Treating cancer

摘要

Provided is a cyclic peptide which comprises:
(i) a CDK4 peptide region; and(ii) a cell-penetrating region;

wherein the CDK4 peptide region comprises the amino acid sequence P1R1x1y1R2P2V (SEQ ID NO: 1), in which P1 and P2 are each proline, R1 and R2 are each arginine and each of x1 and y1 are either a linker or proline, wherein if x1 is a linker then y1 is proline or if x1 is proline then y1 is a linker, or wherein x1 and y1 when taken together form a linker, and wherein V may be present or absent; and

wherein the cell-penetrating region is capable of enhancing the uptake of the cyclic peptide or a part thereof into cancer cells and comprises an amphiphilic amino acid sequence; and wherein the cyclic peptide or a part thereof is cytotoxic to and/or inhibiting to the growth of a cancer cell.

主权项

1. A cyclic peptide which comprises:
(i) a CDK4 peptide region; and (ii) a cell-penetrating region; wherein the CDK4 peptide region comprises the amino acid sequence P1R1x1y1R2P2V (SEQ ID NO: 1), in which P1 and P2 are each proline, R1 and R2 are each arginine and each of x1 and y1 are either a linker or proline, wherein if x1 is a linker then y1 is proline or if x1 is proline then y1 is a linker, or wherein x1 and y1 when taken together form a linker, and wherein V may be present or absent; wherein each amino acid is the L stereoisomer or wherein the valine residue of the amino acid sequence P1R1x1y1R2P2V (SEQ ID NO: 1) of the CDK4 peptide region is the D stereoisomer and all other amino acids in the cyclic peptide are the L stereoisomer; and wherein the cell-penetrating region is capable of enhancing the uptake of the cyclic peptide or a part thereof into cancer cells and comprises an amphiphilic amino acid sequence; and wherein the cyclic peptide or a part thereof is cytotoxic to and/or inhibiting to the growth of a cancer cell.