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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Quantitative prediction of fold resistance for inhibitors of EGFR.
Trent E. Balius,Robert C. Rizzo +1 more
TL;DR: The present results indicate that drug resistance more likely involves disruption of favorable interactions, including a water-mediated H-bond network between the ligands and residues T854, T790, and Q791, which could have important implication for guiding rational design of inhibitors with improved resistance profiles.
Journal ArticleDOI
Membranous expression of her3 is associated with a decreased survival in head and neck squamous cell carcinoma
Mikiko Takikita,Ran Xie,Joon-Yong Chung,Hanbyoul Cho,Kris Ylaya,Seung-Mo Hong,Christopher A. Moskaluk,Stephen M. Hewitt +7 more
TL;DR: It is suggested that membranous Her3 expression is strongly associated with poor prognosis of patients with HNSCC and is a potential candidate molecule for targeted therapy.
Journal ArticleDOI
ErbB Receptors in the Biology and Pathology of the Aerodigestive Tract
Sarah Morgan,Jennifer R. Grandis +1 more
TL;DR: Cetuximab was FDA approved in 2006 for treatment of SCCHN and the signaling pathways of EGFR are explored, underscoring the importance of understanding the biology of these malignancies.
Journal ArticleDOI
Reduction-sensitive liposomes from a multifunctional lipid conjugate and natural phospholipids: reduction and release kinetics and cellular uptake.
Björn Goldenbogen,Nicolai Brodersen,Andrea Gramatica,Martin Loew,Jürgen Liebscher,Andreas Herrmann,Holger Egger,Bastian Budde,Anna Arbuzova +8 more
TL;DR: Reduction-sensitive liposomes composed of a novel multifunctional lipidlike conjugate, containing a disulfide bond and a biotin moiety, and natural phospholipids are reported on, implying the potential of using this system for active targeting and delivery.
Journal ArticleDOI
Drug Resistance Mechanisms in Non-Small Cell Lung Carcinoma.
TL;DR: Molecular mechanisms that are potential drivers of resistance in non-small cell lung carcinoma are examined, which include resistance to molecular targeted therapies as well as conventional chemotherapy through the activity of multidrug resistance proteins.
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.
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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
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EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy.
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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