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Acidic pH‐Responsive siRNA Conjugate for Reversible Carrier Stability and Accelerated Endosomal Escape with Reduced IFNα‐Associated Immune Response
Author(s) -
Takemoto Hiroyasu,
Miyata Kanjiro,
Hattori Shota,
Ishii Takehiko,
Suma Tomoya,
Uchida Satoshi,
Nishiyama Nobuhiro,
Kataoka Kazunori
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201300178
Subject(s) - endosome , conjugate , gene silencing , cytosol , chemistry , microbiology and biotechnology , combinatorial chemistry , computer science , biophysics , biochemistry , cell , gene , biology , mathematics , enzyme , mathematical analysis
An siRNA conjugate is based on an acid‐labile maleic acid amide linkage for programmed transfer of siRNA from the endosome to the cytosol and siRNA release in the cell interior. The procedure relies on reversible stability in response to endosomal acidic pH value. The complexed polyionic conjugate achieved gene silencing in cultured cancerous cells with negligible side effects.