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.
MeSH terms
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Animals
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Antibodies, Antinuclear / immunology
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Antibodies, Antinuclear / metabolism
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Biomimetic Materials / chemical synthesis*
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Biomimetic Materials / chemistry
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Biomimetic Materials / pharmacology*
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Enzyme-Linked Immunosorbent Assay
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Humans
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Immunoglobulin G / immunology
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Immunoglobulin G / metabolism
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Kidney / drug effects
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Kidney / immunology
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Lupus Erythematosus, Systemic / drug therapy*
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Lupus Erythematosus, Systemic / immunology
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Lupus Erythematosus, Systemic / metabolism
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Mice
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Models, Molecular
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Molecular Structure
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Protein Conformation
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Staphylococcal Protein A / immunology
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Staphylococcal Protein A / metabolism*
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Structure-Activity Relationship
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Triazines / chemical synthesis*
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Triazines / chemistry
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Triazines / pharmacology*
Substances
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Antibodies, Antinuclear
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Immunoglobulin G
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Staphylococcal Protein A
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Triazines