新型组蛋白去乙酰化酶抑制剂FK228对体内肿瘤生长及p21和c-myc基因表达的影响
Effects of FK228, a novel histone deacetylase inhibitor, on tumor growth and expression of p21 and c-myc genes in vivo.
作者信息
Sasakawa Yuka, Naoe Yoshinori, Inoue Takeshi, Sasakawa Tatsuya, Matsuo Masahiko, Manda Toshitaka, Mutoh Seitaro
机构信息
Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka, 532-8514, Japan.
出版信息
Cancer Lett. 2003 Jun 10;195(2):161-8. doi: 10.1016/s0304-3835(03)00184-8.
In this study, we examined the effects of FK228 (FR901228, depsipeptide) on tumor growth and expression of p21 and c-myc genes in vivo. FK228 induced the expression of p21 mRNA and decreased c-myc mRNA in tumor xenograft sensitive to FK228. However, FK228 did not sufficiently modulate the expression of p21 mRNA and increased the expression of c-myc in tumor xenograft less sensitive to FK228. The modulation of p21 and/or c-myc genes may be critical for the marked antitumor activity of FK228 in vivo.
在本研究中，我们检测了FK228（FR901228，缩酚酸肽）对体内肿瘤生长以及p21和c-myc基因表达的影响。FK228可诱导对FK228敏感的肿瘤异种移植瘤中p21 mRNA的表达并降低c-myc mRNA的表达。然而，FK228未能充分调节对FK228不太敏感的肿瘤异种移植瘤中p21 mRNA的表达，反而增加了c-myc的表达。p21和/或c-myc基因的调节可能对FK228在体内显著的抗肿瘤活性至关重要。
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