Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2

…, E Galliera, P Di Benedetto, P Vigilante…

Index: 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 Journal of Medicinal Chemistry, 2007 ,  vol. 50,  # 17  p. 3984 - 4002

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Citation Number: 58

Abstract

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 candidate, is ...