TY  - JOUR
PY  - 1991//
TI  - A cyclopeptidic suicide substrate preferentially inactivates urokinase-type plasminogen activator
JO  - Biochemical and biophysical research communications
A1  - Reboud-Ravaux, M.
A1  - Vilain, A. C.
A1  - Boggetto, N.
A1  - Maillard, J.
A1  - Favreau, C.
A1  - Xie, J.
A1  - Mazaleyrat, J. P.
A1  - Wakselman, M.
SP  - 352
EP  - 359
VL  - 178
IS  - 1
N2  - c[Arg-aB-(CH2+SCH3 phi)-Gly4] was designed and studied as a mechanism-based inactivator (suicide substrate) for plasminogen activators (u-PA and t-PA) and plasmin. This compound inhibited u-PA and fulfills criteria expected for the involvement of an enzyme-activated inhibitor: first-order and irreversible process, saturation kinetics, protection by substrate. The limiting first-order rate constant kinact and the apparent enzyme-inhibitor dissociation constant KI were 0.021 s-1 and 9 microM, respectively at pH 7.5 and 25 degrees C. The activation of plasminogen by u-PA is compromised after this enzyme has been treated by the reagent. Plasmin and t-PA were inactivated 40- and 2330-fold less efficiently than u-PA, respectively.<p /> <p>Language: en</p>
LA  - en
SN  - 0006-291X
UR  - http://dx.doi.org/10.1016/0006-291x(91)91821-s
ID  - ref1
ER  -