Polyphosphoinsitide binding peptides for intracellular drug delivery
AssigneeThe Brigham and Women's Hospital, Inc.
InventorsPaul A. Janmey, C. Casey Cunningham, John H. Hartwig, Thomas P. Stossel, Roland Vegner
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Abstract
Methods and compositions for facilitating the transport of a membrane-impermeable extracellular agent having an intracellular activity across the membrane of a cell are provided. The methods involve covalently coupling an amino terminal blocking group to a transport-mediating peptide to form a carrier molecule. The carrier molecule is covalently coupled to the extracellular agent to form a membrane-permeable prodrug. The transport-mediating peptides are highly basic and bind to polyphosphoinositides.
Claims13
A molecule having the formula X-P, wherein
- (a) P is a peptide selected from the group consisting of Seq. I.D. No. 1 and Seq. I.D. No. 2;
- and
- (b) X is rhodamine or a rhodamine derivative, wherein X is covalently coupled to the N-terminus amine of the peptide.
A molecule having the formula X-P, wherein
- (a) P is a peptide fragment of a peptide selected from the group consisting of Seq. I.D. No. 1 and Seq. I.D. No. 2, wherein the peptide fragment is a basic polyphosphoinositide binding peptide and contains between three and ten amino acids;
- and
- (b) X is rhodamine or a rhodamine derivative, wherein X is covalently coupled to the N-terminus amine of the peptide fragment.
A molecule having the formula X-P, wherein
- (a) P is a peptide that is a polyphosphoinositide binding peptide consisting essentially of between 3 and 10 amino acids of a polyphosphoinositide domain of a polyphosphoinositide binding protein;
- and
- (b) X is rhodamine or a rhodamine derivative, wherein X is covalently coupled to the N-terminus amine of the peptide.
Dependencies are inferred from the claim text.