Apoptosis Inducing, Conformationally Constrained, Dimeric Peptide Analogs of KLA with Submicromolar Cell Penetrating Abilities

• Published in: Biomacromolecules Vol. 15; no. 10; pp. 3746 - 3752
• Main Authors: Hyun, Soonsil, Lee, Seonju, Kim, Seoyeon, Jang, Sangmok, Yu, Jaehoon, Lee, Yan
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 13.10.2014
• Subjects: Antineoplastic agents; Apoptosis - physiology; Biological and medical sciences; Cell Line, Tumor; Cell-Penetrating Peptides - metabolism; Chemistry; Chemotherapy; Dimerization; Exact sciences and technology; HeLa Cells; Humans; Medical sciences; Mitochondria - metabolism; Mitochondria - physiology; Molecular Conformation; Organic chemistry; Peptides; Peptides - metabolism; Pharmacology. Drug treatments; Preparations and properties; Antineoplastic agent; Peptides; Experimental study; Oxidative coupling; In vitro; Hela cell line; Biological activity; Mechanism; Organic disulfide; Internalization; Dimer; Helical structure; Peptide synthesis; Apoptosis

The apoptosis inducing KLA peptide, (KLAKLAK)2, possesses an ability to disrupt mitochondrial membranes. However, this peptide has a poor eukaryotic cell penetrating potential and, as a result, it requires the assistance of other cell penetrating peptides for effective translocation in micromolar co...