血管扩张剂和利钾尿肽抑制人前列腺癌细胞中ERK 1/2的激活。

Vessel dilator and kaliuretic peptide inhibit ERK 1/2 activation in human prostate cancer cells.

作者信息

Sun Ying, Eichelbaum Ehrentraud J, Wang Hai, Vesely David L

机构信息

Department of Internal Medicine, University of South Florida Cardiac Hormone Center and James A. Haley Veterans Medical Center Tampa, Florida 33612, USA.

出版信息

Anticancer Res. 2006 Sep-Oct;26(5A):3217-22.

PMID:17094432

Abstract

BACKGROUND

Vessel dilator and kaliuretic peptide have anticancer effects in human prostate adenocarcinomas.

MATERIALS AND METHODS

Vessel dilator, kaliuretic peptide and cyclic GMP's effects on ERK 1/2 kinase were examined in human prostate adenocarcinoma cells.

RESULTS

Vessel dilator and kaliuretic peptide decreased the activation of ERK 1/2 over a concentration range of 0.01 microM to 1 microM. Vessel dilator and kaliuretic peptide (each 1 microM) inhibited the phosphorylation of ERK 1/2 kinase 96% (p < 0.0001) and 70% (p < 0.001), respectively. Both had significant effects within five minutes at their 0.01 microM concentrations. The inhibition of ERK 1/2 lasted for at least two hours secondary to both. Their ability to inhibit ERK 1/2 was decreased by cyclic GMP antibody and cyclic GMP itself decreased ERK 1/2 phosphorylation.

CONCLUSION

Vessel dilator and kaliuretic peptide both inhibit ERK 1/2 kinase mediated via cyclic GMP as part of their anticancer mechanism(s) of action.

摘要

背景

血管舒张肽和利钾尿肽对人前列腺腺癌具有抗癌作用。

材料与方法

在人前列腺腺癌细胞中检测血管舒张肽、利钾尿肽和环磷酸鸟苷对ERK 1/2激酶的影响。

结果

在0.01微摩尔至1微摩尔的浓度范围内，血管舒张肽和利钾尿肽降低了ERK 1/2的激活。血管舒张肽和利钾尿肽（各1微摩尔）分别抑制ERK 1/2激酶磷酸化96%（p < 0.0001）和70%（p < 0.001）。两者在0.01微摩尔浓度下五分钟内均有显著作用。两者对ERK 1/2的抑制作用至少持续两小时。环磷酸鸟苷抗体降低了它们抑制ERK 1/2的能力，且环磷酸鸟苷本身降低了ERK 1/2的磷酸化。