title: 2,4,6-trisubstituted triazines as protein a mimetics for the treatment of autoimmune diseases.
abstract: A first-in-class series of low molecular weight trisubstituted triazines were synthesized and evaluated for their ability to mimic protein A binding to human IgG antibody. The structure-activity relationship (SAR) demonstrates that the 1,3-phenylenediamine component was essential for robust activity. Twenty-two compounds, represented by lead molecule 34, displayed significant activity compared to protein A. These compounds may prove useful for the treatment of autoimmune disease.
authors.affiliation: ProMetic BioSciences Inc., 500 Boulevard Cartier Ouest, Bureau 150, Laval, Québec H7V 5B7, Canada. b.zacharie@prometic.com
authors.forename: Boulos
authors.initials: B
authors.lastname: Zacharie
authors.forename: Shaun D
authors.initials: SD
authors.lastname: Abbott
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Bienvenu
authors.forename: Alan D
authors.initials: AD
authors.lastname: Cameron
authors.forename: Josée
authors.initials: J
authors.lastname: Cloutier
authors.forename: Jean-Simon
authors.initials: JS
authors.lastname: Duceppe
authors.forename: Abdallah
authors.initials: A
authors.lastname: Ezzitouni
authors.forename: Daniel
authors.initials: D
authors.lastname: Fortin
authors.forename: Karine
authors.initials: K
authors.lastname: Houde
authors.forename: Caroline
authors.initials: C
authors.lastname: Lauzon
authors.forename: Nancie
authors.initials: N
authors.lastname: Moreau
authors.forename: Valérie
authors.initials: V
authors.lastname: Perron
authors.forename: Nicole
authors.initials: N
authors.lastname: Wilb
authors.forename: Michel
authors.initials: M
authors.lastname: Asselin
authors.forename: André
authors.initials: A
authors.lastname: Doucet
authors.forename: Marie-Eve
authors.initials: ME
authors.lastname: Fafard
authors.forename: Dannyck
authors.initials: D
authors.lastname: Gaudreau
authors.forename: Brigitte
authors.initials: B
authors.lastname: Grouix
authors.forename: François
authors.initials: F
authors.lastname: Sarra-Bournet
authors.forename: Natalie
authors.initials: N
authors.lastname: St-Amant
authors.forename: Lyne
authors.initials: L
authors.lastname: Gagnon
authors.forename: Christopher L
authors.initials: CL
authors.lastname: Penney
mesh_terms: D000818:Animals; D000974:Antibodies, Antinuclear / Q000276:immunology / Q000378:metabolism; D040761:Biomimetic Materials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D007074:Immunoglobulin G / Q000276:immunology / Q000378:metabolism; D007668:Kidney / Q000187:drug effects / Q000276:immunology; D008180:Lupus Erythematosus, Systemic / Q000188:drug therapy* / Q000276:immunology / Q000378:metabolism; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D011487:Protein Conformation; D013205:Staphylococcal Protein A / Q000276:immunology / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000974:Antibodies, Antinuclear; D007074:Immunoglobulin G; D013205:Staphylococcal Protein A; D014227:Triazines