Synthesis and investigation of a radioiodinated F3 peptide analog as a SPECT tumor imaging radioligand.
Synthesis and investigation of a radioiodinated F3 peptide analog as a SPECT tumor imaging radioligand.
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DOI：
10.1371/journal.pone.0022418
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发表时间：
2011
期刊：
影响因子：
3.7
通讯作者：
Van Dort ME
中科院分区：
文献类型：
--
作者：
Bhojani MS;Ranga R;Luker GD;Rehemtulla A;Ross BD;Van Dort ME
A radioiodinated derivative of the tumor-homing F3 peptide, (N-(2-{3-[125I]Iodobenzoyl}aminoethyl)maleimide-F3Cys peptide, [125I]IBMF3 was developed for investigation as a SPECT tumor imaging radioligand. For this purpose, we custom synthesized a modified F3 peptide analog (F3Cys) incorporating a C-terminal cysteine residue for site-specific attachment of a radioiodinated maleimide conjugating group. Initial proof-of-concept Fluorescence studies conducted with AlexaFluor 532 C5 maleimide-labeled F3Cys showed distinct membrane and nuclear localization of F3Cys in MDA-MB-435 cells. Additionally, F3Cys conjugated with NIR fluorochrome AlexaFluor 647 C2 maleimide demonstrated high tumor specific uptake in melanoma cancer MDA-MB-435 and lung cancer A549 xenografts in nude mice whereas a similarly labeled control peptide did not show any tumor uptake. These results were also confirmed by ex vivo tissue analysis. No-carrier-added [125I]IBMF3 was synthesized by a radioiododestannylation approach in 73% overall radiochemical yield. In vitro cell uptake studies conducted with [125I]IBMF3 displayed a 5-fold increase in its cell uptake at 4 h when compared to controls. SPECT imaging studies with [125I]IBMF3 in tumor bearing nude mice showed clear visualization of MDA-MB-435 xenografts on systemic administration. These studies demonstrate a potential utility of F3 peptide-based radioligands for tumor imaging with PET or SPECT techniques.
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影响因子：
4.7
作者：
Derfus, Austin M.;Chen, Alice A.;Bhatia, Sangeeta N.
通讯作者：
Bhatia, Sangeeta N.
影响因子：
4.8
作者：
Said, EA;Krust, B;Hovanessian, AG
通讯作者：
Hovanessian, AG
DOI：
10.1007/s00259-006-0136-0
发表时间：
2006-07-01
影响因子：
9.1
作者：
Haubner, Roland
通讯作者：
Haubner, Roland
影响因子：
3.7
作者：
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通讯作者：
Essler, Markus
影响因子：
64.5
作者：
BORER, RA;LEHNER, CF;NIGG, EA
通讯作者：
NIGG, EA