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Adv Mater. 2013 Sep 14;25(34):4718-22. doi: 10.1002/adma.201301385. Epub 2013 Jul 12.

Novel conjugation of tumor-necrosis-factor-related apoptosis-inducing ligand (TRAIL) with monomethyl auristatin E for efficient antitumor drug delivery.

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  • 1Department of Pharmacology, Toxicology and Biochemical Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.


Monomethyl auristatin E (MMAE) is conjugated with TNF-related apoptosis-inducing ligand (TRAIL) via a linker that is stable in extracellular fluid, while it is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the antimitotic mechanism of MMAE. The TRAIL-MMAE conjugate is a conceptually viable therapeutic strategy with improved in vitro antitumor activity, cell circle arrest and specific accumulation in tumor to treat TRAIL-resistant tumors.

Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


antitumor agents; biomedical applications; drug delivery; protein modifications; protein-protein interactions

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