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.

Conformational Properties of New Thiosemicarbazone and Thiocarbohydrazone Derivatives and Their Possible Targets.

The structure assignment and conformational analysis of thiosemicarbazone and thiocarbohydrazone were performed through homonuclear and heteronuclear 2D Nuclear Magnetic Resonance (NMR) spectroscopy (2D-COSY, 2D-NOESY, 2D-HSQC, and 2D-HMBC) and quantum mechanics (QM) calculations using Functional Density Theory (DFT). After the structure identification of the compounds, various conformations of the two compounds were calculated using DFT. The two molecules showed the most energy-favorable values when their two double bonds adopted the configuration.

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.

Nanostructured Polymeric, Liposomal and Other Materials to Control the Drug Delivery for Cardiovascular Diseases.

Cardiovascular diseases (CVDs) are the leading cause of death globally, taking an estimated 17.9 million lives each year, representing one third of global mortality. As existing therapies still have limited success, due to the inability to control the biodistribution of the currently approved drugs, the quality of life of these patients is modest.