FIBRONECTIN ADHESION INHIBITORS

摘要

Cyclic peptides of formula (1) wherein: AA1 is an L or D amino acid selected form Ile and Leu or amino acid analogue thereof; AA2 is an L amino acid selected from Leu or amino acid analogue thereof; AA3 is an L amino acid selected from Asp or amino acid analogue thereof containing a carboxyl group in its side chain; AA4 is an L amino acid selected from Val or amino acid analogue thereof and; LINKER represents a linking moiety for linking N terminus of AA1 to C terminus of AA4 to form a cyclic peptide containing a heterocyclic ring having 17 to 30 members. The cyclic peptides inhibit the interaction of vascular cell adhesion molecule-1 and fibronectin with integrin very late antigen 4 and have therapeutic applications such as in rheumatoid arthritis or multiple sclerosis.