Targeting SH2 domains in breast cancer.

Targeting SH2 domains in breast cancer.
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DOI:
10.4155/fmc.14.120
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发表时间:
2014
影响因子:
4.2
通讯作者:
McMurray JS
McMurray JS
中科院分区:
医学3区
文献类型:
--
作者:
Morlacchi P;Robertson FM;Klostergaard J;McMurray JS

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乳腺癌是世界范围内女性最常见的癌症类型之一,也是美国癌症相关疾病的第二大原因。SH2结构域将信号蛋白招募到异常激活的生长因子和细胞因子受体上的磷酸酪氨酸残基上,参与癌细胞循环、转移、血管生成等过程。在此,我们回顾了针对Grb2、Grb7和STAT3的SH2结构域的磷酸肽模拟和小分子方法,这些方法抑制了它们的靶点并减少了体外乳腺癌模型中的增殖。只有STAT3抑制剂在体内模型中被评估并导致肿瘤减少。综上所述,这些研究表明靶向SH2结构域是治疗乳腺癌的重要途径。
Breast cancer is among the most commonly diagnosed cancer types in women worldwide and is the second leading cause of cancer-related disease in the USA. SH2 domains recruit signaling proteins to phosphotyrosine residues on aberrantly activated growth factor and cytokine receptors and contribute to cancer cell cycling, metastasis, angiogenesis and so on. Herein we review phosphopeptide mimetic and small-molecule approaches targeting the SH2 domains of Grb2, Grb7 and STAT3 that inhibit their targets and reduce proliferation in in vitro breast cancer models. Only STAT3 inhibitors have been evaluated in in vivo models and have led to tumor reduction. Taken together, these studies suggest that targeting SH2 domains is an important approach to the treatment of breast cancer.
DOI: 10.1186/bcr1680
发表时间: 2007
期刊: Breast cancer research : BCR
影响因子: --
作者:
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