Novel Conjugation of Tumor-Necrosis-Factor-Related Apoptosis-Inducing Ligand (TRAIL) with Monomethyl Auristatin E for Efficient Antitumor Drug Delivery

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 conjugat...

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Bibliographic Details
Published in:Advanced materials (Weinheim) 2013-09, Vol.25 (34), p.4718-4722
Main Authors: Pan, Li-Qiang, Wang, Hai-Bin, Xie, Zhang-Ming, Li, Zhao-Hui, Tang, Xiao-Jing, Xu, Ying-Chun, Zhang, Chen, Naranmandura, Hua, Chen, Shu-Qing
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemistry
Antineoplastic Agents - toxicity
antitumor agents
Apoptosis - drug effects
biomedical applications
Cathepsins - metabolism
Cell Cycle Checkpoints - drug effects
Conjugates
Conjugation
Drug Carriers - chemistry
drug delivery
Fluid dynamics
Fluid flow
Fluids
Humans
Ligands
MCF-7 Cells
Microscopy, Confocal
Oligopeptides - chemistry
protein modifications
protein-protein interactions
Recombinant Proteins - biosynthesis
Recombinant Proteins - chemistry
Recombinant Proteins - toxicity
Strategy
TNF-Related Apoptosis-Inducing Ligand - chemistry
TNF-Related Apoptosis-Inducing Ligand - genetics
TNF-Related Apoptosis-Inducing Ligand - toxicity
Tumors
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Summary: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.
ISSN:0935-9648
1521-4095
DOI:10.1002/adma.201301385