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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

Quantitative prediction of fold resistance for inhibitors of EGFR.

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

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

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.

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.
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.
Journal ArticleDOI

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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