Impact of PKM Linkers on Biodistribution Characteristics of the 99mTc-Labeled Cyclic RGDfK Dimer
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- 作者：Shuang Liu ; Zhengjie He ; Wen-Yuan Hsieh ; Young-Seung Kim ; Young Jiang
- 刊名：Bioconjugate Chemistry
- 出版年：2006
- 出版时间：November 2006
- 年：2006
- 卷：17
- 期：6
- 页码：1499 - 1507
- 全文大小：183K
- 年卷期：v.17,no.6(November 2006)
- ISSN：1520-4812
文摘
This report describes synthesis of three new cyclic RGDfK peptide conjugates, HYNIC-PKM-SU016 (PKM =E, K and PEG4) and in vivo evaluation of the impact of PKM linkers on biodistribution characteristics of theirternary ligand complexes [99mTc(HYNIC-PKM-SU016)1(tricine)(TPPTS)] in athymic nude mice bearing theMDA-MB-435 human breast cancer xenografts. Results from biodistribution studies show that PKM linkers haveminimal impact on the integrin 
v
3 binding capability of radiotracers. Even though they have different chargesunder physiological conditions, all three linkers (E, K, and PEG4) are able to reduce the uptake of 99mTc-labeledE[c(RGDfK)]2 in blood, kidneys, liver, and lungs, and increase target-to-background (T/B) ratios at >30 minpostinjection. E and K may have advantages over PEG4 due to a combination of relatively low liver uptake andhigh tumor/liver and tumor/lung ratios of ternary ligand complexes [99mTc(HYNIC-PKM-SU016)(tricine)(TPPTS)] (PKM = E and K).
v3 binding capability of radiotracers. Even though they have different chargesunder physiological conditions, all three linkers (E, K, and PEG4) are able to reduce the uptake of 99mTc-labeledE[c(RGDfK)]2 in blood, kidneys, liver, and lungs, and increase target-to-background (T/B) ratios at >30 minpostinjection. E and K may have advantages over PEG4 due to a combination of relatively low liver uptake andhigh tumor/liver and tumor/lung ratios of ternary ligand complexes [99mTc(HYNIC-PKM-SU016)(tricine)(TPPTS)] (PKM = E and K).