The sterical requirements for the activity of Mycobacteria phagocytosis inhibitors,demonstrated by guanidino acids as the mimetics of antiadhesive peptides

摘要

The phagocytosis of Mycobacteria determines the formation of a complex between the bacterial Ag85 antigen and the serum protein-fibronectin.Only in this form this bacteria can interact with the integrin receptor and penetrate host cells.So,a new approach to the therapy of Mycobacteria induced diseases may consist in the inhibition of Mycobacteria phagocytosis,mediated by fibronectin.Our investigations on the Mycobacterium kansasii phagocytosis inhibition shows that a crucial role in this process is played by the guanidine group of the Arg residue and the carboxylic group of the Asp residue in the inhibitor molecule.These groups must be situated at the distance about 9.2 A.This evidence was used by us as the criterium in the construction of Mycobacteria phagocytosis inhibitors.