4 research outputs found
Replacement of the Disulfide Bridge in a KLK3-Stimulating Peptide Using Orthogonally Protected Building Blocks
Peptide âB-2â, which
is one of the most potent kallikrein-related
peptidase 3 (KLK3)-stimulating compounds, consists of 12 amino acids
and is cyclized by a disulfide bridge between the N- and C-terminal
cysteines. Orthogonally protected building blocks were used in the
peptide synthesis to introduce a disulfide bridge mimetic consisting
of four carbon atoms. The resulting pseudopeptides with alkane and <i>E</i>-alkene linkers doubled the proteolytic activity of KLK3
at a concentration of 14 ÎŒM. They were almost as potent as the
parent âB-2â peptide, which gives a 3.6-fold increase
in the proteolytic activity of KLK3 at the same concentration