In this present study, we prepared cRGD-conjugates using different linkers and determined how they altered the tumor targeting efficiency in vitro and in vivo. The results demonstrate that different linkers significantly altered the pharmacokinetics of the cRGD conjugates and the tumor uptake kinetics. Unlike large antibodies, this preliminary finding shows that linkers used to attach drugs and fluorescent molecular probes to small peptides play a major role in the accuracy of tumor targeting and treatment outcomes. As a result, considerable attention should be paid to the nature of linkers used in the design of molecular probes and targeted therapeutics.
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Partha Karmakar, Dorota Grabowska, Gail Sudlow, Kostiantyn Ziabrev, Nibedita Sanyal, Samuel Achilefu, "Effect of linkers on the αvβ3 integrin targeting efficiency of cyclic RGD-conjugates.," Proc. SPIE 10508, Reporters, Markers, Dyes, Nanoparticles, and Molecular Probes for Biomedical Applications X, 1050809 (20 February 2018);