title: Inhibition of rat tissue kallikrein gene family members by rat kallikrein-binding protein and alpha 1-proteinase inhibitor.
abstract: 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.
authors.affiliation: Laboratoire d'Enzymologie et Chimie des Protéines, URA CNRS1334, Université François Rabelais, Tours, France.
authors.forename: C
authors.initials: C
authors.lastname: Serveau
authors.forename: T
authors.initials: T
authors.lastname: Moreau
authors.forename: G X
authors.initials: GX
authors.lastname: Zhou
authors.forename: A
authors.initials: A
authors.lastname: ElMoujahed
authors.forename: J
authors.initials: J
authors.lastname: Chao
authors.forename: F
authors.initials: F
authors.lastname: Gauthier
mesh_terms: 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*
chemical_list: D037263:Asialoglycoprotein Receptor; D011971:Receptors, Immunologic; D000515:alpha 1-Antitrypsin; D007610:Kallikreins