TY  - JOUR
PY  - 1996//
TI  - [Synthetic inhibitors targeting serine and aspartic acid proteases]
JO  - Journal de Pharmacie de Belgique
A1  - Reboud-Ravaux, M. C.
A1  - Boggetto, N. D.
A1  - Doucet, C. E.
A1  - de Rosny, E. H.
A1  - Vergely, I. B.
A1  - Thierry, N. M.
A1  - Amour, A. J.
SP  - 161
EP  - 164
VL  - 51
IS  - 3
N2  - The interaction of novel series of synthetic inhibitors with various serine proteases (leukocyte elastase, thrombin, cathepsin G, chymotrypsin, plasminogen activators and plasmin) and an aspartic protease (HIV-1 protease) were studied. Various aspects were analyzed: mechanism of action, structure-activity relationships, and in some cases, molecular modelling and biological evaluation. Functionalized cyclopeptides and N-aryl azetidin-2-ones behaved as suicide substrates acting specifically on trypsin-like proteases (thrombin or urokinase) and elastases, respectively. Novel hydrazinopeptides acted as reversible inhibitors of elastases. Coumarin derivatives inactivated very efficiently chymotrypsin-like proteases (k(inact)/K(I) = 760,000 M(-1).s(-1)). Inhibitors of HIV-1 protease acting either as inactivators or dimerization inhibitors are under investigation. The inhibitors described above are useful for elucidating the biological roles of the target enzymes and constitute potential drugs.<p /> <p>Language: fr</p>
LA  - fr
SN  - 0047-2166
UR  - http://dx.doi.org/
ID  - ref1
ER  -