Department of Pathology, University of Kansas Medical Center, Kansas City, KS 66160, USA.
Proc Natl Acad Sci U S A. 2010 Sep 21;107(38):16619-24. doi: 10.1073/pnas.1010722107. Epub 2010 Sep 7.
The Notch signaling pathway plays an important role in cellular proliferation, differentiation, and apoptosis. Unregulated activation of Notch signaling can result in excessive cellular proliferation and cancer. Human T-cell leukemia virus type 1 (HTLV-I) is the etiological agent of adult T-cell leukemia (ATL). The disease has a dismal prognosis and is invariably fatal. In this study, we report a high frequency of constitutively activated Notch in ATL patients. We found activating mutations in Notch in more than 30% of ATL patients. These activating mutations are phenotypically different from those previously reported in T-ALL leukemias and may represent polymorphisms for activated Notch in human cancers. Compared with the exclusive activating frameshift mutations in the proline, glutamic acid, serine, and threonine (PEST) domain in T-ALLs, those in ATLs have, in addition, single-substitution mutations in this domain leading to reduced CDC4/Fbw7-mediated degradation and stabilization of the intracellular cleaved form of Notch1 (ICN1). Finally, we demonstrated that inhibition of Notch signaling by γ-secretase inhibitors reduced tumor cell proliferation and tumor formation in ATL-engrafted mice. These data suggest that activated Notch may be important to ATL pathogenesis and reveal Notch1 as a target for therapeutic intervention in ATL patients.
Notch 信号通路在细胞增殖、分化和凋亡中发挥着重要作用。 Notch 信号的不受调控的激活可导致细胞过度增殖和癌症。人类 T 细胞白血病病毒 1 型(HTLV-I)是成人 T 细胞白血病(ATL)的病因。该疾病预后不良,且总是致命的。在这项研究中,我们报告了 ATL 患者中 Notch 持续激活的高频率。我们发现,超过 30%的 ATL 患者存在 Notch 的激活突变。这些激活突变与先前在 T-ALL 白血病中报道的突变不同,可能代表人类癌症中激活 Notch 的多态性。与 T-ALL 中仅有的脯氨酸、谷氨酸、丝氨酸和苏氨酸(PEST)结构域的框移激活突变相比,ATL 中的突变除了导致 CDC4/Fbw7 介导的 Notch1 (ICN1)胞内裂解形式的降解减少和稳定性增加之外,还存在单一取代突变。最后,我们证明了 Notch 信号通路的抑制通过 γ-分泌酶抑制剂减少了 ATL 移植小鼠中的肿瘤细胞增殖和肿瘤形成。这些数据表明,激活的 Notch 可能对 ATL 的发病机制很重要,并揭示了 Notch1 作为 ATL 患者治疗干预的靶标。