Antimicrobial Agents and Chemotherapy · 1999 · 114 citations · 4 references
PharmacyMedicinal ChemistryAntimicrobial PharmacologyDrug DesignDrug DiscoveryAmino Acid ChemistryAntibacterial AgentsAntimicrobial PeptidesPeptide ChemistryPeptide Drug DiscoveryPeptidomimetic DesignAntibacterial PeptidesAntimicrobial Peptide ActivityAntimicrobial Spectrum NarrowingCationic Antimicrobial PeptidesCyclic Peptide DesignCyclic PeptidesPeptide Medicinal ChemistryPeptide Structure-activity Relationships
Both linear and cyclic derivatives of the cyclic 12-amino-acid antimicrobial peptide bactenecin were designed based on optimization of amphipathicity and charge location. In general, increasing the number of positive charges at the N and C termini and adding an extra tryptophan residue in the loop not only increased the activities against both gram-positive and gram-negative bacteria but also broadened the antimicrobial spectrum.
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