Cationic Pillar[6]arene Induces Cell Apoptosis by Inhibiting Protein Tyrosine Phosphorylation Via Host-Guest Recognition
Cationic Pillar[6]arene Induces Cell Apoptosis by Inhibiting Protein Tyrosine Phosphorylation Via Host-Guest Recognition
复制标题
阳离子柱[6]芳烃通过主客体识别抑制蛋白质酪氨酸磷酸化，诱导细胞凋亡
DOI：
10.3390/ijms21144979
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发表时间：
2020-07-01
影响因子：
5.6
通讯作者：
Zhang, Ya-Ping
中科院分区：
文献类型：
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作者：
Li, Can-Peng;Lu, Yu-Xun;Zhang, Ya-Ping
我们首次报道了阳离子柱[6]芳烃(CPA6)能与酪氨酸(Tyr)磷酸化的人工底物多肽聚合物(分子量约20-50 kDa)紧密结合，并通过主客体识别有效地抑制Tyr蛋白的磷酸化。为了探讨cPA6对细胞的影响，我们合成了一种负载cPA6的黑磷纳米片纳米复合材料(BPNS@cPA6)。BPNS@cPA6可通过降低Tyr的磷酸化水平进入HepG2细胞，诱导细胞凋亡，抑制细胞增殖。此外，BPNS@cPA6对肿瘤细胞的增殖抑制作用明显强于正常细胞。我们的结果揭示了cPA6的主客体识别对酶促Tyr磷酸化的超分子调控。
We reported for the first time that cationic pillar[6]arene (cPA6) could tightly bind to peptide polymer (MW similar to 20-50 kDa), an artificial substrate for tyrosine (Tyr) phosphorylation, and efficiently inhibit Tyr protein phosphorylation through host-guest recognition. We synthesized a nanocomposite of black phosphorus nanosheets loaded with cPA6 (BPNS@cPA6) to explore the effect of cPA6 on cells. BPNS@cPA6 was able to enter HepG2 cells, induced apoptosis, and inhibited cell proliferation by reducing the level of Tyr phosphorylation. Furthermore, BPNS@cPA6 showed a stronger ability of inhibiting cell proliferation in tumor cells than in normal cells. Our results revealed the supramolecular modulation of enzymatic Tyr phosphorylation by the host-guest recognition of cPA6.