Specific VDAC inhibitors: phosphorothioate oligonucleotides.
Specific VDAC inhibitors: phosphorothioate oligonucleotides.
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特异性 VDAC 抑制剂：硫代磷酸酯寡核苷酸。
DOI：
10.1007/s10863-008-9139-9
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发表时间：
2008
影响因子：
3
通讯作者：
Colombini,Marco
中科院分区：
文献类型：
--
作者：
Stein,CA;Colombini,Marco
VDAC通道是线粒体外膜上的一种古老的、高度保守的电压门控通道。它们是代谢物在细胞质和线粒体之间移动的途径。它们参与了细胞凋亡的过程，可能还参与了其他功能。过去，缺乏特定的抑制剂阻碍了研究，但现在硫代寡核苷酸可以发挥这一功能。这些分子在细胞胞浆中是稳定的，但与具有生理磷酸二酯键的寡核苷酸不同，它们具有结合和阻断VDAC通道的能力。他们是强有力的，具体的，并在商业上可用。在1μM浓度下，它们阻断线粒体上的VDAC通道，但不影响呼吸复合体、腺核苷酸转运体或三磷酸腺苷合成酶。
VDAC channels are ancient, highly-conserved voltage-gated channels in the mitochondrial outer membrane. They are the pathways by which metabolites travel between the cytosol and mitochondria. They are involved in the apoptotic process and probably other functions as well. The lack of specific inhibitors has hampered research in the past but now phosphothioate oligonucleotides can serve this function. These molecules were generated to be stable in the cytosol of cells but, unlike the oligonucleotides with the physiological phosphodiester linkage, these have the ability to bind to and block VDAC channels. They are potent, specific, and available commercially. At 1 μM concentration they block VDAC channels in mitochondria but do not affect the respiration complexes, the adenine nucleotide translocator or the ATP synthase.