Preparation and preliminary characterization of poly(ethylene glycol)-pepstatin conjugate.
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.
Brygier
J
J
Protein Chemistry Unit, Faculty of Medicine, University of Brussels, Belgium.
Vincentelli
J
J
Nijs
M
M
Guermant
C
C
Paul
C
C
Baeyens-Volant
D
D
Looze
Y
Y
D002268:Carboxypeptidases / Q000037:antagonists & inhibitors; D003546:Cysteine Endopeptidases; D006863:Hydrogen-Ion Concentration; D061965:Matrix Metalloproteinase Inhibitors; D010434:Pepsin A / Q000037:antagonists & inhibitors; D010436:Pepstatins / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry*; D011480:Protease Inhibitors / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014361:Trypsin Inhibitors
D061965:Matrix Metalloproteinase Inhibitors; D010436:Pepstatins; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; C014195:Streptomyces pepsin inhibitor; D011092:Polyethylene Glycols; C028210:monomethoxypolyethylene glycol; D002268:Carboxypeptidases; C022633:serine carboxypeptidase; D003546:Cysteine Endopeptidases; D010434:Pepsin A; C031375:pepstatin