Author/Authors :
Theodore Tselios، نويسنده , , Ioanna Daliani، نويسنده , , Spyros Deraos، نويسنده , , Soteria Thymianou، نويسنده , , Elisabeth Matsoukas، نويسنده , , Anastasios Troganis، نويسنده , , Ioannis Gerothanassis، نويسنده , , Athanasia Mouzaki، نويسنده , , Thomas Mavromoustakos، نويسنده , , Lesley Probert، نويسنده , , John Matsoukas، نويسنده ,
Abstract :
In this report the rational design, synthesis and pharmacological properties of an amide-linked cyclic antagonist analogue of the guinea pig myelin basic protein epitope MBP72–85 are described. Design of the potent cyclic analogue was based on 2D NOESY nuclear magnetic resonance and molecular dynamics studies carried out in the linear antagonist Ala81MBP72–85. The cyclic antagonist completely prevented the induction of experimental allergic/autoimmune encephalomyelitis when coinjected with linear and cyclic agonist analogues MBP72–85 and cyclo(2–9)MBP72–85.
