The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in rats as a measure of emetogenicity.

Autor: Davis TG; Respiratory Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, Pennsylvania 19406, USA., Peterson JJ, Kou JP, Capper-Spudich EA, Ball D, Nials AT, Wiseman J, Solanke YE, Lucas FS, Williamson RA, Ferrari L, Wren P, Knowles RG, Barnette MS, Podolin PL

Publikováno v: The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 2009 Sep; Vol. 330 (3), pp. 922-31. Date of Electronic Publication: 2009 Jun 04.

Inhibition of invariant chain processing, antigen-induced proliferative responses, and the development of collagen-induced arthritis and experimental autoimmune encephalomyelitis by a small molecule cysteine protease inhibitor.

Autor: Podolin PL; Respiratory and Inflammation Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA 19406, USA. patty_podolin@gsk.com, Bolognese BJ, Carpenter DC, Davis TG, Johanson RA, Fox JH, Long E 3rd, Dong X, Marquis RW, Locastro SM, Terfloth GJ, Kurali E, Peterson JJ, Smith BR, McQueney MS, Yamashita DS, Capper-Spudich EA

Publikováno v: Journal of immunology (Baltimore, Md. : 1950) [J Immunol] 2008 Jun 15; Vol. 180 (12), pp. 7989-8003.