Journal article
A drug delivery strategy: Binding enkephalin to asialoglycoprotein receptor by enzymatic galactosylation
MP Christie, P Simerská, FEC Jen, WM Hussein, MFM Rawi, LE Hartley-Tassell, CJ Day, MP Jennings, I Toth
Plos One | PUBLIC LIBRARY SCIENCE | Published : 2014
Abstract
Glycosylation of biopharmaceuticals can mediate cell specific delivery by targeting carbohydrate receptors. Additionally, glycosylation can improve the physico-chemical (drug-like) properties of peptide based drug candidates. The main purpose of this study was to examine if glycosylation of the peptide enkephalin could facilitate its binding to the carbohydrate receptor, asialoglycoprotein. Firstly, we described the one-pot enzymatic galactosylation of lactose modified enkephalin in the presence of uridine-5′- diphosphogalactose 4-epimerase and lipopolysaccharyl α-1,4- galactosyltransferase. Stability experiments using human plasma and Caco-2 cell homogenates showed that glycosylation consid..
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Awarded by Australian Research Council
Funding Acknowledgements
This work was supported by an Australian Research Council Discovery Project Grant (DP1092829). P. S. was supported by an Australian Postdoctoral Fellowship (DP1092829), M.P.J. was supported by a (NHMRC program grant 565526 and DP103130141) and I. T. was supported by a Professorial Research Fellowship (DP110100212), http://www.arc.gov.au, http://www.nhmrc.gov.au. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.