PEGylation of a Trail ligand.

This patent describes the synthesis of a polymeric conjugate of KillerTRAIL suitable for anti-cancer and anti-inflammatory therapies. The synthesis of therapeutic biomacromolecules was carried out by conjugating thiol group (-SH) of cysteine 230 of KillerTRAIL with PEG maleimide and thus obtains mPEG-KillerTRAIL derivative. This approach got the synthesis of stable biomacromolecules which can increase the stability of native KillerTRAIL, prevent its aggregation and improve KillerTRAIL shelf-life as well as other pharmacokinetic, biopharmaceutical parameters and the relative anti-cancer activity in vitro and in vivo.