Bangor University, Bangor, UK.
Xi'an Jiaotong-Liverpool University, Suzhou, China.
Microbiologyopen. 2020 Oct;9(10):e1110. doi: 10.1002/mbo3.1110. Epub 2020 Sep 26.
Directed enzyme prodrug therapy (DEPT) is a cancer chemotherapy strategy in which bacterial enzymes are delivered to a cancer site before prodrug administration, resulting in prodrug activation at the cancer site and more localized treatment. A major limitation to DEPT is the poor effectiveness of the most studied enzyme for the CB1954 prodrug, NfnB from Escherichia coli, at concentrations suitable for human use. Much research into finding alternative enzymes to NfnB has resulted in the identification of the Xenobiotic reductases, XenA and XenB, which have been shown in the literature to reduce environmentally polluting nitro-compounds. In this study, they were assessed for their potential use in cancer prodrug therapy strategies. Both proteins were cloned into the pET28a+ expression vector to give the genetically modified proteins XenA-his and XenB-his, of which only XenB-his was active when tested with CB1954. XenB-his was further modified to include a cysteine-tag to facilitate direct immobilization on to a gold surface for future magnetic nanoparticle DEPT (MNDEPT) treatments and was named XenB-cys. When tested using high-performance liquid chromatography (HPLC), XenB-his and XenB-cys both demonstrated a preference for reducing CB1954 at the 4-nitro position. Furthermore, XenB-his and XenB-cys successfully induced cell death in SK-OV-3 cells when combined with CB1954. This led to XenB-cys being identified as a promising candidate for use in future MNDEPT treatments.
导向酶前药治疗(DEPT)是一种癌症化疗策略,其中在给予前药之前将细菌酶递送到癌症部位,导致在癌症部位激活前药并进行更局部的治疗。DEPT 的一个主要限制是最常用于 CB1954 前药的酶,即来自大肠杆菌的 NfnB,在适合人类使用的浓度下效果不佳。为了寻找替代 NfnB 的酶,大量研究已经鉴定出了 Xenobiotic reductases,XenA 和 XenB,文献表明它们可以还原环境污染的硝基化合物。在这项研究中,评估了它们在癌症前药治疗策略中的潜在用途。这两种蛋白质都被克隆到 pET28a+表达载体中,得到了基因修饰的蛋白质 XenA-his 和 XenB-his,只有 XenB-his 在与 CB1954 一起测试时才具有活性。XenB-his 进一步修饰为包含半胱氨酸标签,以方便直接固定在金表面上,用于未来的磁性纳米颗粒 DEPT(MNDEPT)治疗,并被命名为 XenB-cys。当使用高效液相色谱(HPLC)进行测试时,XenB-his 和 XenB-cys 都表现出对 4-硝基位置的 CB1954 还原的偏好。此外,当与 CB1954 结合使用时,XenB-his 和 XenB-cys 成功诱导 SK-OV-3 细胞死亡。这导致 XenB-cys 被确定为未来 MNDEPT 治疗的有前途的候选药物。