Autoimmune disease

In vitro and mouse studies identified an isopropylcarboxamide-based Hsp90B1 inhibitor that could help treat ulcerative colitis (UC). Structure-based design, chemical synthesis and in vitro activity and binding assays of isopropylcarboxamide analogs yielded a compound that inhibited Hsp90B1 with an IC₅₀ of 2 nM and bound Hsp90B1 with a K_d of 19.6 nM. In a mouse model of UC, the compound decreased clinical disease scores and levels of proinflammatory cytokines in the serum and colon and increased body weight compared with vehicle. Next steps could include optimizing and testing the inhibitor in additional models of UC...