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Biological activities of retro and diastereo analogs of a 13-residue peptide with antimicrobial and hemolytic activities: Authors' affiliations:.
- Source :
-
Journal of Peptide Research . Jan2001, Vol. 57 Issue 1, p59-67. 9p. 2 Charts, 6 Graphs. - Publication Year :
- 2001
-
Abstract
- Abstract: The biological activities of synthetic retro and diastereo analogs of PKLLKTFLSKWIG (SPFK), a 13-residue peptide with antimicrobial and hemolytic activities, have been investigated. Retro peptides with C-terminal acid and amide exhibited antibacterial activities comparable with those of SPFK. Their hemolytic activities were, however, only marginally lower. The diastereo analog with C-terminal acid was not antibacterial and was weakly hemolytic. Amidation of this analog could restore antibacterial activity. Both retro analogs were unordered in aqueous medium but had a propensity for a helical structure in trifluoroethanol. However, diastereo analogs were unordered in both aqueous medium and trifluoroethanol. Thus, reversing the sequence in a short amphiphilic peptide may not always result in the selective loss of biological activity such as hemolytic activity. Also, introduction of enantiomeric amino acids in a short peptide to generate a diastereomer may result in loss of structure as well as antimicrobial and hemolytic activities, unless compensated by an increase in positive charges. [ABSTRACT FROM AUTHOR]
- Subjects :
- *PEPTIDES
*HEMOLYSIS & hemolysins
Subjects
Details
- Language :
- English
- ISSN :
- 1397002X
- Volume :
- 57
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Journal of Peptide Research
- Publication Type :
- Academic Journal
- Accession number :
- 5787812
- Full Text :
- https://doi.org/10.1034/j.1399-3011.2001.00800.x