DISULFIDE-LINKED POLYETHYLENEGLYCOL/PEPTIDE CONJUGATES FOR THE TRANSFECTION OF NUCLEIC ACIDS

  • US 20110053829A1
  • Filed: 09/03/2009
  • Published: 03/03/2011
  • Est. Priority Date: 09/03/2009
  • Status: Abandoned Application
First Claim
Patent Images

1. Polymeric carrier molecule according to generic formula (I):


  • L-P1

    S—

    [S—

    P2

    S]n

    S—

    P3-Lwherein,P1 and P3 represent a linear or branched hydrophilic polymer chain, each P1 and P3 exhibiting at least one —

    SH-moiety, capable to form a disulfide linkage upon condensation with component P2, the linear or branched hydrophilic polymer chain selected independent from each other from polyethylene glycol (PEG), poly-N-(2-hydroxypropyl)methacrylamide, poly-2-(methacryloyloxy)ethyl phosphorylcholines, poly(hydroxyalkyl L-asparagine) or poly(hydroxyalkyl L-glutamine), wherein the hydrophilic polymer chain exhibits a molecular weight of about 1 kDa to about 100 kDa;

    P2 is a cationic or polycationic peptide or protein, having a length of about 3 to 100 amino acids, oris a cationic or polycationic polymer, having a molecular weight of about 0.5 kDa to about 100 kDa,each P2 exhibiting at least two —

    SH-moieties, capable to form a disulfide linkage upon condensation with component(s) P1 and/or P3;



    S—

    S—

    is a (reversible) disulfide bond;

    L is an optional ligand, selected independent from the other from RGD, Transferrin, Folate, a signal peptide or signal sequence, a localization signal or sequence, a nuclear localization signal or sequence (NLS), an antibody, a cell penetrating peptide, or TAT;

    n is an integer, selected from a range of about 1 to 50.

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