N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: amino acid structure-activity relationship |
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| Authors: | Burdick Daniel J Paris Ken Weese Kenneth Stanley Mark Beresini Maureen Clark Kevin McDowell Robert S Marsters James C Gadek Thomas R |
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| Institution: | Department of Bioorganic Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA. burdick.dan@gene.com |
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| 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. |
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