表皮生长因子受体配体11C-PD153035的进一步特性研究。

Further characterization of the epidermal growth factor receptor ligand 11C-PD153035.

作者信息

Wang Hui, Yu Jin-ming, Yang Guo-ren, Song Xian-rang, Sun Xiao-rong, Zhao Shu-qiang, Wang Xing-wu, Zhao Wei

机构信息

Medical School of Shandong University, Jinan 250012, China.

出版信息

Chin Med J (Engl). 2007 Jun 5;120(11):960-4.

PMID:17624262

Abstract

BACKGROUND

(11)C-4-N-(3-bromoanilino)-6,7-dimethoxyquinazoline ((11)C-PD153035) has been reported as a tracer for imaging human tumors that overexpress epidermal growth factor receptor (EGFR). However it is still unclear whether (11)C-PD153035 uptake correlates with EGFR expression levels. The objective of this study was to investigate the relationship between (11)C-PD153035 accumulation and EGFR expression levels.

METHODS

Synthesis of (11)C-PD153035 was performed in the Tracerlab FXc system. Accumulation of (11)C-PD153035 by MDA-MB-468, A549 and MDA-MB-231 cells was measured in vitro. There were six tumor-bearing mice in each group. (11)C-PD153035 uptake in tumors was determined by positron emission tomography/computed tomography (PET/CT). Tumor/normal muscle tissue (T/NT) analysis in PET images was applied to quantify the PET data. Sixty minutes after PET/CT scanning, the nude mice were sacrificed and the tumors were excised. The (11)C-PD153035 accumulation in different tumors was determined by a gamma counter.

RESULTS

Close correlation existed between the uptake and the level of EGFR expression both in vitro and ex vivo (r(2) = 0.72, P < 0.001; r(2) = 0.63, P = 0.003). When the static T/NT analysis method was applied to analyze the PET data, the observed correlation was again excellent (r(2) = 0.70, P = 0.001).

CONCLUSIONS

The uptake of PET tracer (11)C-PD153035 closely correlates with the EGFR expression levels in tumor cells. (11)C-PD153035 has the potential to yield useful information for both cancer diagnosis and therapy.

摘要

背景

据报道，（11）C-4-N-（3-溴苯胺基）-6,7-二甲氧基喹唑啉（（11）C-PD153035）是一种用于对过表达表皮生长因子受体（EGFR）的人类肿瘤进行成像的示踪剂。然而，（11）C-PD153035摄取是否与EGFR表达水平相关仍不清楚。本研究的目的是探讨（11）C-PD153035蓄积与EGFR表达水平之间的关系。

方法

在Tracerlab FXc系统中进行（11）C-PD153035的合成。体外测定MDA-MB-468、A549和MDA-MB-231细胞对（11）C-PD153035的摄取。每组有6只荷瘤小鼠。通过正电子发射断层扫描/计算机断层扫描（PET/CT）测定肿瘤中（11）C-PD153035的摄取。PET图像中的肿瘤/正常肌肉组织（T/NT）分析用于量化PET数据。PET/CT扫描60分钟后，处死裸鼠并切除肿瘤。通过γ计数器测定不同肿瘤中（11）C-PD153035的蓄积。