Highly water-soluble, near-infrared emissive BODIPY polymeric dye bearing RGD peptide residues for cancer imaging.

Highly water-soluble, near-infrared emissive BODIPY polymeric dye bearing RGD peptide residues for cancer imaging.
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DOI:
10.1016/j.aca.2012.10.026
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发表时间:
2013-01-03
影响因子:
6.2
通讯作者:
Liu H
Liu H
中科院分区:
化学1区
文献类型:
--
作者:
Zhu S;Zhang J;Janjanam J;Bi J;Vegesna G;Tiwari A;Luo FT;Wei J;Liu H

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通过在温和碱性条件下将通过四乙二醇栓系的间隔基(聚合物A)带有溴基团的BODIPY聚合物染料与通过硫醚键的硫醇官能化的RGD癌症归巢肽(聚合物B)进行后聚合官能化,制备了带有癌症归巢环甘氨酸-甘氨酸-天冬氨酸(RGD)肽残基的近红外发射BODIPY聚合物染料(聚合物B)。聚合物B具有优良的水溶性、良好的光稳定性、生物相容性和对正常内皮细胞的非特异性相互作用的抗性,并且可以通过癌症归巢RGD肽与癌细胞的αVβ3整合素的特异性协同结合来有效地检测乳腺肿瘤细胞,而其母体聚合物A具有外RGD残基而不能靶向癌细胞。
Near-infrared emissive BODIPY polymeric dye bearing cancer-homing cyclic arginine-glycine-aspartic acid (RGD) peptide residues (polymer B) was prepared by post-polymerization functionalization of BODIPY polymeric dye bearing bromo groups through tetra(ethylene glycol tethered spacers (polymer A) with thiol-functionalized RGD cancer-homing peptide through thioether bonds under a mild basic condition. Polymer B possesses excellent water solubility, good photostability, biocompatibility and resistance to nonspecific interactions to normal endothelial cells, and can efficiently detect breast tumor cells through specific cooperative binding of cancer-homing RGD peptides to αVβ3 integrins of cancer cells while its parent polymer Awith outRGD residues fails to target cancer cells.
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