CPT-11 converting carboxylesterase and topoisomerase activities in tumour and normal colon and liver tissues.
CPT-11 converting carboxylesterase and topoisomerase activities in tumour and normal colon and liver tissues.
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DOI：
10.1038/sj.bjc.6690364
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发表时间：
1999-05
影响因子：
8.8
通讯作者：
Canal, P
中科院分区：
文献类型：
--
作者：
Guichard, S;Terret, C;Hennebelle, I;Lochon, I;Chevreau, P;Frétigny, E;Selves, J;Chatelut, E;Bugat, R;Canal, P
CPT-11是一种被羧酸酯酶激活为拓扑异构酶I抑制剂的活性代谢物SN-38的前体药物，CPT-11在结直肠癌的治疗中具有临床意义。我们检测了53例结直肠癌、8例肝转移瘤和癌旁正常组织中CPT-11转换羧酸酯酶(CPT-CE)和拓扑异构酶I(TOPO I)的活性。CPT-CE和Topo I活性在结直肠癌患者的癌组织和正常组织中变化很大。CPT-CE在原发肿瘤中只比正常肝脏低两到三倍，这表明肿瘤细胞可能发生了局部转化为SN-38。CPT-CE在肝脏和正常结肠组织中的表达相似。肿瘤组织中Topo I的含量范围为580~84900U mg蛋白−1，其中11例高于40000 U mg蛋白−1。同样，在53例患者中，有12例观察到肿瘤和正常组织之间有很高的比率(>；5)。Topo I活性与临床分期呈负相关。我们机构正在进行临床研究，以探索结直肠癌患者肿瘤细胞中CPT-CE和Topo I活性与以CPT-11为基础的化疗反应之间的可能关系。©1999癌症研究活动
CPT-11 is a prodrug activated by carboxylesterases to the active metabolite SN-38 which is a potent inhibitor of topoisomerase I. CPT-11 is of clinical interest in the treatment of colorectal cancer. We evaluated the activities of CPT-11 converting carboxylesterase (CPT-CE) and topoisomerase I (topo I) in 53 colorectal tumours, in eight liver metastases and in normal tissue adjacent to the tumours. Both CPT-CE and topo I activities were widely variable in the malignant and the normal tissue of patients with colorectal carcinomas. CPT-CE was only two to threefold lower in primary tumours compared to normal liver, suggesting that a local conversion to SN-38 might occur in tumour cells. CPT-CE was similar in liver and in normal colon tissues. Levels of topo I in tumour ranged from 580 to 84 900 U mg protein−1 and was above 40 000 U mg protein−1 in 11 of 53 patients. Similarly, a very high ratio (> 5) between tumour and normal tissues were observed in 12 of 53 patients. An inverse correlation was observed between the topo I activity and the clinical stage of disease. Clinical studies are in progress in our institution to explore a possible relationship between CPT-CE and topo I activities in tumour cells and the response to CPT-11-based chemotherapy in patients with colorectal cancer. © 1999 Cancer Research Campaign
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影响因子：
56.9
作者：
GIOVANELLA, BC;STEHLIN, JS;POTMESIL, M
通讯作者：
POTMESIL, M
影响因子：
15.9
作者：
Kojima, A;Hackett, NR;Crystal, RG
通讯作者：
Crystal, RG
影响因子：
2.9
作者：
BRADFORD, MM
通讯作者：
BRADFORD, MM
影响因子：
6.4
作者：
MCLEOD, HL;DOUGLAS, F;KEITH, WN
通讯作者：
KEITH, WN
DOI：
10.1111/j.1349-7006.1995.tb02997.x
发表时间：
1995-01-01
期刊：
JAPANESE JOURNAL OF CANCER RESEARCH
影响因子：
--
作者：
OGASAWARA, H;NISHIO, K;SAIJO, N
通讯作者：
SAIJO, N