TY  - JOUR
AB  - The effective delivery of cytotoxic agents to the 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. Here we report the synthesis and biological evaluation of a multimeric conjugate containing the high-affinity integrin alpha v beta 3 binding ligand RAFT- c (RGDfK) 4 , a lysosomally cleavable Val-Cit linker and cryptophycin-55 glycinate, a potent inhibitor of tubulin polymerization. In vitro cytotoxicity assays verified that the multimeric RGD-cryptophycin conjugate displays improved potency compared to the monomeric analogue in integrin alpha v beta 3 overexpressing tumor cell lines, while significantly reduced activity was observed in the integrin-negative cell line. © 2020 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
DA  - 2020
DO  - 10.1002/chem.201905437
LA  - eng
IS  - 12
M2  - 2602
PY  - 2020
SN  - 0947-6539
SP  - 2602-2605
T2  - Chemistry - A European Journal
TI  - Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates.
UR  - https://nbn-resolving.org/urn:nbn:de:0070-pub-29403828
Y2  - 2024-11-22T08:16:52
ER  -