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Li-Qiang Pan, Hai-Bin Wang, Zhang-Ming Xie, Zhao-Hui Li, Xiao-Jing Tang, Ying-Chun Xu, Chen Zhang, Hua Naranmandura and Shu-Qing Chen Novel Conjugation of Tumor-Necrosis-Factor-Related Apoptosis-Inducing Ligand (TRAIL) with Monomethyl Auristatin E for Efficient Antitumor Drug Delivery Advanced Materials 25

Version of Record online: 12 JUL 2013 | DOI: 10.1002/adma.201301385

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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.

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