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Mesoporous Silica Nanocarriers with Cyclic Peptide Gatekeeper: Specific Targeting of Aminopeptidase N and Triggered Drug Release by Stimuli‐Responsive Conformational Transformation
Author(s) -
Lee Jeonghun,
Oh EunTaex,
Han Yeji,
Kim Ha Gyeong,
Park Heon Joo,
Kim Chulhee
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201704309
Subject(s) - nanocarriers , mesoporous silica , intracellular , peptide , glutathione , endocytosis , biophysics , chemistry , cancer cell , cyclic peptide , a549 cell , drug delivery , microbiology and biotechnology , biochemistry , mesoporous material , apoptosis , cancer , enzyme , cell , biology , medicine , organic chemistry , catalysis
Utilizing stimuli‐responsive conformational transformation of a cyclic peptide as a gatekeeper for mesoporous nanocarriers has several advantages such as facile introduction of targeting capabilities, low enzymatic degradation during blood circulation and enhanced specific binding to selected cells. In this report, a Asn‐Gly‐Arg (NGR)‐containing dual‐functional cyclic peptide gatekeeper on the surface of mesoporous nanocarrier is prepared not only for active targeting of the aminopeptidase N (APN) expressed on cancer cells but also stimuli‐responsive intracellular drug release triggered by a glutathione (GSH)‐induced conformational transformation of the peptide gatekeeper. The peptide gatekeeper on the surface of nanocarriers exhibits on–off gatekeeping by conformational transformation triggered by intracellular glutathione of the cancer cells. H1299 cells (high APN expression) showed greater uptake of the nanocarrier by endocytosis and higher apoptosis than A549 cells (low APN expression).