Multi-LEU peptides and analogues thereof as selective PACE4 inhibitors and effective antiproliferative agents
OwnerRobert Day, Martin Fugère +1inventors
InventorsRobert Day, Martin Fugère, Witold A. Neugebauer
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Abstract
Disclosed herein are PACE4 inhibitors, compositions comprising PACE4 inhibitors and their uses thereof for lowering PACE4 activity, reducing cell proliferation, reducing tumor growth, reducing metastasis formation, preventing and/or treating cancer. Also provided are methods for lowering PACE4 activity, reducing the proliferation of a cell, reducing tumor growth and/or treating and preventing cancer. Methods for screening PACE4 inhibitors and cell proliferation inhibitors are further provided.
Claims9
A paired basic amino acid-cleaving enzyme 4 (PACE4) inhibitor comprising a peptide sequence consisting of the following formula:
- Y-Arg4-Val3-Lys2-Arg1-NH2;
- (SEQ ID NO:
- 1)
- wherein
- Arg1 is an arginine, or an arginine derivative;
- and
- Y comprises the formula Z-Xaa8-Xaa7-Xaa6-Xaa5, wherein
- Xaa5, Xaa6, Xaa7 and Xaa8 are Leu, Iso or Val;
- and
- Z is absent or comprises an N-terminal acyl group linked to the N-terminal of the peptide sequence.
Dependencies are inferred from the claim text.