Evaluation of (64)Cu(DO3A-xy-TPEP) as a potential PET radiotracer for monitoring tumor multidrug resistance.
Evaluation of (64)Cu(DO3A-xy-TPEP) as a potential PET radiotracer for monitoring tumor multidrug resistance.
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DOI：
10.1021/bc800545e
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发表时间：
2009-04
影响因子：
4.7
通讯作者：
Hou G
中科院分区：
文献类型：
--
作者：
Liu S;Kim YS;Zhai S;Shi J;Hou G
In this study, we evaluated the potential of 64Cu(DO3A-xy-TPEP) (DO3A-xy-TPEP = (2-(diphenylphosphoryl)ethyl)diphenyl(4-((4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)methyl)benzyl)phosphonium) as a PET (positron emission tomography) radiotracer for noninvasive monitoring of multidrug resistance (MDR) transport function in several xenografted tumor models (MDR-negative: U87MG; MDR-positive: MDA-MB-435, MDA-MB-231, KB-3-1 and KB-v-1). It was found that 64Cu(DO3A-xy-TPEP) has a high initial tumor uptake (5.27 ± 1.2 %ID/g at 5 min p.i.) and show a steady uptake increase between 30 and 120 min p.i. (2.09 ± 0.53 and 3.35 ± 1.27 %ID/g at 30 and 120 min p.i., respectively) in the MDR-negative U87MG glioma tumors. 64Cu(DO3A-xy-TPEP) has a greater uptake difference between U87MG glioma and MDR-positive tumors (MDA-MB-231: 1.57 ± 0.04, 1.00 ± 0.17, and 0.93 ± 0.15; MDA-MB-435: 1.15 ± 0.19, 1.12 ± 0.20, and 0.81 ± 0.11; KB-3-1: 1.45 ± 0.31, 1.43 ± 0.16, and 1.08 ± 0.19; and KB-v-1: 1.63 ± 0.47, 1.81 ± 0.31, and 1.14 ± 0.22 %ID/g at 30, 60 and 120 min p.i., respectively) than 99mTc-Sestamibi. Regardless of the source of MDR, the overall net effect is the rapid efflux of 64Cu(DO3A-xy-TPEP) from tumor cells, which leads to a significant reduction of its tumor uptake. It was concluded that 64Cu(DO3A-xy-TPEP) is more efficient than 99mTc-Sestamibi as the substrate for MDR P-glycoproteins (MDR Pgps) and multidrug resistance-associated proteins (MRPs), and might be a more efficient radiotracer for noninvasive monitoring of the tumor MDR transport function. 64Cu(DO3A-xy-TPEP) and 99mTc-Sestamibi share almost identical subcellular distribution patterns in U87MG glioma tumors. Thus, it is reasonable to believe that 64Cu(DO3A-xy-TPEP), like 99mTc-Sestamibi, is able to localize in mitochondria due to the increased plasma and mitochondrial transmembrane potentials in tumor cells.
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影响因子：
10.6
作者：
Duchen, Michael R.
通讯作者：
Duchen, Michael R.
影响因子：
64.8
作者：
GROS, P;BEN-NERIAH, Y;HOUSMAN, DE
通讯作者：
HOUSMAN, DE
DOI：
10.1093/jnci/89.22.1706
发表时间：
1997-11-19
期刊：
JOURNAL OF THE NATIONAL CANCER INSTITUTE
影响因子：
--
作者：
Chan, HSL;Grogan, TM;Ling, V
通讯作者：
Ling, V
影响因子：
2.8
作者：
Dyszlewski, Mary;Blake, Helen M;Piwnica-Worms, David
通讯作者：
Piwnica-Worms, David
影响因子：
3.5
作者：
HIJAZI, YM;AXIOTIS, CA;TSOKOS, M
通讯作者：
TSOKOS, M