Effect of the protein kinase inhibitors, 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine H-7 and N-(2-[methylamino]ethyl)-5-isoquinoline-sulfonamide H-8 on Lewis lung carcinoma tumor progression.

Effect of the protein kinase inhibitors, 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine H-7 and N-(2-[methylamino]ethyl)-5-isoquinoline-sulfonamide H-8 on Lewis lung carcinoma tumor progression.
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蛋白激酶抑制剂 1-(5-异喹啉磺酰基)-2-甲基哌嗪 H-7 和 N-(2-[甲基氨基]乙基)-5-异喹啉磺酰胺 H-8 对 Lewis 肺癌肿瘤进展的影响。

DOI:
10.1016/s0014-2999(98)00434-8
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发表时间:
1998
影响因子:
5
通讯作者:
S. Aliño
S. Aliño
中科院分区:
医学2区
文献类型:
--
作者:
C. Blaya;J. Crespo;A. Crespo;S. Aliño

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研究了依赖cAMP的蛋白激酶和蛋白激酶C抑制剂1-(5-isoquinolinylsulfonyl)-2-methylpiperazine H-7、依赖于cAMP和cGMP的蛋白激酶抑制剂n-(2-[methylamino]ethyl)-5-isoquinoline-sulfonamide H-8和环氧合酶抑制剂吲哚美辛对3LL(Lewis肺癌)细胞自发转移能力和抗肿瘤宿主反应的影响。对肿瘤进展的研究表明,H-7和H-8(2 mg kg−1day−1,i.p,连续8天)显著减少了对照组的肺转移数目(分别为0.8±0.2和1.0±0.7,P<0.0 5)。反过来,当动物和肿瘤细胞都用H-8处理时,观察到最高的肿瘤特异性细胞毒性反应(与未治疗的靶细胞相比增加50%)。这表明,蛋白激酶抑制剂可能通过阻断由增加细胞内cAMP的药物触发的免疫抑制机制来抑制肿瘤向肺转移形成的进展。
The effects of 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine H-7 (a cAMP-dependent protein kinase and protein kinase C inhibitor), n-(2-[methylamino]ethyl)-5-isoquinoline-sulfonamide H-8 (a cAMP- and cGMP-dependent protein kinase inhibitor) and indomethacin (IND, a cyclooxygenase inhibitor) on both the spontaneous metastatic ability of 3LL (Lewis lung carcinoma) tumor cells and anti-tumor host response were studied. The study of tumor progression showed that H-7 and H-8 (2 mg kg−1day−1, i.p., for 8 days) significantly reduced the mean number of metastases (0.8±0.2 and 1.0±0.7, respectively, P<0.05) with respect to the number of lung metastases (4.2±2.1) observed in the control group. In turn, the highest tumor-specific cytotoxicity response (50% increase vs. non-treated target cells) was observed when both animal and tumor cells were treated with H-8. This suggests that the protein kinase inhibitors could inhibit tumor progression toward lung metastases formation by blocking the immunosuppressor mechanism triggered by agents that increase intracellular cAMP.
前列腺素E2受体在乳腺肿瘤转移中的作用。
DOI: --
发表时间: 1991
期刊: Cancer research
影响因子: 11.2
作者:
Fulton,AM;Zhang,SZ;Chong,YC
通讯作者: Chong,YC
DOI: --
发表时间: 1990-10
期刊: Cancer research
影响因子: 11.2
作者:
I. Fidler
通讯作者: I. Fidler
天然效应细胞和前列腺素在控制转移中的相互作用。
DOI: --
发表时间: 1987
期刊: Journal of the National Cancer Institute
影响因子: --
作者:
Fulton,AM
通讯作者: Fulton,AM