Yu Fei-Yan, Hong Ying-Ying, Qu Jia-Fei, Chen Feng, Li Tie-Jun
Department of Oral Pathology, Peking University School and Hospital of Stomatology, Haidian District, Beijing 100081, P.R. China.
Central Laboratory, Peking University School and Hospital of Stomatology, Haidian District, Beijing 100081, P.R. China.
Int J Mol Med. 2014 Aug;34(2):507-12. doi: 10.3892/ijmm.2014.1783. Epub 2014 May 16.
Mutations in the transmembrane receptor patched homolog 1 (Homo sapiens) (ptch1) are responsible for nevoid basal cell carcinoma syndrome (NBCCS), an autosomal dominant disorder that causes developmental abnormalities and predisposes the affected individuals to cancer. Many of these mutations, including mutations in the C-terminus of the large intracellular loop (ICL) of ptch1 (p.C727VfsX745 and p.S733IfsX736), result in the premature truncation of the protein. The ptch1‑C727VfsX745 and ptch1-S733IfsX736 mutations have been identified in patients with NBCCS‑associated keratocystic odontogenic tumors (KCOTs). In the present study, we found that the molecular mechanisms regulated by the non-canonical Hedgehog (Hh) signaling pathway through cyclin B1 are involved in the pathogenesis of NBCCS-associated KCOTs. In contrast to wild-type ptch1, ptch1-C727VfsX745 and ptch1‑S733IfsX736 clearly exhibited reduced binding to cyclin B1. Moreover, the cells expressing these two mutations demonstrated an increase in cell cycle progression and these two mutation constructs failed to inhibit cell proliferation. In addition, the mutants enhanced the activity of glioma-associated oncogene family zinc finger 1 (GLI1), a downstream reporter of Hh signaling. Thus, our data suggest that the non-canonical Hh pathway mediated through ptch1 and cyclin B1 is involved in the pathogenesis of NBCCS-associated KCOTs. The C-terminus of ICL in ptch1 may also be a potential therapeutic target in the treatment of this disease.
跨膜受体patched同源物1(智人)(ptch1)的突变是痣样基底细胞癌综合征(NBCCS)的病因,NBCCS是一种常染色体显性疾病,可导致发育异常,并使受影响个体易患癌症。这些突变中的许多,包括ptch1大细胞内环(ICL)C末端的突变(p.C727VfsX745和p.S733IfsX736),会导致蛋白质过早截断。在患有NBCCS相关牙源性角化囊性瘤(KCOT)的患者中已鉴定出ptch1-C727VfsX745和ptch1-S733IfsX736突变。在本研究中,我们发现非经典刺猬(Hh)信号通路通过细胞周期蛋白B1调控的分子机制参与了NBCCS相关KCOT的发病机制。与野生型ptch1相比,ptch1-C727VfsX745和ptch1-S733IfsX736与细胞周期蛋白B1的结合明显减少。此外,表达这两种突变的细胞显示细胞周期进程加快,并且这两种突变构建体未能抑制细胞增殖。此外,这些突变体增强了Hh信号下游报告基因胶质瘤相关癌基因家族锌指1(GLI1)的活性。因此,我们的数据表明,通过ptch1和细胞周期蛋白B1介导的非经典Hh通路参与了NBCCS相关KCOT的发病机制。ptch1中ICL的C末端也可能是治疗该疾病的潜在治疗靶点。