Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2 non-competitive allosteric inhibitor.

@article{Bertini2012ReceptorBM,
  title={Receptor binding mode and pharmacological characterization of a potent and selective dual CXCR1/CXCR2 non-competitive allosteric inhibitor.},
  author={Riccardo Bertini and Luc{\'i}ola da Silva Barcelos and Andrea R. Beccari and Barbara Cavalieri and Alessio Moriconi and Cinzia Bizzarri and Paola Di Benedetto and Claudia Di Giacinto and Isabelle Gloaguen and Emanuela Galliera and Massimiliano Marco Corsi and Rosal{\'i}a Cordo Russo and S{\'i}lvia Passos Andrade and Maria Candida Cesta and Giuseppe Nano and Andrea Aramini and Juan Carlos Cutrin and Massimo Locati and Marcello Allegretti and Mauro M Teixeira},
  journal={British journal of pharmacology},
  year={2012},
  volume={165 2},
  pages={436-54}
}
BACKGROUND AND PURPOSE DF 2156A is a new dual inhibitor of IL-8 receptors CXCR1 and CXCR2 with an optimal pharmacokinetic profile. We characterized its binding mode, molecular mechanism of action and selectivity, and evaluated its therapeutic potential. EXPERIMENTAL APPROACH The binding mode, molecular mechanism of action and selectivity were investigated using chemotaxis of L1.2 transfectants and human leucocytes, in addition to radioligand and [(35) S]-GTPγS binding approaches. The… CONTINUE READING