Treatment of experimental allergic encephalomyelitis (EAE) by a rationallydesigned cyclic analogue of myelin basic protein (MBP) epitope 72-85

Citation
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
Citations number
27
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
24
Year of publication
2000
Pages
2713 - 2717
Database
ISI
SICI code
0960-894X(200012)10:24<2713:TOEAE(>2.0.ZU;2-A
Abstract
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. All rights reserved.