ArticleBioconjugate chemistry2009
Evaluation of (64)Cu(DO3A-xy-TPEP) as a potential PET radiotracer for monitoring tumor multidrug resistance.
Article in Bioconjugate chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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7 citing papers in PubMed, 18 citations in OpenAlex.
- Imaging probes for non-invasive tumoral detection and functional monitoring of cancer multidrug resistance.Cancer drug resistance (Alhambra, Calif.) · 2020Article
- Mitochondria-Targeted Triphenylphosphonium-Based Compounds: Syntheses, Mechanisms of Action, and Therapeutic and Diagnostic Applications.Chemical reviews · 2017Review
- Optical imaging of tumors with copper-labeled rhodamine derivatives by targeting mitochondria.Theranostics · 2012Article
- The development of copper radiopharmaceuticals for imaging and therapy.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2011Review
- 64Cu-labeled phosphonium cations as PET radiotracers for tumor imaging.Bioconjugate chemistry · 2011Review
- 64Cu-labeled lissamine rhodamine B: a promising PET radiotracer targeting tumor mitochondria.Molecular pharmaceutics · 2011Article
- Evaluation of 64Cu-labeled acridinium cation: a PET radiotracer targeting tumor mitochondria.Bioconjugate chemistry · 2011Article
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Authors and funding
5 authors at 1 institution in 1 country.
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Abstract
In this study, we evaluated the potential of (64)Cu(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 (64)Cu(DO3A-xy-TPEP) has a high initial tumor uptake (5.27 +/- 1.2%ID/g at 5 min p.i.) and shows 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. (64)Cu(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 (99m)Tc-Sestamibi. Regardless of the source of MDR, the overall net effect is the rapid efflux of (64)Cu(DO3A-xy-TPEP) from tumor cells, which leads to a significant reduction of its tumor uptake. It was concluded that (64)Cu(DO3A-xy-TPEP) is more efficient than (99m)Tc-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. (64)Cu(DO3A-xy-TPEP) and (99m)Tc-Sestamibi share almost identical subcellular distribution patterns in U87MG glioma tumors. Thus, it is reasonable to believe that (64)Cu(DO3A-xy-TPEP), like (99m)Tc-Sestamibi, is able to localize in mitochondria due to the increased plasma and mitochondrial transmembrane potentials in tumor cells.
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