Description
LY3000328 is a potent cathepsin S inhibitor (IC
50 = 7.7 nM for the human enzyme). It is selective for cathepsin S over cathepsin L, K, B, and V (IC
50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.
Uses
LY 3000328 is a cathepsin S inhibitor for treatment of abdominal aortic aneurysm. Further provides methods for treating plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a disclosed compound.
References
[1] wiener jj, sun s, thurmond rl. recent advances in the design of cathepsin s inhibitors. curr top med chem. 2010;10(7):717-32.
[2] lee-dutra a, wiener dk, sun s. cathepsin s inhibitors: 2004-2010. expert opin ther pat. 2011;21(3):311-37.
