Drug intelligence / Profile preview

D(KLAKLAK)2

Development stage
Preclinical
Modality
Peptides
Administration
Intratumoral
01

Overview

D(KLAKLAK)2 is a synthetic, all-D-amino-acid cationic amphipathic helical peptide derived from the antibacterial motif (KLAKLAK)2 and designed as a mitochondria-disrupting proapoptotic agent with both antimicrobial and antitumor activity.[1][3][5][6][9][10] Because the D-enantiomer resists proteolytic degradation, it is more stable in biological systems and can selectively kill bacteria by damaging their negatively charged membranes and, when efficiently internalized into mammalian cells via conjugation to targeting ligands or delivery systems, disrupts mitochondrial membranes to induce apoptosis or necrotic-like cell death in tumor cells.[3][4][5][6][9][10] It is widely used as a modular cytotoxic payload in experimental conjugates (e.g., RGD-, TMTP1-, CNGRC- or antibody-linked constructs and cationic liposomal formulations) to enhance targeted antitumor efficacy while maintaining low systemic toxicity, but remains a research peptide rather than an approved therapeutic.[5][6][8][9]

Other names
d-(KLAKLAK)2proapoptotic peptide D(KLAKLAK)2antimicrobial peptide D(KLAKLAK)2
02

Targets

Cardiolipin

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