Abstract
Novel Pt(iv) tumour penetrating peptide (TPP) conjugates are reported. They are the first example of metallodrugs to target a membrane bound heat shock protein 70 positive (memHSP70+) phenotype in cancer cells. The conjugates exhibit superior cytotoxicity as compared to oxaliplatin alone in Pt resistant colorectal cancer cells with relatively high memHSP70+ expression. Substitution of TPP in Pt(iv) peptide conjugates with scrambled peptide (ScP) essentially abolishes the observed cytotoxicity.
MeSH terms
-
Amino Acid Sequence
-
Antineoplastic Agents / chemistry*
-
Antineoplastic Agents / toxicity
-
Cell Line, Tumor
-
Cell Survival / drug effects
-
Colorectal Neoplasms / metabolism
-
Colorectal Neoplasms / pathology
-
HCT116 Cells
-
HSP70 Heat-Shock Proteins / metabolism*
-
HT29 Cells
-
Humans
-
Organoplatinum Compounds / chemistry*
-
Oxaliplatin
-
Peptides / chemistry*
-
Platinum / chemistry*
Substances
-
Antineoplastic Agents
-
HSP70 Heat-Shock Proteins
-
Organoplatinum Compounds
-
Peptides
-
Oxaliplatin
-
Platinum