PREPARATION AND PRELIMINARY CHARACTERIZATION OF POLY(ETHYLENE GLYCOL)-PEPSTATIN CONJUGATE

Authors
BRYGIER J VINCENTELLI J NIJS M GUERMANT C PAUL C BAEYENSVOLANT D LOOZE Y
Citation
J. Brygier et al., PREPARATION AND PRELIMINARY CHARACTERIZATION OF POLY(ETHYLENE GLYCOL)-PEPSTATIN CONJUGATE, Applied biochemistry and biotechnology, 47(1), 1994, pp. 1-10
Citations number
35
Categorie Soggetti
Biothechnology & Applied Migrobiology",Biology
Journal title
Applied biochemistry and biotechnology → ACNP
ISSN journal
02732289
Volume
47
Issue
1
Year of publication
1994
Pages
1 - 10
Database
ISI
SICI code
0273-2289(1994)47:1<1:PAPCOP>2.0.ZU;2-D
Abstract
The carboxyl function of pepstatin has been coupled, through an amide bond, to methoxypoly(ethylene glycol) (5 kDa), to which an amino funct ion had been previously grafted. The mPEG-pepstatin conjugate inhibits hog pepsin (aspartic proteinase) in vitro as pepstatin itself, howeve r, with a 400 times higher apparent K-i. The conjugate apparently does not inhibit proteinases belonging to other proteinase families such a s serine (trypsin, carboxypeptidase Y), cysteine (Papaya proteinase II I), or metallo (collagenase) proteinases.