HER3, serious partner in crime: therapeutic approaches and potential biomarkers for effect of HER3-targeting.

作者: Arjan Kol , Anton G.T. Terwisscha van Scheltinga , Hetty Timmer-Bosscha , Laetitia E. Lamberts , Frederike Bensch

DOI: 10.1016/J.PHARMTHERA.2014.01.005

关键词:

摘要: The human epidermal growth factor receptor (HER) family members are targeted by a growing numbers of small molecules and monoclonal antibodies. Resistance against the (EGFR) HER2-targeting agents is clinically relevant problem forcing research on optimizing targeting HER family. In view its overexpression in tumors, compensatory role signaling, HER3 has gained much interest as potential additional target within It only member lacking intrinsic tyrosine kinase activity therefore cancer long been underestimated. Drugs that block or interfere with dimer including fully anti-HER3 antibodies, bispecific antibodies inhibitors (TKIs), currently becoming available. Several compounds have already entered clinical trial. meantime biomarkers tested such tumor analysis expression, functional assays for downstream effector molecular imaging techniques. This review describes biology relevance cancer, effect HER3-targeting.

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