Mechanism of anticancer activity of buforin IIb, a histone H2A-derived peptide.
Buforin IIb is a novel cell-penetrating anticancer peptide derived from histone H2A. Here we analyzed the anticancer activity and cancer cell-killing mechanism of buforin IIb. Buforin IIb displayed selective cytotoxicity against 62 cancer cell lines by specifically targeting cancer cells through interaction with cell surface gangliosides. It traversed cancer cell membranes without damaging them and accumulated primarily in the nuclei. Once inside the cells, buforin IIb induced mitochondria-dependent apoptosis. In vivo analysis revealed that buforin IIb displayed significant tumor suppression activity in mice with tumor xenograft. Overall, these results suggest that buforin IIb constitutes a novel therapeutic agent for the treatment of cancers.
Lee
Hyun Soo
HS
Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, South Korea.
Park
Chan Bae
CB
Kim
Jung Min
JM
Jang
Su A
SA
Park
In Yup
IY
Kim
Mi Sun
MS
Cho
Ju Hyun
JH
Kim
Sun Chang
SC
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005434:Flow Cytometry; D006801:Humans; D051379:Mice; D018613:Microscopy, Confocal; D008856:Microscopy, Fluorescence; D009368:Neoplasm Transplantation; D011506:Proteins / Q000494:pharmacology*
D000970:Antineoplastic Agents; D011506:Proteins; C097849:buforin II