We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the. ne role of the propionic/acetic chain in the modulation of CXCL8 receptors. (C) 2009 Elsevier Ltd. All rights reserved.
Structure–Activity Relationship of novel phenylacetic CXCR1 inhibitors
ASCHI, MASSIMILIANO;CRUCIANELLI, MARCELLO;
2009-01-01
Abstract
We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the. ne role of the propionic/acetic chain in the modulation of CXCL8 receptors. (C) 2009 Elsevier Ltd. All rights reserved.File in questo prodotto:
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