Method for delivery of molecules to intracellular targets
AssigneeWisconsin Alumni Research Foundation
InventorsSamuel H. Gellman, Naoki Umezawa, Michael A. Gelman, Ronald T. Raines, Terra Potocky
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Abstract
Disclosed are β-peptides and β-peptide conjugates that are capable of diffusing or otherwise being transported across the cell membranes of living cells. The β-peptides contain at least six β-amino acid residues, at leastsix of which are preferably β3-homoarginine residues. It has been found that when pharmacologically-active agents are conjugated to these types of β-peptides, the resulting conjugates (also disclosed herein) are also capable of diffusing or otherwise being transported across the cell membranes of living cells, including mammalian cells.
Claims26
A method of translocating a molecule across a membrane of a living cell, the method comprising:
- conjugating the molecule to an oligopeptide, the oligopeptide comprising at least 6 β-amino acid residues, at least 6 of which residues are substituted at their β-position carbon with a substituent selected from the group consisting of —C1-C6-NH—C(═NH2+)—NH2, to thereby yield a conjugate;
- and then
- contacting the conjugate with the living cell.
A method of translocating a molecule across a membrane of a living cell, the method comprising contacting a conjugate with the living cell, the conjugate comprising the molecule conjugated to an oligopeptide comprising at least 6 β-amino acid residues, at least 6 of which residues are substituted at their β-position carbon with a substituent selected from the group consisting of —C1-C6-NH—C(═NH2+)—NH2.
A β-peptide comprising at least 6 β-amino acid residues, at least 6 of which residues are substituted at their β-position carbon with a substituent selected from the group consisting of-C1-C6-NH—C(═NH2+)—NH2, the β-peptide being capable of translocating across a membrane of a living cell.
A conjugate comprising:
- a β-peptide vehicle, the β-peptide vehicle comprising at least 6 β-amino acid residues, at least 6 of which residues are substituted at their β-position carbon with a substituent selected from the group consisting of —C1-C6-NH—C(═NH2+)—NH2;
- and
- a molecule of interest conjugated to the β-peptide vehicle.
Dependencies are inferred from the claim text.