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/Site-specific PEGylation of a mutated-cysteine residue and its effect on tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL)
Site-specific PEGylation of a mutated-cysteine residue and its effect on tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) November 13,2023.
Biomaterials. 2013 Dec;34(36):9115-23.   doi: 10.1016/j.biomaterials.2013.08.020.   Epub 2013 Aug 24.

Site-specific PEGylation of a mutated-cysteine residue and its effect on tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL)

Li-Qiang Pan 1, Hai-Bin Wang, Jun Lai, Ying-Chun Xu, Chen Zhang, Shu-Qing Chen

Abstract


Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a promising antitumor agent that specifically induces apoptosis in broad-spectrum tumor cell lines, meanwhile leaving normal cells unaffected.   Unfortunately, the clinical development of TRAIL was hampered, and could be attributed to its instability, bioavailability or poor delivery.   Although N-terminal specific PEGylation provides a means to improve the pharmacokinetic and stability of TRAIL, it took a bit longer time to accomplish the PEGylation process than expected.   We therefore designed another PEGylation approach, mutated Cys-SH site-specific PEGylation, to conjugate methoxypoly(ethylene glycol) maleimide (mPEG-MAL) with TRAIL (95-281) mutant N109C.   Asn-109 was chosen as the PEGylated site for it is a potential N-linked glycosylation site.   It was shown that ~90% TRAIL mutant N109C could be PEGylated by mPEG-MAL within 40 min. And mPEG(MAL)-N109C was revealed to possess superior in vitro stability and antitumor activity than N-terminal specifically PEGylated TRAIL (114-281) (mPEG(ALD)-TRAIL(114-281)).   What's more, mPEG(MAL)-N109C exhibited more therapeutic potentials than mPEG(ALD)-TRAIL(114-281) in tumor xenograft model, benefitting from better drug delivery and bioavailability.   These results have demonstrated mutated Cys-SH specific PEGylation is an alternative to site-specifically PEGylate TRAIL efficiently and effectively other than N-terminal specific PEGylation.

Keywords: Antitumor agent;   Glycosylation site;   PEG-TRAIL;   Protein delivery;   Site-specific PEGylation.

Related products

Abbreviation: mPEG-pALD
Name: Methoxypoly(ethylene glycol) propionaldehyde

Abbreviation: mPEG-MAL
Name: Methoxypoly(ethylene glycol) maleimide

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