Interaction of KLAKLAK-NH and Analogs with Biomimetic Membrane Models.

Background: Specifically designed peptide mimetics offer higher selectivity regarding their toxicity to mammalian cells. In addition to the α-helix conformation, the specific activity is related to the peptide's ability to penetrate the cell membrane. The alterations in lipid membrane properties were addressed in the presence of the peptide KLAKLAK-NH and analogs containing β-alanine, strengthening the antibacterial activity and/or naphtalimide with proven anticancer properties.

Synthesis and Biological Studies on (KLAKLAK)-NH Analog Containing Unnatural Amino Acid β-Ala and Conjugates with Second Pharmacophore.

(1) Background: Peptides are good candidates for anticancer drugs due to their natural existence in the body and lack of secondary effects. (KLAKLAK) is an antimicrobial peptide that also shows good anticancer properties. (2) Methods: The Solid Phase Peptide Synthesis (Fmoc-strategy) was used for the synthesis of target molecules, analogs of (KLAKLAK)-NH.

Synthesis, Antitumor and Antibacterial Studies of New Shortened Analogues of (KLAKLAK)-NH and Their Conjugates Containing Unnatural Amino Acids.

(1) Background: (KLAKLAK) is a representative of the antimicrobial peptide group which also shows good anticancer properties. (2) Methods: Herein, we report synthesis using SPPS and characterization by HPLC/MS of a series of shortened analogues of (KLAKLAK). They contain single sequence KLAKLAK as C-terminal amides.