CEINGE Biotecnologie Avanzate, Naples, Italy.
Blood. 2011 Sep 29;118(13):3634-44. doi: 10.1182/blood-2011-03-341073. Epub 2011 Aug 5.
We prove that the SH2-containing tyrosine phosphatase 1 (SHP-1) plays a prominent role as resistance determinant of imatinib (IMA) treatment response in chronic myelogenous leukemia cell lines (sensitive/KCL22-S and resistant/KCL22-R). Indeed, SHP-1 expression is significantly lower in resistant than in sensitive cell line, in which coimmunoprecipitation analysis shows the interaction between SHP-1 and a second tyrosine phosphatase SHP-2, a positive regulator of RAS/MAPK pathway. In KCL22-R SHP-1 ectopic expression restores both SHP-1/SHP-2 interaction and IMA responsiveness; it also decreases SHP-2 activity after IMA treatment. Consistently, SHP-2 knocking-down in KCL22-R reduces either STAT3 activation or cell viability after IMA exposure. Therefore, our data suggest that SHP-1 plays an important role in BCR-ABL-independent IMA resistance modulating the activation signals that SHP-2 receives from both BCR/ABL and membrane receptor tyrosine kinases. The role of SHP-1 as a determinant of IMA sensitivity has been further confirmed in 60 consecutive untreated patients with chronic myelogenous leukemia, whose SHP-1 mRNA levels were significantly lower in case of IMA treatment failure (P < .0001). In conclusion, we suggest that SHP-1 could be a new biologic indicator at baseline of IMA sensitivity in patients with chronic myelogenous leukemia.
我们证明了含有 SH2 结构域的酪氨酸磷酸酶 1(SHP-1)在慢性髓系白血病细胞系(敏感/KCL22-S 和耐药/KCL22-R)的伊马替尼(IMA)治疗反应的耐药决定因素中起着重要作用。事实上,耐药细胞系中 SHP-1 的表达明显低于敏感细胞系,共免疫沉淀分析显示 SHP-1 与第二种酪氨酸磷酸酶 SHP-2 相互作用,SHP-2 是 RAS/MAPK 途径的正调节剂。在 KCL22-R 中,SHP-1 的异位表达恢复了 SHP-1/SHP-2 的相互作用和 IMA 的反应性;它还降低了 IMA 处理后的 SHP-2 活性。一致地,在 KCL22-R 中敲低 SHP-2 会降低 IMA 暴露后 STAT3 的激活或细胞活力。因此,我们的数据表明 SHP-1 在 BCR-ABL 独立的 IMA 耐药中发挥重要作用,调节 SHP-2 从 BCR/ABL 和膜受体酪氨酸激酶接收到的激活信号。SHP-1 作为 IMA 敏感性决定因素的作用在 60 例连续未经治疗的慢性髓系白血病患者中得到进一步证实,其 SHP-1 mRNA 水平在 IMA 治疗失败的情况下明显降低(P <.0001)。总之,我们建议 SHP-1 可以作为慢性髓系白血病患者 IMA 敏感性的基线新的生物学指标。