Novel conjugation of tumor-necrosis-factor-related apoptosis-inducing ligand (TRAIL) with monomethyl auristatin E for efficient antitumor drug delivery.
basic_science · Level V
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- Record sourced from PubMed, PMID 23847045.
- Also identified by DOI 10.1002/adma.201301385.
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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.
Medical subject headings
- Antineoplastic Agents
- Drug Carriers
- Oligopeptides
- TNF-Related Apoptosis-Inducing Ligand