Immune Imaging Program, Centenary Institute, Faculty of Medicine and Health, The University of Sydney, Camperdown, NSW 2050, Australia.
Sydney Medical School, The University of Sydney, Camperdown, NSW 2050, Australia.
Proc Natl Acad Sci U S A. 2023 Nov 21;120(47):e2303978120. doi: 10.1073/pnas.2303978120. Epub 2023 Nov 14.
Robust high-throughput assays are crucial for the effective functioning of a drug discovery pipeline. Herein, we report the development of Invasion-Block, an automated high-content screening platform for measuring invadopodia-mediated matrix degradation as a readout for the invasive capacity of cancer cells. Combined with Smoothen-Mask and Reveal, a custom-designed, automated image analysis pipeline, this platform allowed us to evaluate melanoma cell invasion capacity posttreatment with two libraries of compounds comprising 3840 U.S. Food and Drug Administration (FDA)-approved drugs with well-characterized safety and bioavailability profiles in humans as well as a kinase inhibitor library comprising 210 biologically active compounds. We found that Abl/Src, PKC, PI3K, and Ataxia-telangiectasia mutated (ATM) kinase inhibitors significantly reduced melanoma cell invadopodia formation and cell invasion. Abrogation of ATM expression in melanoma cells via CRISPR-mediated gene knockout reduced 3D invasion in vitro as well as spontaneous lymph node metastasis in vivo. Together, this study established a rapid screening assay coupled with a customized image-analysis pipeline for the identification of antimetastatic drugs. Our study implicates that ATM may serve as a potent therapeutic target for the treatment of melanoma cell spread in patients.
高通量检测方法的稳健性对于药物发现管道的有效运作至关重要。在此,我们报告了 Invasion-Block 的开发,这是一种自动化高内涵筛选平台,用于测量侵袭伪足介导的基质降解,作为癌细胞侵袭能力的读数。与 Smoothen-Mask 和 Reveal 相结合,这是一个定制的自动化图像分析管道,该平台使我们能够在两种化合物文库处理后评估黑素瘤细胞的侵袭能力,这两种文库包括 3840 种美国食品和药物管理局 (FDA) 批准的药物,这些药物在人类中具有良好的安全性和生物利用度特征,以及一个包含 210 种具有生物活性的化合物的激酶抑制剂文库。我们发现,Abl/Src、PKC、PI3K 和共济失调毛细血管扩张突变 (ATM) 激酶抑制剂显著减少了黑素瘤细胞侵袭伪足的形成和细胞侵袭。通过 CRISPR 介导的基因敲除使黑素瘤细胞中的 ATM 表达缺失,减少了体外 3D 侵袭以及体内自发的淋巴结转移。总之,这项研究建立了一种快速筛选测定法,结合了定制的图像分析管道,用于鉴定抗转移药物。我们的研究表明,ATM 可能作为治疗患者黑素瘤细胞扩散的有效治疗靶点。