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吡咯并苯并二氮杂䓬衍生物在培养细胞中的抗增殖作用：与外周型苯二氮䓬结合位点结合无相关性。

Antiproliferative action of pyrrolobenzoxazepine derivatives in cultured cells: absence of correlation with binding to the peripheral-type benzodiazepine binding site.

作者信息

Zisterer D M, Hance N, Campiani G, Garofalo A, Nacci V, Williams D C

机构信息

Department of Biochemistry, Trinity College, Dublin, Ireland.

出版信息

Biochem Pharmacol. 1998 Feb 15;55(4):397-403. doi: 10.1016/s0006-2952(97)00500-5.

DOI:10.1016/s0006-2952(97)00500-5
PMID:9514073
Abstract

Three novel peripheral-type benzodiazepine binding site (PBBS) ligands, NF 182, 213 and 262, along with the classically used PBBS ligands, PK 11195 and Ro5-4864, were found to inhibit, at micromolar concentrations and in dose-dependent manner, the proliferation of rat C6 glioma and human 1321N1 astrocytoma, without being cytotoxic. This antiproliferative effect is mediated by arrest in the G1 phase of the cell cycle and does not appear to be mediated by a specific interaction of these ligands with the peripheral-type benzodiazepine binding site.

摘要

研究发现，三种新型外周型苯二氮䓬结合位点（PBBS）配体NF 182、213和262，与经典使用的PBBS配体PK 11195和Ro5-4864一样，在微摩尔浓度下以剂量依赖性方式抑制大鼠C6胶质瘤和人1321N1星形细胞瘤的增殖，且无细胞毒性。这种抗增殖作用是由细胞周期G1期停滞介导的，似乎不是由这些配体与外周型苯二氮䓬结合位点的特异性相互作用介导的。

相似文献

1
Antiproliferative action of pyrrolobenzoxazepine derivatives in cultured cells: absence of correlation with binding to the peripheral-type benzodiazepine binding site.吡咯并苯并二氮杂䓬衍生物在培养细胞中的抗增殖作用：与外周型苯二氮䓬结合位点结合无相关性。
Biochem Pharmacol. 1998 Feb 15;55(4):397-403. doi: 10.1016/s0006-2952(97)00500-5.
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Antiproliferative action of benzodiazepines in cultured brain cells is not mediated through the peripheral-type benzodiazepine acceptor.苯二氮䓬类药物在培养的脑细胞中的抗增殖作用并非通过外周型苯二氮䓬受体介导。
J Neurochem. 1989 Sep;53(3):849-55. doi: 10.1111/j.1471-4159.1989.tb11782.x.
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A new aspect of the antiproliferative action of peripheral-type benzodiazepine receptor ligands.外周型苯二氮䓬受体配体抗增殖作用的一个新方面。
Eur J Pharmacol. 1995 Jan 16;272(2-3):289-92. doi: 10.1016/0014-2999(94)00652-n.
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Stimulation of cell growth and DNA synthesis by peripheral benzodiazepine.外周苯二氮䓬对细胞生长和DNA合成的刺激作用。
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Cofractionation of the 17-kD PK 14105 binding site protein with solubilized peripheral-type benzodiazepine binding sites.
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Opposite effects of an agonist, RO5-4864, and an antagonist, PK 11195, of the peripheral type benzodiazepine binding sites on audiogenic seizures in DBA/2J mice.外周型苯二氮䓬结合位点的激动剂RO5-4864和拮抗剂PK 11195对DBA/2J小鼠听源性惊厥的相反作用。
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Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging.异喹啉与外周型苯二氮䓬在胶质瘤中的结合：对诊断成像的意义。
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Opposite effects of two ligands for peripheral type benzodiazepine binding sites, PK 11195 and RO5-4864, in a conflict situation in the rat.
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Benzodiazepines that bind at peripheral sites inhibit cell proliferation.在外周部位结合的苯二氮卓类药物会抑制细胞增殖。
Proc Natl Acad Sci U S A. 1984 Feb;81(3):753-6. doi: 10.1073/pnas.81.3.753.
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Peripheral benzodiazepine receptor ligands: mitochondrial transmembrane potential depolarization and apoptosis induction in rat C6 glioma cells.外周苯二氮䓬受体配体：大鼠C6胶质瘤细胞中线粒体跨膜电位去极化及凋亡诱导
Biochem Pharmacol. 2004 Jul 1;68(1):125-34. doi: 10.1016/j.bcp.2004.03.008.

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