Title
pH-controllable cell-penetrating polypeptide possessing cancer targeting
Author
DaeYong Lee, IlKoo Noh, Jisang Yoo, N.Sanoj Rejinold, Yeu-Chun Kim
Year
2017
Journal
Acta Biomaterialia
Abstract
Helical peptides were naturally-occurring ordered conformations that mediated various biological functions essential for biotechnology. However, it was difficult for natural helical polypeptides to be applied in biomedical fields due to low bioavailability. To avoid these problems, synthetic alpha-helical polypeptides have recently been introduced by further modifying pendants in the side chain. In spite of an attractive biomimetic helical motif, these systems could not be tailored for targeted delivery mainly due to nonspecific binding events. To address these issues, we created a conformation-transformable polypeptide capable of eliciting a pH-activated cell-penetrating property solely at the cancer region. The developed novel polypeptide showed that the bare helical conformation had a function at physiological conditions while the pH-induced helical motif provided an active cell-penetrating characteristic at a tumor extracellular matrix pH. The unusual conformation-transformable system can elicit bioactive properties exclusively at mild acidic pH.
Instrument
J-815
Keywords
Circular dichroism, Secondary structure, Chemical stability, Biochemistry