FUT-175 as a potent inhibitor of C5/C3 convertase activity for production of C5a and C3a.
We examined the inhibitory effect of FUT-175 on the C3/C5 convertase activity of the cobra venom factor-derived enzyme CVF,Bb by measuring C5b6-mediated reactive lysis of unsensitized guinea pig erythrocytes and by measuring directly the released fragments C3-des-Arg and C5a-des-Arg. In this study, we showed that the concentration of 4.5 X 10(-6) M of FUT-175 caused 50% inhibition of C5 convertase activity of CVF,Bb in reactive hemolysis assays, and that 4.0 X 10(-6) M FUT-175 caused 50% inhibition of the production of C3a and C5a generated by the C3/C5 convertase activity of CVF,Bb.
Inagi
R
R
Department of Immunology, Nagoya University School of Medicine, Japan.
Miyata
T
T
Maeda
K
K
Sugiyama
S
S
Miyama
A
A
Nakashima
I
I
D000818:Animals; D001550:Benzamidines; D050577:Complement C3-C5 Convertases / Q000037:antagonists & inhibitors*; D015926:Complement C3a / Q000096:biosynthesis* / Q000378:metabolism; D015936:Complement C5a / Q000096:biosynthesis*; D015937:Complement C5a, des-Arginine / Q000378:metabolism; D004546:Elapid Venoms / Q000378:metabolism; D004912:Erythrocytes / Q000378:metabolism; D006146:Guanidines / Q000494:pharmacology*; D006168:Guinea Pigs; D006801:Humans
D001550:Benzamidines; D015937:Complement C5a, des-Arginine; D004546:Elapid Venoms; D006146:Guanidines; C016310:cobra venom factor; C044541:complement C3a, des-Arg-(77)-; D015926:Complement C3a; D015936:Complement C5a; D050577:Complement C3-C5 Convertases; C032855:nafamostat