Mesoporous Silica Nanocarriers with Cyclic Peptide Gatekeeper: Specific Targeting of Aminopeptidase N and Triggered Drug Release by Stimuli‐Responsive Conformational Transformation. Issue 67 (15th November 2017)

• Record Type: Journal Article
• Authors: Lee, Jeonghun; Oh, Eun‐Taex; Han, Yeji; Kim, Ha Gyeong; Park, Heon Joo; Kim, Chulhee
• Is Part Of: Chemistry. Volume 23:Issue 67(2017)
• Page Start: 16966
• Page End: 16971
• Publication Date: 2017-11-15
• Subjects: conformational transformation -- mesoporous silica -- nanomaterials -- peptides -- stimuli responses; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.201704309
• Languages: English
• ISSNs: 0947-6539

Abstract

Abstract: 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). Abstract : Watch out for the gatekeeper : A NGR‐containing dual‐functional cyclic peptide gatekeeper on the surface of mesoporous nanocarrier is prepared not only for active targeting of the aminopeptidase N expressed on cancer cells but also stimuli‐responsive intracellular drug release triggered by a glutathione‐induced conformational transformation of the peptide gatekeeper.