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EnglishWe 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.
http://hdl.handle.net/11697/3632| Titolo: | Structure–Activity Relationship of novel phenylacetic CXCR1 inhibitors |
| Autori interni: | ASCHI, MASSIMILIANO CRUCIANELLI, MARCELLO |
| Data di pubblicazione: | 2009 |
| Rivista: | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
| 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. |
| Handle: | http://hdl.handle.net/11697/3632 |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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