Neoplasms - pathology Drug Resistance, Neoplasm - drug effects Drug Synergism Enzyme Activation - drug effects Erlotinib Hydrochloride Feedback, Physiological - drug effects Female Gastroenterology. Liver. Pancreas. Abdomen HEK293 Cells Humanities and Social Sciences Humans Indoles - pharmacology Indoles - therapeutic use Kinases letter Library collections Medical sciences Melanoma - drug therapy Melanoma - metabolism Mice multidisciplinary Pharmacology. Drug treatments Phosphorylation Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Proteins Proto-Oncogene Proteins B-raf - antagonists & inhibitors Proto-Oncogene Proteins B-raf - chemistry Proto-Oncogene Proteins B-raf - genetics Proto-Oncogene Proteins B-raf - metabolism Quinazolines - pharmacology Quinazolines - therapeutic use Receptor, Epidermal Growth Factor - agonists Receptor, Epidermal Growth Factor - antagonists & inhibitors Receptor, Epidermal Growth Factor - metabolism RNA Interference Science Science (multidisciplinary) Stomach. Duodenum. Small intestine. Colon. Rectum. Anus Studies Sulfonamides - pharmacology Sulfonamides - therapeutic use Tumors Xenograft Model Antitumor Assays Antineoplastic agent Epidermal growth factor receptor BRAF Gene Colon cancer Cancerology Established cell line Genetics Intestinal disease Protooncogene Human Rodentia Enzyme inhibitor Malignant tumor In vitro Colonic disease In vivo Vertebrata Chemotherapy Mammalia Treatment Mouse Animal C-Onc gene Digestive diseases Cancer
ISSN:	0028-0836, 1476-4687, 1476-4687
Online Access:	Get full text
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