1516886-27-3Relevant articles and documents
Replacement of the disulfide bridge in a KLK3-stimulating peptide using orthogonally protected building blocks
Meinander, Kristian,Pakkala, Miikka,Weisell, Janne,Stenman, Ulf-Haiskan,Koistinen, Hannu,Naervaenen, Ale,Wallen, Erik A. A.
, p. 162 - 165 (2014)
Peptide B-2 , 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 E-alkene linkers doubled the proteolytic activity of KLK3 at a concentration of 14 μM. They were almost as potent as the parent B-2 peptide, which gives a 3.6-fold increase in the proteolytic activity of KLK3 at the same concentration.