Mannella Viviana, Boehm Kira, Celik Suheyla, Ali Tasnim, Mirza Amnah N, El Hasnaouy Mariam, Kaffa Andreas, Lyu Yanshuang, Kafaei Golahmadi Donya, Leigh Irene M, Bergamaschi Daniele, Harwood Catherine A, Maffucci Tania
Centre for Cell Biology and Cutaneous Research, Blizard Institute, Barts and The London School of Medicine and Dentistry, Queen Mary University of London, London E1 2AT, UK.
Department of Clinical Medicine, School of Queen Mary, Nanchang University, Nanchang 330006, China.
Int J Mol Sci. 2021 Mar 30;22(7):3567. doi: 10.3390/ijms22073567.
Cutaneous squamous cell carcinomas (cSCCs) account for about 20% of keratinocyte carcinomas, the most common cancer in the UK. Therapeutic options for cSCC patients who develop metastasis are limited and a better understanding of the biochemical pathways involved in cSCC development/progression is crucial to identify novel therapeutic targets. Evidence indicates that the phosphoinositide 3-kinases (PI3Ks)/Akt pathway plays an important role, in particular in advanced cSCC. Questions remain of whether all four PI3K isoforms able to activate Akt are involved and whether selective inhibition of specific isoform(s) might represent a more targeted strategy. Here we determined the sensitivity of four patient-derived cSCC cell lines to isoform-specific PI3K inhibitors to start investigating their potential therapeutic value in cSCC. Parallel experiments were performed in immortalized keratinocyte cell lines. We observed that pan PI3Ks inhibition reduced the growth/viability of all tested cell lines, confirming the crucial role of this pathway. Selective inhibition of the PI3K isoform p110α reduced growth/viability of keratinocytes and of two cSCC cell lines while affecting the other two only slightly. Importantly, p110α inhibition reduced Akt phosphorylation in all cSCC cell lines. These data indicate that growth and viability of the investigated cSCC cells display differential sensitivity to isoform-specific PI3K inhibitors.
皮肤鳞状细胞癌(cSCC)约占角质形成细胞癌的20%,是英国最常见的癌症。发生转移的cSCC患者的治疗选择有限,更好地了解cSCC发生/进展过程中涉及的生化途径对于确定新的治疗靶点至关重要。有证据表明,磷酸肌醇3-激酶(PI3K)/Akt信号通路发挥着重要作用,尤其是在晚期cSCC中。关于能够激活Akt的所有四种PI3K亚型是否都参与其中,以及对特定亚型的选择性抑制是否可能代表一种更具针对性的策略,仍存在疑问。在这里,我们测定了四种患者来源的cSCC细胞系对亚型特异性PI3K抑制剂的敏感性,以开始研究它们在cSCC中的潜在治疗价值。在永生化角质形成细胞系中进行了平行实验。我们观察到,泛PI3K抑制降低了所有测试细胞系的生长/活力,证实了该信号通路至关重要的作用。对PI3K亚型p110α的选择性抑制降低了角质形成细胞和两种cSCC细胞系的生长/活力,而对另外两种细胞系的影响较小。重要的是,p110α抑制降低了所有cSCC细胞系中Akt的磷酸化水平。这些数据表明,所研究的cSCC细胞的生长和活力对亚型特异性PI3K抑制剂表现出不同的敏感性。