Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity

  title={Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity},
  author={R. J. Hill and K. Dabbagh and D. Phippard and Ching Li and Rebecca T. Suttmann and Mary Welch and E. Papp and K. W. Song and Kung-ching Chang and D. Leaffer and Y. Kim and R. T. Roberts and T. Zabka and D. Aud and J. Porto and A. Manning and S. Peng and D. Goldstein and B. Wong},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={610 - 619}
  • R. J. Hill, K. Dabbagh, +16 authors B. Wong
  • Published 2008
  • Medicine
  • Journal of Pharmacology and Experimental Therapeutics
  • P38α is a protein kinase that regulates the expression of inflammatory cytokines, suggesting a role in the pathogenesis of diseases such as rheumatoid arthritis (RA) or systemic lupus erythematosus. Here, we describe the preclinical pharmacology of pamapimod, a novel p38 mitogen-activated protein kinase inhibitor. Pamapimod inhibited p38α and p38β enzymatic activity, with IC50 values of 0.014 ± 0.002 and 0.48 ± 0.04 μM, respectively. There was no activity against p38δ or p38γ isoforms. When… CONTINUE READING
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