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Targeting the epidermal growth factor receptor in solid tumor malignancies

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@article{655b9d0eba2647d29ab7b9224dfd1942,
title = "Targeting the epidermal growth factor receptor in solid tumor malignancies",
abstract = "The epidermal growth factor receptor (EGFR) is over-expressed, as well as mutated, in many types of cancers. In particular, the EGFR variant type III mutant (EGFRvIII) has attracted much attention as it is frequently and exclusively found on many tumor cells, and hence both EGFR and EGFRvIII have been proposed as valid targets in many cancer therapy settings. Different strategies have been developed in order to either inhibit EGFR/EGFRvIII activity or to ablate EGFR/EGFRvIII-positive tumor cells. Drugs that inhibit these receptors include monoclonal antibodies (mAbs) that bind to the extracellular part of EGFR, blocking the binding sites for the EGFR ligands, and intracellular tyrosine kinase inhibitors (TKIs) that block the ATP binding site of the tyrosine kinase domain. Besides an EGFRvIII-targeted vaccine, conjugated anti-EGFR mAbs have been used in different settings to deliver lethal agents to the EGFR/EGFRvIII-positive cells; among these are radio-labelled mAbs and immunotoxins. This article reviews the current status and efficacy of EGFR/EGFRvIII-targeted therapies.",
keywords = "Animals, Antibodies, Monoclonal, Humans, Molecular Targeted Therapy, Neoplasms, Protein Kinase Inhibitors, Protein-Tyrosine Kinases, Receptor, Epidermal Growth Factor",
author = "Nedergaard, {Mette K} and Hedegaard, {Chris J} and Poulsen, {Hans S}",
year = "2012",
doi = "10.2165/11599760-000000000-00000",
language = "English",
volume = "26",
pages = "83--99",
journal = "BioDrugs",
issn = "1173-8804",
publisher = "Adis International Ltd",
number = "2",

}

RIS

TY - JOUR

T1 - Targeting the epidermal growth factor receptor in solid tumor malignancies

AU - Nedergaard, Mette K

AU - Hedegaard, Chris J

AU - Poulsen, Hans S

PY - 2012

Y1 - 2012

N2 - The epidermal growth factor receptor (EGFR) is over-expressed, as well as mutated, in many types of cancers. In particular, the EGFR variant type III mutant (EGFRvIII) has attracted much attention as it is frequently and exclusively found on many tumor cells, and hence both EGFR and EGFRvIII have been proposed as valid targets in many cancer therapy settings. Different strategies have been developed in order to either inhibit EGFR/EGFRvIII activity or to ablate EGFR/EGFRvIII-positive tumor cells. Drugs that inhibit these receptors include monoclonal antibodies (mAbs) that bind to the extracellular part of EGFR, blocking the binding sites for the EGFR ligands, and intracellular tyrosine kinase inhibitors (TKIs) that block the ATP binding site of the tyrosine kinase domain. Besides an EGFRvIII-targeted vaccine, conjugated anti-EGFR mAbs have been used in different settings to deliver lethal agents to the EGFR/EGFRvIII-positive cells; among these are radio-labelled mAbs and immunotoxins. This article reviews the current status and efficacy of EGFR/EGFRvIII-targeted therapies.

AB - The epidermal growth factor receptor (EGFR) is over-expressed, as well as mutated, in many types of cancers. In particular, the EGFR variant type III mutant (EGFRvIII) has attracted much attention as it is frequently and exclusively found on many tumor cells, and hence both EGFR and EGFRvIII have been proposed as valid targets in many cancer therapy settings. Different strategies have been developed in order to either inhibit EGFR/EGFRvIII activity or to ablate EGFR/EGFRvIII-positive tumor cells. Drugs that inhibit these receptors include monoclonal antibodies (mAbs) that bind to the extracellular part of EGFR, blocking the binding sites for the EGFR ligands, and intracellular tyrosine kinase inhibitors (TKIs) that block the ATP binding site of the tyrosine kinase domain. Besides an EGFRvIII-targeted vaccine, conjugated anti-EGFR mAbs have been used in different settings to deliver lethal agents to the EGFR/EGFRvIII-positive cells; among these are radio-labelled mAbs and immunotoxins. This article reviews the current status and efficacy of EGFR/EGFRvIII-targeted therapies.

KW - Animals

KW - Antibodies, Monoclonal

KW - Humans

KW - Molecular Targeted Therapy

KW - Neoplasms

KW - Protein Kinase Inhibitors

KW - Protein-Tyrosine Kinases

KW - Receptor, Epidermal Growth Factor

U2 - 10.2165/11599760-000000000-00000

DO - 10.2165/11599760-000000000-00000

M3 - Journal article

VL - 26

SP - 83

EP - 99

JO - BioDrugs

JF - BioDrugs

SN - 1173-8804

IS - 2

ER -

ID: 36890041