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

  title={Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2.},
  author={Alessio Moriconi and Maria Candida Cesta and Maria Neve Cervellera and Andrea Aramini and Silvia Coniglio and Sandro Colagioia and Andrea R. Beccari and Cinzia Bizzarri and Michela Rita Cavicchia and Massimo Locati and Emanuela Galliera and Paola Di Benedetto and Paolo Vigilante and Riccardo Bertini and Marcello Allegretti},
  journal={Journal of medicinal chemistry},
  volume={50 17},
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 currently under clinical investigation in the prevention of ischemia… CONTINUE READING