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

TitleNovel conjugation of tumor-necrosis-factor-related apoptosis-inducing ligand (TRAIL) with monomethyl auristatin E for efficient antitumor drug delivery.
Publication TypeJournal Article
Year of Publication2013
AuthorsPan L-Q, Wang H-B, Xie Z-M, Li Z-H, Tang X-J, Xu Y-C, Zhang C, Naranmandura H, Chen S-Q
JournalAdvanced materials (Deerfield Beach, Fla.)
Volume25
Issue34
Pagination4718-22
Date Published2013 Sep 14
Abstract

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.

DOI10.1002/asia.201300600
Alternate JournalAdv. Mater. Weinheim