Increased binding to sigma sites of N-(1'(2-piperidinyl)ethyl)-4-(I-125)-iodobenzamide (I-125-PAB) with onset of tumor cell proliferation.

Zamora PO; Moody TW; John CS

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Increased binding to sigma sites of N-(1'(2-piperidinyl)ethyl)-4-(I-125)-iodobenzamide (I-125-PAB) with onset of tumor cell proliferation.

机译：随着肿瘤细胞增殖的开始，与N-（1'（2-哌啶基）乙基）-4-（I-125）-碘苯甲酰胺（I-125-PAB）的sigma位点的结合增加。

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This study evaluated if the density of sigma sites was modulated following stimulation of mitosis and progression through the cell cycle. The sigma ligand N-[1'(2-piperidinyl)ethyl)-4-[I-125]-iodobenzamide (I-125-PAB) was a binding probe on the mammary tumor cell lines T47D and MCF-7, and the prostate tumor cell line DU-145. Cells at low density and in log phase growth bound more I-125-IPAB than those at high density at or the near plateau phase. Stimulation of mitosis with insulin or fresh 10% serum increased I-125-IPAB binding in all three cell lines. In cell-cycle synchronized cells, the highest amount of binding was found in cells treated with colcemid to block cells in the M-phase, while the lowest amount of binding was found in cells treated with low serum to block the cells in G1. Cells treated with aphidicolin to block cells at G1/S also bound less than cells block in the M-phase. Collectively, these results support a direct correlation between I-125-PAB binding and proliferative status, and suggest an up-regulation of sigma binding sites prior to mitosis.

机译：这项研究评估了在刺激有丝分裂和整个细胞周期进程后是否调节了sigma位点的密度。 σ配体N- [1'（2-哌啶基）乙基）-4- [I-125]-碘苯甲酰胺（I-125-PAB）是乳腺肿瘤细胞系T47D和MCF-7上的结合探针，前列腺肿瘤细胞系DU-145。与处于高密度阶段或接近平稳阶段的细胞相比，处于低密度并处于对数期生长的细胞结合更多的I-125-IPAB。用胰岛素或新鲜的10％血清刺激有丝分裂可增加所有三种细胞系中I-125-IPAB的结合。在细胞周期同步细胞中，在用秋水仙胶处理的细胞中发现最高的结合量，以阻断M期细胞，而在用低血清处理的细胞中发现的结合量最低，以阻断G1细胞。用蚜虫蛋白处理以在G1 / S处阻断细胞的细胞结合也少于在M期阻断的细胞。总体而言，这些结果支持I-125-PAB结合与增殖状态之间的直接相关性，并提示有丝分裂之前sigma结合位点的上调。

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《Life sciences》 |1998年第18期|共8页
作者
Zamora PO; Moody TW; John CS;
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正文语种 eng
中图分类生命的起源;生命科学总论;
关键词
Benzamides; Mitosis; Piperidines; Receptors; sigma; Up Regulation Physiology physiology; 苯甲酰胺类; 有丝分裂; 哌啶类; 受体; Σ;

机译：Benzamides;Mitosis;Piperidines;Receptors;sigma;Up Regulation Physiology physiology;苯甲酰胺类;有丝分裂;哌啶类;受体;Σ;

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1. Increased binding to sigma sites of N-(1'(2-piperidinyl)ethyl)-4-(I-125)-iodobenzamide (I-125-PAB) with onset of tumor cell proliferation. [J] . Zamora PO, Moody TW, John CS Life sciences . 1998,第18期

机译：随着肿瘤细胞增殖的开始，与N-（1'（2-哌啶基）乙基）-4-（I-125）-碘苯甲酰胺（I-125-PAB）的sigma位点的结合增加。
2. Sigma Receptor Scintigraphy with N-[2-(1a€2-Piperidinyl)Ethyl]-3-123I-Iodo-4-Methoxybenzamide of Patients with Suspected Primary Breast Cancer: First Clinical Results [J] . Vicky Caveliers, Hendrik Everaert, Christy S. John, The Journal of Nuclear Medicine . 2002,第12期

机译：可疑原发性乳腺癌患者的N- [2-（1a€2-哌啶基）乙基] -3-123I-碘-4-甲氧基苯甲酰胺西格玛受体闪烁扫描：首次临床结果
3. The beta3-adrenoceptor agonist 4-(((Hexylamino)carbonyl)amino)-N-(4-(2-(((2S)-2-hydroxy-3-(4-hydroxyphenoxy)prop yl)amino)ethyl)-phenyl)-benzenesulfonamide (L755507) and antagonist (S)-N-(4-(2-((3-(3-(acetamidomethyl)phenoxy)-2-hydroxypropyl)amino)-ethyl]phenyl]benzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K1 cells stably expressing the human beta3-adrenoceptor. [J] . Sato M, Hutchinson DS, Evans BA, Molecular pharmacology. . 2008,第5期

机译：β3-肾上腺素受体激动剂4-（（（（己基氨基）羰基）氨基）-N-（4-（2-（（（（2S）-2-羟基-3-（4-羟基苯氧基）丙基）氨基）乙基）-苯基）-苯磺酰胺（L755507）和拮抗剂（S）-N-（4-（2-（（3-（3-（3-（乙酰氨基甲基）苯氧基）-2-羟丙基）氨基）-乙基]苯基]苯磺酰胺（L748337）活化仓鼠卵巢K1细胞中不同的信号通路稳定表达人β3-肾上腺素受体。
4. ~(123)I-Vascular Endothelial Growth Factor165 (~(123)I-VEGF_(165)) Binding Sites in Tumor Cells: Implication for Tumor Scintigraphy [C] . S.R. Li, C. Bischof, S. Kapiotis, NATO Advanced Study Institute on Vascular Endothelium : Mechanisms of Cell Signaling . 1999

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5. The M2 splice isoform of pyruvate kinase is a phosphotyrosine binding protein critical for tumor cell metabolism and proliferation. [D] . Christofk, Heather Renee. 2007

机译：丙酮酸激酶的M2剪接同工型是对肿瘤细胞代谢和增殖至关重要的磷酸酪氨酸结合蛋白。
6. Autoradiographic localization of sigma receptor binding sites in guinea pig and rat central nervous system with (+)3H-3-(3-hydroxyphenyl)-N-(1- propyl)piperidine [O] . AL Gundlach, BL Largent, SH Snyder 1986

机译：（+）3H-3-（3-羟苯基）-N-（1-丙基）哌啶在豚鼠和大鼠中枢神经系统中sigma受体结合位点的放射自显影定位
7. LTBP-2 Has a Single High-Affinity Binding Site for FGF-2 and Blocks FGF-2-Induced Cell Proliferation. [O] . Clementine Menz, Mahroo K Parsi, Julian R J Adams, 2015

机译：LTBp-2具有FGF-2的单一高亲和力结合位点并阻断FGF-2诱导的细胞增殖。

Increased binding to sigma sites of N-(1'(2-piperidinyl)ethyl)-4-(I-125)-iodobenzamide (I-125-PAB) with onset of tumor cell proliferation.

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