Article
Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2.
Journal of medicinal chemistry - 23 Aug 2007
Moriconi Alessio, Cesta Maria Candida, Cervellera Maria Neve, Aramini Andrea, Coniglio Silvia, Colagioia Sandro, Beccari Andrea Rosario, Bizzarri Cinzia, Cavicchia Michela Rita, Locati Massimo, Galliera Emanuela, Di Benedetto Paola, Vigilante Paolo, Bertini Riccardo, Allegretti Marcello
Abstract excerpt
Chemokines CXCL8 and CXCL1 play a key role in the recruitment of neutrophils at the site of inflammation. CXCL8 binds two membrane receptors, CXCR1 and CXCR2, whereas CXCL1 is a selective agonist for CXCR2. In the past decade, the physiopathological role of CXCL8 and CXCL1 has been investigated. A novel class of small molecular weight allosteric CXCR1 inhibitors was identified, and reparixin, the first drug...
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