T. Tselios et al., Treatment of experimental allergic encephalomyelitis (EAE) by a rationallydesigned cyclic analogue of myelin basic protein (MBP) epitope 72-85, BIOORG MED, 10(24), 2000, pp. 2713-2717
In this report the rational design, synthesis and pharmacological propertie
s of an amide-linked cyclic antagonist analogue of the guinea pig myelin ba
sic protein epitope MBP72-85 are described. Design of the potent cyclic ana
logue was based on 2D NOESY nuclear magnetic resonance and molecular dynami
cs studies carried out in the linear antagonist Alas(81)MBP(72-85). The cyc
lic 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. (C) 2000 Elsevier Science Ltd.
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