Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

An allosteric inhibitor, EAI045, is reported that is selective for certain drug-resistant EGFR mutants, but spares the wild-type receptor; combination therapy of EAI045 with EGFR-dimerization-blocking antibodies is effective in mouse models of lung cancer driven by mutant versions of EGFR that are r...

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Bibliographic Details
Published in:	Nature (London) Vol. 534; no. 7605; pp. 129 - 132
Main Authors:	Jia, Yong, Yun, Cai-Hong, Park, Eunyoung, Ercan, Dalia, Manuia, Mari, Juarez, Jose, Xu, Chunxiao, Rhee, Kevin, Chen, Ting, Zhang, Haikuo, Palakurthi, Sangeetha, Jang, Jaebong, Lelais, Gerald, DiDonato, Michael, Bursulaya, Badry, Michellys, Pierre-Yves, Epple, Robert, Marsilje, Thomas H., McNeill, Matthew, Lu, Wenshuo, Harris, Jennifer, Bender, Steven, Wong, Kwok-Kin, Jänne, Pasi A., Eck, Michael J.
Format:	Journal Article
Language:	English
Published:	London Nature Publishing Group UK 02.06.2016 Nature Publishing Group
Subjects:	13/1 42/109 49/47 59/36 631/154 631/535/1266 631/67 631/67/1612/1350 631/92/275 64/110 82 82/83 96/95 Allosteric Regulation - drug effects Allosteric Site - drug effects Animals Antineoplastic Agents - pharmacology ATP Benzeneacetamides - pharmacology Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - enzymology Carcinoma, Non-Small-Cell Lung - pathology Cell Line, Tumor Cell Proliferation - drug effects Cetuximab - pharmacology Disease Models, Animal Drug Resistance, Multiple - drug effects Drug Resistance, Multiple - genetics Drug Resistance, Neoplasm - drug effects Drug Resistance, Neoplasm - genetics Drug Synergism Enzyme kinetics Epidermal growth factor ErbB Receptors - antagonists & inhibitors ErbB Receptors - chemistry ErbB Receptors - genetics ErbB Receptors - metabolism Humanities and Social Sciences Inhibitors Kinases letter Lung cancer Lung Neoplasms - drug therapy Lung Neoplasms - enzymology Lung Neoplasms - pathology Mice multidisciplinary Mutant Proteins - antagonists & inhibitors Mutant Proteins - chemistry Mutant Proteins - genetics Mutant Proteins - metabolism Mutants Mutation NMR Nuclear magnetic resonance Phosphorylation Protein Conformation - drug effects Protein Kinase Inhibitors - pharmacology Protein Multimerization - drug effects Science Studies Thiazoles - pharmacology Tumors
ISSN:	0028-0836, 1476-4687, 1476-4687
Online Access:	Get full text
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