Peptides whose uptake by cells is controllable
A generic structure for the peptides of the present invention includes A-X-B-C, where C is a cargo moiety, the B portion includes basic amino acids, X is a cleavable linker sequence, and the A portion includes acidic amino acids. The intact structure is not significantly taken up by cells; however, upon extracellular cleavage of X, the B-C portion is taken up, delivering the cargo to targeted cells. Cargo may be, for example, a contrast agent for diagnostic imaging, a chemotherapeutic drug, or a radiation-sensitizer for therapy. Cleavage of X allows separation of A from B, unmasking the normal ability of the basic amino acids in B to drag cargo C into cells near the cleavage event. X is cleaved extracellularly, preferably under physiological conditions. D-amino acids are preferred for the A and B portions, to minimize immunogenicity and nonspecific cleavage by background peptidases or proteases.
- Research Organization:
- The Regents of the University of California, Oakland, CA, USA
- Sponsoring Organization:
- USDOE
- DOE Contract Number:
- FG03-01ER63276
- Assignee:
- The Regents of the University of California (Oakland, CA)
- Patent Number(s):
- 8,642,561
- Application Number:
- 13/314,134
- OSTI ID:
- 1118269
- Resource Relation:
- Patent File Date: 2011 Dec 07
- Country of Publication:
- United States
- Language:
- English
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