已入深夜,您辛苦了!由于当前在线用户较少,发布求助请尽量完整的填写文献信息,科研通机器人24小时在线,伴您度过漫漫科研夜!祝你早点完成任务,早点休息,好梦!

Novel camptothecin derivative BNP1350 in experimental human ovarian cancer: Determination of efficacy and possible mechanisms of resistance

拓扑替康 喜树碱 拓扑异构酶 卵巢癌 米托蒽醌 序号38 Abcg2型 药理学 癌症研究 生物 化学 医学 伊立替康 癌症 生物化学 内科学 化疗 基因 ATP结合盒运输机 结直肠癌 运输机
作者
Annemarie H. Van Hattum,Hennie M.M. Schlüper,Frederick H. Hausheer,Herbert M. Pinedo,Epie Boven
出处
期刊:International Journal of Cancer [Wiley]
卷期号:100 (1): 22-29 被引量:41
标识
DOI:10.1002/ijc.10434
摘要

Abstract The novel camptothecin derivative BNP1350 (7‐[2‐trimethylsilyl)ethyl]‐20( S )‐camptothecin), also known as Karenitecin, has been developed for superior oral bioavailability and increased lactone stability. In our study, we describe the antiproliferative effects of BNP1350, SN‐38 and topotecan in 4 human ovarian cancer cell lines. BNP1350 was found to be slightly more potent than SN‐38 ( p <0.01) and was considerably more potent than topotecan ( p <0.01). We extended these studies to well‐established human ovarian cancer xenografts in which we compared the growth inhibition induced by BNP1350 with that of topotecan given in equitoxic schedules. The growth inhibition in all 3 xenografts induced by BNP1350 was ≥75%, which was significantly better than that resulting from topotecan ( p <0.05). We then selected BNP1350‐resistant variants of the A2780 human ovarian cancer cell line, 2780K4 (resistance factor: 41) and 2780K32 (resistance factor: 90), to analyze possible resistance mechanisms. These variants exhibited cross‐resistance against all camptothecins tested. In comparison with 2780K4 cells, 2780K32 cells were relatively more resistant against SN‐38, topotecan, DX‐8951f and BNP1350. In addition, 2780K32 cells were highly cross‐resistant against mitoxantrone. In both 2780K4 and 2780K32, the amount of topoisomerase I was not changed but the catalytic activity was reduced. Furthermore, 2780K32 cells clearly overexpressed the breast cancer resistance protein (BCRP), as demonstrated for both the gene and the protein. In contrast to topotecan, BNP1350 proved not to be a good substrate for BCRP. Overall, we conclude that BNP1350 offers advantages over topotecan expressed by high efficacy in experimental human ovarian cancer and poor affinity for BCRP. © 2002 Wiley‐Liss, Inc.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
大幅提高文件上传限制,最高150M (2024-4-1)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
下文献完成签到,获得积分10
1秒前
凶狠的寄风完成签到 ,获得积分10
2秒前
zhvjdb发布了新的文献求助10
3秒前
xingzai101发布了新的文献求助10
6秒前
CC完成签到 ,获得积分10
7秒前
sun完成签到,获得积分20
8秒前
9秒前
信件箱完成签到 ,获得积分10
12秒前
12秒前
雨雨雨雨雨文完成签到 ,获得积分10
12秒前
sun发布了新的文献求助30
14秒前
领导范儿应助郜雨寒采纳,获得10
15秒前
xiuxiuzhang完成签到 ,获得积分10
16秒前
阿宅完成签到 ,获得积分10
17秒前
czy完成签到 ,获得积分10
19秒前
小田心完成签到 ,获得积分10
19秒前
Makta完成签到,获得积分10
21秒前
贝贝完成签到 ,获得积分10
24秒前
Dean完成签到 ,获得积分10
24秒前
24秒前
动听靖完成签到 ,获得积分10
25秒前
止戈完成签到 ,获得积分10
25秒前
小葵完成签到 ,获得积分10
25秒前
m(_._)m完成签到 ,获得积分0
26秒前
junkook完成签到 ,获得积分10
27秒前
胖崽胖崽发布了新的文献求助10
29秒前
30秒前
满唐完成签到 ,获得积分10
30秒前
夏爽2023完成签到,获得积分10
32秒前
微笑的梦山完成签到,获得积分10
32秒前
zhvjdb完成签到,获得积分20
34秒前
学术骗子小刚完成签到,获得积分10
34秒前
yunsww完成签到,获得积分10
35秒前
yema完成签到 ,获得积分10
36秒前
37秒前
wenhuanwenxian完成签到 ,获得积分10
39秒前
meng发布了新的文献求助10
42秒前
沉静海安完成签到 ,获得积分10
42秒前
852应助六个核桃采纳,获得10
49秒前
胖崽胖崽完成签到,获得积分10
50秒前
高分求助中
Kinetics of the Esterification Between 2-[(4-hydroxybutoxy)carbonyl] Benzoic Acid with 1,4-Butanediol: Tetrabutyl Orthotitanate as Catalyst 1000
The Young builders of New china : the visit of the delegation of the WFDY to the Chinese People's Republic 1000
Rechtsphilosophie 1000
Handbook of Qualitative Cross-Cultural Research Methods 600
Chen Hansheng: China’s Last Romantic Revolutionary 500
Mantiden: Faszinierende Lauerjäger Faszinierende Lauerjäger 500
PraxisRatgeber: Mantiden: Faszinierende Lauerjäger 500
热门求助领域 (近24小时)
化学 医学 生物 材料科学 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 基因 遗传学 催化作用 物理化学 免疫学 量子力学 细胞生物学
热门帖子
关注 科研通微信公众号,转发送积分 3139398
求助须知:如何正确求助?哪些是违规求助? 2790314
关于积分的说明 7794847
捐赠科研通 2446748
什么是DOI,文献DOI怎么找? 1301366
科研通“疑难数据库(出版商)”最低求助积分说明 626153
版权声明 601141