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FCHO1 肽,一种 PKB 激酶基序,抑制肿瘤进展。

FCHO1 peptide, a PKB kinase motif, inhibits tumor progression.

机构信息

Laboratory of Genetics, University of Wisconsin-Madison, Madison, WI, 53706, USA; Department of Pharmacology, Metabolic Syndrome and Cell Signaling Laboratory, Institute for Cancer Research, College of Medicine, Chungnam National University, Daejeon, 35015, South Korea.

Department of Pharmacology, Metabolic Syndrome and Cell Signaling Laboratory, Institute for Cancer Research, College of Medicine, Chungnam National University, Daejeon, 35015, South Korea; Department of Medical Science, College of Medicine, Chungnam National University, Daejeon, 35015, South Korea.

出版信息

Biochem Biophys Res Commun. 2020 Jul 30;528(3):478-484. doi: 10.1016/j.bbrc.2020.05.173. Epub 2020 Jun 4.

Abstract

BACKGROUND

Cell division is regulated by protein kinase B (PKB)-mediated FCH domain only 1 (FCHO1) phosphorylation.

METHODS

FCHO1, a synthetic water-soluble peptide, was generated from the PKB substrate motif PPRRLRSRKVSC found in the human FCHO1 protein.

RESULTS

In this study, we found that in vitro FCHO1 inhibits cell proliferation via PKB/ERK/SMAD4 pathways in K-mutated A549 lung cancer cells. In addition, FCHO1, at effective doses of 15 and 30 mg/kg, significantly suppressed tumor growth and decreased the size and weight of tumors in A549-xenograft mice.

CONCLUSION

These results suggest that the FCHO1 peptide could be a potential therapy for lung cancer.

摘要

背景

细胞分裂受蛋白激酶 B(PKB)介导的 FCH 结构域仅 1(FCHO1)磷酸化调节。

方法

FCHO1 是一种合成的水溶性肽,来源于人 FCHO1 蛋白中 PKB 底物基序 PPRRLRSRKVSC。

结果

在这项研究中,我们发现 FCHO1 在体外通过 PKB/ERK/SMAD4 通路抑制 K 突变 A549 肺癌细胞的增殖。此外,FCHO1 在有效剂量为 15 和 30mg/kg 时,显著抑制了 A549 异种移植小鼠的肿瘤生长,并降低了肿瘤的大小和重量。

结论

这些结果表明,FCHO1 肽可能是一种治疗肺癌的潜在疗法。

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