title: Treatment of experimental allergic encephalomyelitis (EAE) by a rationally designed cyclic analogue of myelin basic protein (MBP) epitope 72-85.
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 MBP(72-85) 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 Ala81MBP(72-85). The cyclic antagonist completely prevented the induction of experimental allergic/autoimmune encephalomyelitis when coinjected with linear and cyclic agonist analogues MBP(72-85) and cyclo(2-9)MBP(72-85).
authors.affiliation: Department of Chemistry, University of Patras, Greece.
authors.forename: T
authors.initials: T
authors.lastname: Tselios
authors.forename: I
authors.initials: I
authors.lastname: Daliani
authors.forename: S
authors.initials: S
authors.lastname: Deraos
authors.forename: S
authors.initials: S
authors.lastname: Thymianou
authors.forename: E
authors.initials: E
authors.lastname: Matsoukas
authors.forename: A
authors.initials: A
authors.lastname: Troganis
authors.forename: I
authors.initials: I
authors.lastname: Gerothanassis
authors.forename: A
authors.initials: A
authors.lastname: Mouzaki
authors.forename: T
authors.initials: T
authors.lastname: Mavromoustakos
authors.forename: L
authors.initials: L
authors.lastname: Probert
authors.forename: J
authors.initials: J
authors.lastname: Matsoukas
mesh_terms: D000818:Animals; D015195:Drug Design; D004681:Encephalomyelitis, Autoimmune, Experimental / Q000188:drug therapy* / Q000473:pathology / Q000517:prevention & control; D000939:Epitopes / Q000008:administration & dosage / Q000494:pharmacology; D006168:Guinea Pigs; D007114:Immunization; D008958:Models, Molecular; D004676:Myelin Basic Protein / Q000138:chemical synthesis / Q000276:immunology / Q000494:pharmacology*; D019906:Nuclear Magnetic Resonance, Biomolecular; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000276:immunology / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000276:immunology / Q000494:pharmacology; D051381:Rats; D011917:Rats, Inbred Lew; D013116:Spinal Cord / Q000187:drug effects / Q000473:pathology
chemical_list: D000939:Epitopes; D004676:Myelin Basic Protein; D010446:Peptide Fragments; D010456:Peptides, Cyclic; C118872:myelin basic protein 72-85