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- W2406758445 abstract "Fluorescein-conjugated cyclic decapeptides, CGLIIQKNEC (CLT1) and CNAGESSKNC (CLT2), abbreviated as fluorescent CLT peptides, are two peptide agents that specifically home to tumors and wounds and are potentially useful for tumor-targeted imaging and therapy (1).Tumor tissue is different from normal tissue in the content and function of its stroma. At the initial stage of tumor development, tumor cells secrete growth factors, including vascular permeability factor that renders the local microvasculature hyperpermeable to fibrinogen and other plasma proteins. Extravasated fibrinogen crosslinks with fibrin and other proteins, forming a meshwork in the tumor stroma (1, 2). This sequence also occurs in the process of wound-healing and in the progression of many other diseases, but the tumor stroma contains increased amounts of fibrinogen, collagen, fibronectin, fibrinogen-derived products, and other proteins (3). These proteins either come from the leaky blood vessels or are inappropriately synthesized by the tumor cells. Functionally, normal stroma generates an antiproliferative environment, whereas tumor stroma promotes tumor cell proliferation, migration, and lymphovascular invasion by providing adhesion proteins, proteases, and growth factors (2, 4).Abnormal formation of clotted plasma protein meshwork in the tumor stroma and on the tumor blood vessel walls has prompted investigators to generate tumor stroma-targeted imaging and therapeutic agents. Pilch et al. screened a phage library on plasma clots and obtained two cyclic decapeptides (CLT; CLT1 and CLT2) (1). The fluorescence-labeled CLT peptides specifically accumulated in the fibrillar meshwork that existed in the tumor stroma, but they were not detectable in other tissues in animal models of human tumors. Ye et al. conjugated the CLT1 peptide with gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA), and the generated agent Gd-DTPA-CLT1 exhibited high specificity to the fibronectin-fibrin complexes in the tumor stroma (5). Simberg et al. also reported the clotted plasma protein-targeted multimodal agent CREKA-SPIO-Cy7 , which was synthesized by conjugation of the peptide CREKA with superparamagnetic iron oxide and cyanine 7 (6). On the basis of the interaction between the fibrinogen-derived products and heparin, Yuk et al. synthesized the MRI contrast agent, Composite NPs, using heparin as the specific ligand (7, 8). Composite NPs have been shown to selectively distribute in tumors in an animal model of murine squamous cell carcinoma (7). This chapter summarizes the data obtained with the fluorescent CLT peptides (1)." @default.
- W2406758445 created "2016-06-24" @default.
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- W2406758445 date "2012-08-28" @default.
- W2406758445 modified "2023-09-23" @default.
- W2406758445 title "Fluorescein-conjugated cyclic decapeptides, CGLIIQKNEC (CLT1) and CNAGESSKNC (CLT2)" @default.
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