Development of Radiolabeled Membrane Type-1 Matrix Metalloproteinase Activatable Cell Penetrating Peptide Imaging Probes
作者： Sander van Duijnhoven , Marc Robillard , Klaas Nicolay , Holger Grüll
DOI: 10.3390/MOLECULES200712076
关键词:
摘要: Membrane type-1 matrix metalloproteinase (MT1-MMP or MMP-14) plays an important role in adverse cardiac remodelling. Here, we aimed to develop radiolabeled activatable cell penetrating peptides (ACPP) sensitive MT1-MMP for the detection of elevated levels Three ACPP analogs were synthesized and most potent analog was selected using sensitivity enzyme specificity assays. This ACPP, called ACPP-B, showed high towards MT1-MMP, soluble MMP-2, MT2-MMP, while limited measured other members MMP family. In vitro assays, ACPP-B efficient cellular uptake upon activation. A pilot vivo study increased probe regions infarcted myocardium compared remote myocardium, warranting further evaluation.
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