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Cy5.5-Polyethylene glycol-CGS25966 inhibitor of matrix metalloproteinases.


Leung K.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2013 Feb 14 [updated 2013 May 09].


Extracellular matrix (ECM) adhesion molecules consist of a complex network of fibronectins, collagens, chondroitins, laminins, glycoproteins, heparin sulfate, tenascins, and proteoglycans that surround connective tissue cells, and they are mainly secreted by fibroblasts, chondroblasts, and osteoblasts (1). Cell substrate adhesion molecules are considered essential regulators of cell migration, differentiation, and tissue integrity and remodeling. These molecules play a role in inflammation and atherogenesis, but they also participate in the process of invasion and metastasis of malignant cells in the host tissue (2). Tumor cells adhere to the ECM, which provides a matrix environment for permeation of tumor cells through the basal lamina and underlying interstitial stroma of the connective tissue. Overexpression of matrix metalloproteinases (MMPs) and other proteases by tumor cells allows intravasation of tumor cells into the circulatory system after degrading the basement membrane and ECM (3). Several families of MMPs are involved in atherogenesis, myocardial infarction, angiogenesis, and tumor invasion and metastasis (4-7). MMP expression is highly regulated in normal cells, such as trophoblasts, osteoclasts, neutrophils, and macrophages. Elevated levels of MMPs have been found in tumors associated with a poor prognosis for cancer patients (8). There are four members of endogenous tissue inhibitors of metalloproteinases (TIMP1-4), which regulate the activity of MMPs and lead to the inhibition of tumor growth and metastasis (9, 10). CGS25966 is a broad-spectrum, small-molecule inhibitor of MMPs (11). Faust et al. (11) inserted a polyethylene glycol (PEG) linker with an amino functional group for conjugation with the near-infrared (NIR) fluorescence dye Cy5.5 to form Cy5.5-PEG-CGS25966 (CY5.5-AF489). Waschkau et al. (12) evaluated Cy5.5-AF489 for use with in vivo NIR fluorescence imaging of tumors with high or low MMP-2/MMP-9 expression in nude mice.

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