Preparation and preliminary characterization of poly(ethylene glycol)-pepstatin conjugate |
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| Authors: | Jeanne Brygier Jean Vlncentelli Michelle Nljs Claude Guermant Claudine Paul Danielle Baeyens-Volant Yvan Looze |
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| Affiliation: | (1) Protein Chemistry unit, Faculty of Medicine, University of Brussels, Campus Plaine, CP 206/4 Boulevard du Triomphe, B-1050 Brussels, Belgium |
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| Abstract: | The carboxyl function of pepstatin has been coupled, through an amide bond, to methoxypoly(ethylene glycol) (5 kDa), to which an amino function had been previously grafted. The mPEG-pepstatin conjugate inhibits hog pepsin (aspartic proteinase) in vitro as pepstatin itself, however, with a 400 times higher apparent Ki. The conjugate apparently does not inhibit proteinases belonging to other proteinase families such as serine (trypsin, carboxypeptidase Y), cysteine (Papaya proteinase III), or metallo (collagenase) proteinases. |
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| Keywords: | Aspartic proteinases inhibitors polyethylene glycol covalent attachment |
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