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产品 > TCI热门产品信息 > TCI热门产品信息 2020 >
DNA连接酶抑制剂：SCR7吡嗪
最初，SCR7被认为是可以通过抑制DNA连接酶IV来阻断非同源末端连接（NHEJ）介导的DNA修复，从而提高CRISPR-Cas9的基因组编辑效率1-4)。但后来研究人员发现，由最初的合成方法生成的主要产物是SCR7吡嗪，而非SCR7，而SCR7本身不能抑制DNA连接酶IV5,6)。此后，据报道SCR7因其不稳定性而自动环化，并自氧化得到SCR7吡嗪。尽管SCR7吡嗪对DNA连接酶IV的选择性并不是很高，但它能在体外抑制NHEJ 7,8)。
文献
- 1) CRISPR-Cas systems for editing, regulating and targeting genomes
- 2) Increasing the efficiency of precise genome editing with CRISPR-Cas9 by inhibition of nonhomologous end joining
- 3) Increasing the efficiency of homology-directed repair for CRISPR-Cas9-induced precise gene editing in mammalian cells
- 4) An Inhibitor of Nonhomologous End-Joining Abrogates Double-Strand Break Repair and Impedes Cancer Progression
- 5) SCR7 is neither a selective nor a potent inhibitor of human DNA ligase IV
- 6) Synthesis and structure determination of SCR7, a DNA ligase inhibitor
- 7) Autocyclized and oxidized forms of SCR7 induce cancer cell death by inhibiting nonhomologous DNA end joining in a Ligase IV dependent manner
- 8) Water-soluble version of SCR7-pyrazine inhibits DNA repair and abrogates tumor cell proliferation
