Inhibition of rat tissue kallikrein gene family members by rat kallikrein-binding protein and alpha 1-proteinase inhibitor.
The regulation of tissue kallikrein activity by plasma serine proteinase inhibitors (serpins) was investigated by measuring the association rate constants of six tissue-kallikrein family members isolated from the rat submandibular gland, with rat kallikrein-binding protein (rKBP) and alpha 1-proteinase inhibitor (alpha 1-PI). Both these serpins inhibited kallikreins rK2, rK7, rK8, rK9 and rK10 with association rate constants in the 10(3)-10(4) M-1.s-1 range, whereas only 'true' tissue kallikrein rK1 was not susceptible to alpha 1-PI. This results in slow inhibition of rK1 by plasma serpins, which could explain why this kallikrein is the only member of the gene family identified so far that induces a transient decrease in blood pressure when injected in minute amounts into the circulation.
Serveau
C
C
Laboratoire d'Enzymologie et Chimie des Protéines, URA CNRS1334, Université François Rabelais, Tours, France.
Moreau
T
T
Zhou
G X
GX
ElMoujahed
A
A
Chao
J
J
Gauthier
F
F
D000818:Animals; D037263:Asialoglycoprotein Receptor; D007610:Kallikreins / Q000037:antagonists & inhibitors / Q000235:genetics*; D005810:Multigene Family; D051381:Rats; D011971:Receptors, Immunologic / Q000378:metabolism*; D000515:alpha 1-Antitrypsin / Q000494:pharmacology*
D037263:Asialoglycoprotein Receptor; D011971:Receptors, Immunologic; D000515:alpha 1-Antitrypsin; D007610:Kallikreins