FUT-175 as a potent inhibitor of C5/C3 convertase activity for production of C5a and C3a

Immunol Lett. 1991 Jan;27(1):49-52. doi: 10.1016/0165-2478(91)90243-4.

Abstract

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.

MeSH terms

  • Animals
  • Benzamidines
  • Complement C3-C5 Convertases / antagonists & inhibitors*
  • Complement C3a / biosynthesis*
  • Complement C3a / metabolism
  • Complement C5a / biosynthesis*
  • Complement C5a, des-Arginine / metabolism
  • Elapid Venoms / metabolism
  • Erythrocytes / metabolism
  • Guanidines / pharmacology*
  • Guinea Pigs
  • Humans

Substances

  • Benzamidines
  • Complement C5a, des-Arginine
  • Elapid Venoms
  • Guanidines
  • cobra venom factor
  • complement C3a, des-Arg-(77)-
  • Complement C3a
  • Complement C5a
  • Complement C3-C5 Convertases
  • nafamostat