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Journal ArticleDOI

ERBB receptors and cancer: the complexity of targeted inhibitors.

TLDR
This work discusses the significance of these receptors as clinical targets, in particular the molecular mechanisms underlying response, and many ERBB inhibitors used in the clinic.
Abstract
ERBB receptor tyrosine kinases have important roles in human cancer. In particular, the expression or activation of epidermal growth factor receptor and ERBB2 are altered in many epithelial tumours, and clinical studies indicate that they have important roles in tumour aetiology and progression. Accordingly, these receptors have been intensely studied to understand their importance in cancer biology and as therapeutic targets, and many ERBB inhibitors are now used in the clinic. We will discuss the significance of these receptors as clinical targets, in particular the molecular mechanisms underlying response.

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Journal ArticleDOI

Overcoming drug resistance to receptor tyrosine kinase inhibitors: Learning from lung cancer

TL;DR: It is necessary to first understand how receptor TKI resistance is acquired to develop strategies for overcoming resistance to TKIs, and an insight into the specific molecules or signaling pathways that mediate resistance is a key factor for understanding and overcoming acquired drug resistance.
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CIP2A oncoprotein controls cell growth and autophagy through mTORC1 activation

TL;DR: As part of a regulatory loop linking cell metabolism, growth, and proliferation, CIP2A promotes mTORC1-mediated cell growth and autophagy inhibition but is itself down-regulated by autophagic regulation.
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Targeting EGFR in non-small-cell lung cancer: lessons, experiences, strategies.

TL;DR: This review analyses the current state of the art of molecularly-tailored pharmacological approach to lung cancer, addressed to genetic lesions activating the EGFR pathway transducers, focusing on their role as markers of targeted drug response.
Journal ArticleDOI

Her2 activation mechanism reflects evolutionary preservation of asymmetric ectodomain dimers in the human EGFR family

TL;DR: Results from long-timescale molecular dynamics simulations indicating that a single ligand is necessary and sufficient to stabilize the ectodomain interface of Her2 heterodimers, which assume an asymmetric conformation similar to that of dEGFR dimers suggest a dimerization mechanism that has been conserved in the evolution of the EGFR family from Drosophila to human.
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Quercetin-induced ubiquitination and down-regulation of Her-2/neu.

TL;DR: It is observed that quercetin decreased the level of Her‐2/neu protein in time‐ and dose‐dependent manners and also inhibited the downstream survival PI3K‐Akt signaling pathway in Her‐1‐neu‐overexpressing breast cancer SK‐Br3 cells.
References
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Journal ArticleDOI

The hallmarks of cancer.

TL;DR: This work has been supported by the Department of the Army and the National Institutes of Health, and the author acknowledges the support and encouragement of the National Cancer Institute.
Journal ArticleDOI

Human breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogene

TL;DR: Amplification of the HER-2/neu gene was a significant predictor of both overall survival and time to relapse in patients with breast cancer, and had greater prognostic value than most currently used prognostic factors in lymph node-positive disease.
Journal ArticleDOI

Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib

TL;DR: A subgroup of patients with non-small-cell lung cancer have specific mutations in the EGFR gene which correlate with clinical responsiveness to the tyrosine kinase inhibitor gefitinib, and these mutations lead to increased growth factor signaling and confer susceptibility to the inhibitor.
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Use of Chemotherapy plus a Monoclonal Antibody against HER2 for Metastatic Breast Cancer That Overexpresses HER2

TL;DR: The addition of trastuzumab to chemotherapy was associated with a longer time to disease progression, a higher rate of objective response, a longer duration of response, and a lower rate of death at 1 year.
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