Steroid acid-peptide based cytotoxic compounds
AssigneeDefence Therapeutics Inc.
InventorSimon Beaudoin
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Abstract
Agents having cytotoxic activity, as well as compositions, uses, and methods relating thereto, are described herein. Certain steroid acid-peptide conjugates or moieties have the ability to induce killing or inhibition of proliferation of mammalian cells, in vitro or in vivo upon administration to a subject. The steroid acid-peptide conjugates include bile acids and bile acid analogs and peptides that may include a nuclear localisation signal or a portion thereof. Also described herein is a method for treating cancer, an autoimmune disease, or any other disease or disorder ameliorated by treatment with an antiproliferative drug in a subject in a subject with the cytotoxic agents described herein.
Claims20
A pharmaceutical composition comprising a bile acid-peptide conjugate as a cytotoxic or cytostatic agent, the conjugate being free or releasably bound to a carrier molecule and being present in the pharmaceutical composition at an effective concentration of at least 40 micromolar, wherein the peptide comprised in the bile acid-peptide conjugate comprises a nuclear localization signal (NLS), wherein the bile acid-peptide conjugate when releasably bound to the carrier molecule is bound via an enzymatically cleavable linker, a photocleavable linker, a redox-sensitive linker, or a pH-sensitive linker, and wherein the carrier molecule is not a polypeptide antigen.
A pharmaceutical composition comprising a bile acid-peptide conjugate as a cytotoxic or cytostatic agent, the conjugate being free or releasably bound to a carrier molecule and being present in the pharmaceutical composition at an effective concentration of at least 40 micromolar, wherein the bile acid comprises chenodeoxycholic acid (CDCA) and the peptide comprises an SV40 NLS (SEQ ID NO:
- 1 or 2), wherein the bile acid-peptide conjugate when releasably bound to the carrier molecule is bound via an enzymatically cleavable linker, a photocleavable linker, a redox-sensitive linker, or a pH-sensitive linker, and wherein the carrier molecule is not a polypeptide antigen.
Dependencies are inferred from the claim text.