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CD44v6, a cancer-associated membrane glycoprotein splice variant of CD44, is involved in cell adhesion and tumor progression and has been implicated as a novel biomarker for aggressive prostate carcinomas (PCa). Synthetic peptides have advantages for in vivo targeting and imaging, due to their small size and good tissue penetration. The phage display selected peptides targeting CD44v6 were investigated to form the foundation for efficacious aggressive PCa theranostic agents.

Phage libraries displaying linear peptides and disulfide-constrained peptides were subjected to three rounds of selection based on their ability to bind to the v6 region of CD44v6. To enhance the solubility of v6p1, amino acids Asp and Arg were introduced at both ends to produce the peptide DRDv6p1.

Four peptides displayed by phage which demonstrated superior binding and specificity, were …