Short peptides derived from hGAPDH exhibit anti-cancer activity. (1st October 2022)

• Record Type: Journal Article
• Authors: Yoshida, Junjiro; Takayama, Kentaro; Kawada, Manabu
• Is Part Of: Bioorganic & medicinal chemistry. Volume 71(2022)
• Publication Date: 2022-10-01
• Subjects: Peptide drug -- Anti-cancer drug -- GAPDH -- Unnatural amino acid; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2022.116953
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Peptides have become an attractive drug discovery modality alongside small molecule compounds and high molecular weight biomolecules because they bind strongly to their target molecules. Previously, we found that secreted extracellular human GAPDH exhibits inhibitory activity against cancer cell growth. We sought to identify the minimal peptide sequence required for GAPDH activity in an effort to develop a small GAPDH-derived peptide with anti-cancer activity. Moreover, derivatives of the identified peptide, in which some amino acid residues were substituted with unnatural amino acids, were found to show stronger anti-cancer activity than non-substituted peptides.