Matrix metalloproteinases (MMPs) are central to cancer development and metastasis. They are highly active in the tumor environment and absent or inactive in normal tissues; therefore they represent viable targets for cancer drug discovery. In this study we evaluated in silico docking to develop MMP-subtype-selective tumor-activated prodrugs. Proof of principle for this therapeutic approach was demonstrated in vitro against an aggressive human glioma model, with involvement of MMPs confirmed using pharmacological inhibition.

中文翻译：

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基质金属蛋白酶选择性前药的合理计算机辅助设计

基质金属蛋白酶（MMP）对癌症的发展和转移至关重要。它们在肿瘤环境中高度活跃，而在正常组织中不活跃或不活跃。因此，它们代表了癌症药物发现的可行目标。在这项研究中，我们评估了计算机对接开发的MMP亚型选择性肿瘤激活前药。在体外针对侵略性人类神经胶质瘤模型证明了该治疗方法的原理性证明，并通过药理学抑制作用证实了MMP的参与。