C07K14/70585

CD44V6-derived peptides for treating breast cancer

The present invention relates to compounds, pharmaceutical compositions and methods for treating different forms of breast cancer.

CD44 GLYCOEPITOPES AND CHIMERIC VACCINE GLYCOCONJUGATES FOR CANCER THERAPY AND SYNTHESIS METHODS THEREOF

Glycopeptides derived from short CD44 isoforms lacking amino acids encoded by exons 6-14; presenting one or multiple serine or threonine residues substituted with Tn (GalNAc-O-Ser/Thr) and/or sialyl-Tn (STn; Neu5Ac2-6GalNAc-O-Ser/Thr) antigens. Synthesizing the glycopeptides, including one-pot glycosylation of synthetic short isoform CD44 peptides through combination with nucleotide sugars and glycosyltransferases and purification of CD44s-Tn glycopeptides. Immunogenic chimeras derived from the CD44-Tn and/or STn glycopeptides, linked, in polyvalent form, to a carrier immunogenic protein, e.g., KLH CRM197. Conjugating the synthesized CD44s-Tn glycopeptides to the immunogenic protein carriers CRM197 and KLH, generating chimeric glycopeptides, termed CRM197-CD44s-Tn and KLH-CD44s-Tn. CD44-Tn/STn glycopeptides or compositions thereof for treating cancer and pre-neoplastic diseases, e.g., neoplastic diseases expressing short CD44 isoforms, through generating antibodies against cancer cells and treating/preventing cancer by vaccination. The glycopeptides, compositions, synthesis methods and uses can be employed in treating cancer, alone or in combination with immune checkpoint inhibitor therapy, chemotherapy, and radiotherapy.