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Synthesis and Biological Characterization of Monomeric and Tetrameric RGD‐Cryptophycin Conjugates
2020
Chemistry - A European Journal
The effective delivery of cytotoxic agents to tumor cells is a key challenge in anticancer therapy. Multivalent integrinspecific ligands are considered a promising tool to increase the binding affinity, selectivity, and internalization efficiency of small-molecule drug conjugates. Herein, we report the synthesis and biological evaluation of a multimeric conjugate containing the high-affinity integrin αv β3 binding ligand RAFT-c(RGDfK)4 , a lysosomally cleavable Val-Cit linker, and
doi:10.1002/chem.201905437
pmid:31943410
pmcid:PMC7064988
fatcat:zjowirffvzh7lh5gpcwepkwxgm