Author/Authors :
John I. Trujillo، نويسنده , , Marvin J. Meyers، نويسنده , , David R. Anderson، نويسنده , , Shridhar Hegde، نويسنده , , Matthew W. Mahoney، نويسنده , , William F. Vernier، نويسنده , , Ingrid P. Buchler، نويسنده , , Kun K. Wu، نويسنده , , Syaluan Yang، نويسنده , , Susan J. Hartmann، نويسنده , , David B. Reitz، نويسنده ,
Abstract :
A structure–activity relationship study was conducted on a series of tetrahydro-β-carboline-1-carboxylic acid analogs in order to identify the key functionality responsible for activity against the mitogen-activated protein kinase-activated protein kinase 2 enzyme (MK-2). The compounds were further evaluated for their ability to inhibit TNFα production in U937 cells and in vivo. These compounds represent a novel structural class of compounds capable of inhibiting MK-2 with remarkable selectivity.
Keywords :
?-Carboline-1 , rheumatoid arthritis , MAPKAP kinase 2 , MK-2 , TNF-? , inflammation
