223753-68-2Relevant academic research and scientific papers
Synthesis of some pseudo-peptide analogs of thiol proteinase inhibitors
Iguchi, Shin,Kawasaki, Koichi,Okamoto, Hiroshi,Umezawa, Chisae,Okada, Yoshio
, p. 423 - 427 (2007/10/03)
Some pseudo-peptide analogs of thiol proteinase inhibitors were synthesized by a conventional solution method. Among them, Suc-Ala-Val-Val- Ala-Ψ-(CH2-NH)-Ala-pNA (peptide 1) and Suc-Ala-Val-Val-Ψ-(CH2NH)-Ala- Ala-pNA (peptide 2) showed a stronger inhibitory activity compared with parent peptide such as Suc-Ala-Val-Val-Ala-Ala-pNA. In particular, peptide 2 was about 10-fold as active as the parent peptide (IC50=8 μM). Inserting Ψ-(CH2-NH) possibly makes the inhibitor less susceptible to papain and, as a result, pro-duces more potent inhibition.
