Synthesis and preliminary evaluation of a novel 125I-labeled T140 analog for quantitation of CXCR4 expression

Han, Yanjiang; Yin, Duanzhi; Zheng, Ming-Qiang; Zhou, Wei; Lee, ZhenHong; Zhan, Lisi; Ma, Yufei; Wu, Mingxing; Shi, Lingli; Wang, Ni; Lee, Jianbo; Wang, Cheng; Lee, Zheng; Wang, Yongxian

doi:10.1007/s10967-010-0484-x

Cited by 9 publications

(14 citation statements)

References 25 publications

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“…Both cell lines were incubated with 1 mm of Ir III conjugates 8-10, after which the mean fluorescence intensity ratio (MFIR) was measured with flow cytometry by using the luminescent signature of the Ir III complex (Table 3). The ratios of the MFIRs of the two cell lines for Ir-(Ac-TZ14011) (8) and Ir-(Ac-TZ14011) 2 (9) were significantly higher than 1 (p < 0.05), namely 1.17 and 1.32, respectively (Table 3). For Ir-(Ac-TZ14011) 3 (10) the ratio even approached that found with the 12G5-PE antibody: 1.72 (p < 0.01).…”

Section: Cell Viability Cxcr4 Affinity and Specificitymentioning

confidence: 96%

“…With up to 3 mm none of the conjugates yielded effects on the viability (Figure 5 A). At 10 mm conjugate Ir-(Ac-TZ14011) (8) still displayed little toxicity, whereas Ir-(Ac-TZ14011) 2 (9) and Ir-(Ac-TZ14011) 3 (10) were considerably more toxic. The reduced viability of derivatives 9 and 10 could be the result of the large amount of positive charges present: each Ac-TZ14011 peptide possesses five positive charges, thus conjugate 9 is +10 charged and conjugate 10 is even +15 charged.…”

Section: Cell Viability Cxcr4 Affinity and Specificitymentioning

confidence: 99%

“…For competition experiments different concentrations ranging between 0-10 000 nm of Ir-(Ac-TZ14011) (8), Ir-(Ac-TZ14011) 2 (9) or Ir-(Ac-TZ14011) 3 (10) in the presence of Ac-TZ14011-MSAP (11; 250 nm) in 50 mL of bovine serum albumin (BSA; 0.1 %) in PBS were added. Cells were incubated for 1 h at 4 8C.…”

Section: Determination Of Dissociation Constants By Flow Cytometry: Mmentioning

confidence: 99%

“…[6,7] Because of its prominent role in oncology, overexpression of CXCR4 has been suggested to be of value in diagnostic imaging applications. [8,9] For CXCR4 targeting several peptidic probes have been reported, including the cyclic Ac-TZ14011 peptide, and also a chelate-based fluorescent probe. [10][11][12][13][14][15][16] Transition-metal complexes based on, for example, iridium-(III), rhenium(I) and ruthenium(II) are attaining significant interest for application in imaging.…”

Section: Introductionmentioning

confidence: 99%

“…[17,21,22,39] However, a neutral Ir III complex functionalized with peptides for specific targeting of a cancer associated membrane receptor has not been reported yet. In this paper, we present CXCR4 targeting with three different Ac-TZ14011 peptide-conjugated Ir III complexes, Ir-(Ac-TZ14011) (8), Ir-(Ac-TZ14011) 2 (9) and Ir-(Ac-TZ14011) 3 (10).…”

Section: Introductionmentioning

confidence: 99%

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Peptide‐Functionalized Luminescent Iridium Complexes for Lifetime Imaging of CXCR4 Expression

et al. 2011

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The chemokine receptor 4 (CXCR4) is over-expressed in 23 types of cancer in which it plays a role in, among others, the metastatic spread. For this reason it is a potential biomarker for the field of diagnostic oncology. The antagonistic Ac-TZ14011 peptide, which binds to CXCR4, has been conjugated to luminescent iridium dyes to allow for CXCR4 visualization. The iridium dyes are cyclometalated octahedral iridium(III) 2-phenylpyridine complexes that can be functionalized with one, two or three targeting Ac-TZ14011 peptides. Confocal microscopy and fluorescence lifetime imaging microscopy (FLIM) showed that the peptide-iridium complex conjugates can be used to visualize CXCR4 expression in tumor cells. The CXCR4 receptor affinity and specific cell binding of the mono-, di- and trimeric peptide derivatives were assessed by using flow cytometry. The three derivatives possessed nanomolar receptor affinity and could distinguish between cell lines with different CXCR4 expression levels. This yields the first example of a neutral iridium(III) complex functionalized with peptides for FLIM-based visualization of a cancer associated membrane receptor.

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Section: Cell Viability Cxcr4 Affinity and Specificitymentioning

confidence: 96%

Section: Cell Viability Cxcr4 Affinity and Specificitymentioning

confidence: 99%

Section: Determination Of Dissociation Constants By Flow Cytometry: Mmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Peptide‐Functionalized Luminescent Iridium Complexes for Lifetime Imaging of CXCR4 Expression

et al. 2011

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Molecular Imaging of CXCR4 Receptor Expression in Tumors

Woodard

Nimmagadda

2011

Novel Developments in Stem Cell Mobilization

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Metastasis is responsible for most cancer-related deaths. Chemokine receptors have been shown to aid tumor propagation at the key steps of metastasis, including the adherence of tumor cells to the endothelium, extravasation from blood vessels, colonization, angiogenesis, proliferation, and protection from the host immune response. The CXCR4/CXCL12 axis plays a major role in the homing of CXCR4 positive tumor cells to distant metastatic sites. Over the last few years, several agents have been evaluated for monitoring CXCR4 expression using PET, SPECT, and optical imaging modalities in preclinical models. This chapter discusses the current status of CXCR4-targeted probe development. As these agents become clinically available, CXCR4-based imaging could play an important role in detecting tumors with high risk for metastasis, in the early detection of metastases and in therapeutic monitoring.

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Synthesis and preliminary biodistribution studies of [131I]SIB-PEG4-CHC in tumor-bearing mice

Zheng

Dong

Yang

et al. 2010

J Radioanal Nucl Chem

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Synthesis and preliminary evaluation of a novel 125I-labeled T140 analog for quantitation of CXCR4 expression

Cited by 9 publications

References 25 publications

Peptide‐Functionalized Luminescent Iridium Complexes for Lifetime Imaging of CXCR4 Expression

Peptide‐Functionalized Luminescent Iridium Complexes for Lifetime Imaging of CXCR4 Expression

Molecular Imaging of CXCR4 Receptor Expression in Tumors

Synthesis and preliminary biodistribution studies of [131I]SIB-PEG4-CHC in tumor-bearing mice

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