Abstract
The association of ICAM-1 with LFA-1 plays a critical role in several autoimmune diseases. N-2-Bromobenzoyl L-tryptophan, compound 1, was identified as an inhibitor to the formation of the LFA-1/ICAM complex. The SAR of the amino acid indicates that the carboxylic acid is required for inhibition and that L-histidine is the most favored amino acid.
MeSH terms
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Amino Acids / chemical synthesis
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Amino Acids / chemistry
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Amino Acids / pharmacology*
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Carboxylic Acids / chemistry
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Carboxylic Acids / pharmacology
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Enzyme-Linked Immunosorbent Assay
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Histidine / chemistry
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Histidine / pharmacology
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Indicators and Reagents
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Intercellular Adhesion Molecule-1 / drug effects*
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Lymphocyte Function-Associated Antigen-1 / drug effects*
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Structure-Activity Relationship
Substances
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Amino Acids
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Carboxylic Acids
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Indicators and Reagents
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Lymphocyte Function-Associated Antigen-1
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Intercellular Adhesion Molecule-1
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Histidine