6576-05-2Relevant articles and documents
NEW COMPOUNDS FOR TREATMENT OF DISEASES RELATED TO DUX4 EXPRESSION
-
Page/Page column 58; 85, (2021/06/04)
The present invention relates to compounds for the treatment of diseases related to DUX4 expression, such as muscular dystrophies. It also relates to use of such compounds, or to methods of use of such compounds.
Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors
Seerden, Jean-Paul G.,Leusink-Ionescu, Gabriela,Leguijt, Robin,Saccavini, Catherine,Gelens, Edith,Dros, Bas,Woudenberg-Vrenken, Titia,Molema, Grietje,Kamps, Jan A.A.M.,Kellogg, Richard M.
, p. 1352 - 1357 (2014/03/21)
The design, synthesis and biological evaluation of novel triazolyl p38α MAPK inhibitors with improved water solubility for formulation in cationic liposomes (SAINT-O-Somes) targeted at diseased endothelial cells is described. Water-solubilizing groups wer
Ligand-protein interactions of selective casein kinase 1δ inhibitors
Mente, Scot,Arnold, Eric,Butler, Todd,Chakrapani, Subramanyam,Chandrasekaran, Ramalakshmi,Cherry, Kevin,Dirico, Ken,Doran, Angela,Fisher, Katherine,Galatsis, Paul,Green, Michael,Hayward, Matthew,Humphrey, John,Knafels, John,Li, Jianke,Liu, Shenping,Marconi, Michael,McDonald, Scott,Ohren, Jeff,Paradis, Vanessa,Sneed, Blossom,Walton, Kevin,Wager, Travis
, p. 6819 - 6828 (2013/10/01)
Casein kinase 1δ (CK1δ) and 1ε (CK1ε) are believed to be necessary enzymes for the regulation of circadian rhythms in all mammals. On the basis of our previously published work demonstrating a CK1ε-preferring compound to be an ineffective circadian clock modulator, we have synthesized a series of pyrazole-substitued pyridine inhibitors, selective for the CK1δ isoform. Additionally, using structure-based drug design, we have been able to exploit differences in the hinge region between CK1δ and p38 to find selective inhibitors that have minimal p38 activity. The SAR, brain exposure, and the effect of these inhibitors on mouse circadian rhythms are described. The in vivo evaluation of these inhibitors demonstrates that selective inhibition of CK1δ at sufficient central exposure levels is capable of modulating circadian rhythms.