Constructing bioactive peptides with pH-dependent activities

Zhigang Tu, Melanie Volk, Khushali Shah, Kevin Clerkin, Jun F. Liang

Research output: Contribution to journalArticlepeer-review

41 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)1523-1528
Number of pages6
JournalPeptides
Volume30
Issue number8
DOIs
StatePublished - Aug 2009

Keywords

  • Bioactive
  • Cell lysis
  • Histidine
  • Peptide
  • pH sensitivity

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