Multi-leu peptides and analogues thereof as selective pace4 inhibitors and effective antiproliferative agents
AssigneeSociete De Commercialisation Des Produits De La Recherche Appliquee Socpra San
InventorsRobert Day, Martin Fugére, 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.
Claims17
A method of reducing the proliferation of a cell in a subject, comprising administering a PACE4 inhibitor comprising a peptide sequence comprising the following formula:
- Y-Arg4-Xaa3-Xaa2-Arg1-NH2;
- wherein
- Arg1 is an arginine or arginine derivative;
- Xaa2 and Xaa3 are any amino acids or stereoisomers thereof;
- and
- Y is absent or comprises the formula Z-Xaa8-Xaa7-Xaa6-Xaa5, wherein
- Xaa5, Xaa6, Xaa7 and Xaa8 are aliphatic hydrophobic amino acids;
- Z is absent or comprises an N-terminal acyl group linked to the N-terminal of the peptide sequence;
- with the proviso that Xaa5, Xaa6, Xaa7 and Xaa8 are not aromatic or negatively charged amino acids,
- thereby reducing the proliferation of the cell in the subject.
Dependencies are inferred from the claim text.