Influence of the Topology of Poly(L-Cysteine) on the Self-Assembly, Encapsulation and Release Profile of Doxorubicin on Dual-Responsive Hybrid Polypeptides.

Τhe synthesis of a series of novel hybrid block copolypeptides based on poly(ethylene oxide) (PEO), poly(l-histidine) (PHis) and poly(l-cysteine) (PCys) is presented. The synthesis of the terpolymers was achieved through a ring-opening polymerization (ROP) of the corresponding protected -carboxy anhydrides of --l-histidine and --butyl-l-cysteine, using an end-amine-functionalized poly(ethylene oxide) (PEO-NH) as macroinitiator, followed by the deprotection of the polypeptidic blocks. The topology of PCys was either the middle block, the end block or was randomly distributed along the PHis chain.

Synthesis and Characterization of the Novel -9-Fluorenylmethoxycarbonyl-l-Lysine -Carboxy Anhydride. Synthesis of Well-Defined Linear and Branched Polypeptides.

The synthesis of well-defined polypeptides exhibiting complex macromolecular architectures requires the use of monomers that can be orthogonally deprotected, containing primary amines that will be used as the initiator for the Ring Opening Polymerization (ROP) of N-carboxy anhydrides. The synthesis and characterization of the novel monomer -9-Fluorenylmethoxycarbonyl-l-Lysine -carboxy anhydride (-Fmoc-l-Lysine NCA), as well as the novel linear Poly(-Fmoc-l-Lys) homopolypeptide and Poly(l-Lysine)--[Poly(l-Lysine)-t-Poly(l-Histidine)] block-graft copolypeptide, are presented. The synthesis of the graft copolypeptide was conducted via ROP of the -Boc-l-Lysine NCA while using -hexylamine as the initiator, followed by the polymerization of -Fmoc-l-Lysine NCA.