Peptide inhibitors of focal adhesion kinase activity and uses thereof
AssigneeArizona Board of Regents on Behalf of the University of Arizona
InventorsTimothy Marlowe, Warren S. Weiner
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Abstract
This disclosure provides peptides which have an affinity for the focal adhesion targeting (FAT) domain of focal adhesion kinase (FAK). In particular, the peptides are modified and derived from the sequence of the LD2 alpha helical domain of paxillin (e.g., LD2 peptides), the LD4 domain of paxillin (e.g., LD4 peptides), and CD8 peptides. These peptides are capable of blocking an interaction between paxillin and FAK, thereby inhibiting FAK activity related to FAK-paxillin interaction. The invention further provides uses for such peptides as therapeutics for the treatment of cancer and other diseases characterized with FAK activity and/or expression (e.g., fibrosis).
Claims9
A composition comprising a compound comprising Myristoyl-NLR8ELDRLLS5ELN-NH2 (SEQ ID NO:
- 28),
- wherein in the peptide NLR8ELDRLLS5ELN-NH2 (SEQ ID NO:
- 28),
- R8 is (R)-2-(7-octenyl)alanine,
- S5 is (S)-2-(4-pentenyl)alanine, and
- R8 and S5 have undergone a ring-closure metathesis reaction to yield the structure:
- and
- Myristoyl is covalently attached to the N-terminal amino group.
Dependencies are inferred from the claim text.