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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

Cancer Genome Landscapes

TL;DR: This work has revealed the genomic landscapes of common forms of human cancer, which consists of a small number of “mountains” (genes altered in a high percentage of tumors) and a much larger number of "hills" (Genes altered infrequently).
Journal ArticleDOI

Matrix Metalloproteinases: Regulators of the Tumor Microenvironment

TL;DR: In addition to their role in extracellular matrix turnover and cancer cell migration, MMPs regulate signaling pathways that control cell growth, inflammation, or angiogenesis and may even work in a nonproteolytic manner.
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Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer

TL;DR: Panitumumab monotherapy efficacy in mCRC is confined to patients with WT KRAS tumors, and KRAS status should be considered in selecting patients withmCRC as candidates for panitumuab mon Therapy.
References
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Journal ArticleDOI

Tyrosine kinases as targets in cancer therapy - successes and failures.

TL;DR: The preclinical and clinical status of low molecular weight drugs targeted against different tyrosine kinases, briefly describes new targets, and provides a critical analysis of the current situation in the area of tyosine kinase inhibitors.
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Molecular mechanisms underlying IGF-I-induced attenuation of the growth-inhibitory activity of trastuzumab (Herceptin) on SKBR3 breast cancer cells

TL;DR: The results provide an example of resistance to an antineoplastic therapy that targets one tyrosine kinase receptor by increased signal transduction through an alternative pathway in a complex regulatory network.
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The development and clinical use of trastuzumab (Herceptin).

TL;DR: The benefit of trastuzumab is generally confined to patients whose tumours have gene amplification as detected by fluorescence in situ hybridisation (FISH) and this is tightly associated with immunohistochemical staining at the highest (3+) level, but there is emerging evidence that a three-weekly regimen may be as effective.
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A mutant epidermal growth factor receptor with defective protein tyrosine kinase is unable to stimulate proto-oncogene expression and DNA synthesis.

TL;DR: EGF was unable to stimulate the stimulation of various responses, including enhanced expression of proto-oncogenes c-fos and c-myc, morphological changes, and stimulation of DNA synthesis, suggesting that the tyrosine kinase activity is essential for EGF receptor signal transduction.
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Monoclonal antibodies against receptor for epidermal growth factor induce early and delayed effects of epidermal growth factor.

TL;DR: Observations support the notion that the biological information of the EGF-receptor complex resides in the membrane receptor, and the antibodies offer a powerful tool to study the structure, processing, and mode of action of EGF receptors.
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