Lapatinib: functional genomics study leads to insights into mechanism of action.

Gilmer TM

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Lapatinib: functional genomics study leads to insights into mechanism of action.

机译：拉帕替尼：功能基因组学研究可深入了解作用机理。

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The epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor-2 (HER2) have been intensely scrutinized as therapeutic targets in cancer because of the relationship between overexpression of these receptors and poor prognosis. In general, targeting EGFR or HER2 can be accomplished with antibodies directed against the receptor extracellular domains or with small-molecule inhibitors of the intracellular tyro-sine kinase domains. Although both strategies have been clinically promising, considerable variability in efficacy has also been noted; this raises important questions about the molecular basis for drug responsiveness. Moreover, an improved understanding of the mechanisms of action of agents that target the HER family may open new avenues of research into therapeutic resistance and offer patients additional treatment options.

机译：表皮生长因子受体（EGFR）和人表皮生长因子受体2（HER2）已被严格审查为癌症的治疗靶标，因为这些受体的过表达与不良预后之间存在关联。通常，靶向EGFR或HER2的靶向可以通过针对受体胞外域的抗体或细胞内酪氨酸激酶域的小分子抑制剂来实现。尽管两种策略在临床上都很有希望，但疗效也存在很大差异。这引起了有关药物反应性的分子基础的重要问题。而且，对靶向HER家族的药物作用机理的进一步了解可能为治疗耐药性开辟新的研究途径，并为患者提供其他治疗选择。

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《Molecular cancer therapeutics》 |2011年第11期|共1页
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Gilmer TM;
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1. Lapatinib: functional genomics study leads to insights into mechanism of action. [J] . Gilmer TM Molecular cancer therapeutics . 2011,第11期

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Lapatinib: functional genomics study leads to insights into mechanism of action.

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