Journal ArticleDOI
ERBB receptors and cancer: the complexity of targeted inhibitors.
Nancy E. Hynes,Heidi Lane +1 more
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.read more
Citations
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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.
Journal ArticleDOI
CIP2A oncoprotein controls cell growth and autophagy through mTORC1 activation
Pietri Puustinen,Anna Rytter,Monika Mortensen,Pekka Kohonen,Pekka Kohonen,José M.A. Moreira,Marja Jäättelä +6 more
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.
Journal ArticleDOI
Targeting EGFR in non-small-cell lung cancer: lessons, experiences, strategies.
Giulia Maria Stella,Maurizio Luisetti,Simona Inghilleri,Francesca Cemmi,Roberta Scabini,Michele Zorzetto,Ernesto Pozzi +6 more
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.
Journal ArticleDOI
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
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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
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Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
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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
Dennis J. Slamon,Brian Leyland-Jones,Steven Shak,Hank Fuchs,Virginia E. Paton,Alex Bajamonde,Thomas Fleming,Wolfgang Eiermann,Janet M. Wolter,Mark D. Pegram,José Baselga,Larry Norton +11 more
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J. Guillermo Paez,Pasi A. Jänne,Pasi A. Jänne,Jeffrey C. Lee,Sean Tracy,Heidi Greulich,Heidi Greulich,Stacey Gabriel,Paula Herman,Frederic J. Kaye,Neal I. Lindeman,Titus J. Boggon,Katsuhiko Naoki,Hidefumini Sasaki,Yoshitaka Fujii,Michael J. Eck,William R. Sellers,William R. Sellers,William R. Sellers,Bruce E. Johnson,Bruce E. Johnson,Matthew Meyerson,Matthew Meyerson +22 more
TL;DR: Results suggest that EGFR mutations may predict sensitivity to gefitinib, and treatment with the EGFR kinase inhibitor gefitsinib causes tumor regression in some patients with NSCLC, more frequently in Japan.
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