gsk-5498a and Arthritis--Rheumatoid

The role of calcium release-activated calcium (CRAC) channels is well characterized and is of particular importance in T-cell function. CRAC channels are involved in the pathogenesis of several autoimmune diseases, making it an attractive therapeutic target for treating inflammatory diseases, like rheumatoid arthritis (RA). A systematic structure-activity relationship study with the goal of optimizing lipophilicity successfully yielded two lead compounds,

Topics: Administration, Oral; Animals; Area Under Curve; Arthritis, Rheumatoid; Calcium; Calcium Channel Blockers; Calcium Release Activated Calcium Channels; Clinical Trials, Phase I as Topic; Drug Discovery; Humans; Jurkat Cells; Male; Mice; Mice, Inbred BALB C; Rats; Rats, Inbred Lew; Structure-Activity Relationship