Constructing bioactive peptides with pH-dependent activities.

Autor: Tu Z; Department of Chemistry, Chemical Biology, and Biomedical Engineering, Stevens Institute of Technology, Hoboken, NJ 07030, USA., Volk M, Shah K, Clerkin K, Liang JF
Jazyk: angličtina
Zdroj: Peptides [Peptides] 2009 Aug; Vol. 30 (8), pp. 1523-8. Date of Electronic Publication: 2009 May 21.
DOI: 10.1016/j.peptides.2009.05.009
Abstrakt: Many bioactive peptides are featured by their arginine and lysine rich contents. In this study, lysine and arginine residues in lytic peptides were selectively replaced by histidines. Although resulting histidine-containing lytic peptides had decreased activity, they did show pH-dependent cytotoxicity. The activity of the constructed histidine-containing lytic peptides increased 2-8 times as the solution pH changed from 7.4 to 5.5. More importantly, these histidine-containing peptides maintain the same cell killing mechanism as their parent peptides by causing cell lysis. Both the activity and pH-sensitivity of histidine-containing peptides are tunable by adjusting histidine substitution numbers and positions. This study has presented a general strategy to create bioactive peptides with desired pH-sensitivity to meet the needs of various applications such as cancer treatments.
Databáze: MEDLINE