pH-controllable cell-penetrating polypeptide that exhibits cancer targeting

Acta Biomaterialia
DaeYong LeeYeu-Chun Kim

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. We developed pH-controllable cell-penetrating polypeptides (PCCPs) undergoing pH-induced conformational transitions. Unlike natural cell-penetrating peptides, PCCPs was capable of ...Continue Reading

Citations

Jul 18, 2018·Beilstein Journal of Organic Chemistry·Marcelo D T TorresVani X Oliveira
Nov 16, 2018·Frontiers in Pharmacology·Clara FernandesMayur C Yergeri
Apr 10, 2019·Polymers·DaeYong LeeYeu-Chun Kim
Aug 31, 2021·RSC Chemical Biology·Heleen de JongDennis W P M Löwik

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