1219130-54-7Relevant articles and documents
Structural Elucidation of a Nonpeptidic Inhibitor Specific for the Human Immunoproteasome
Cui, Haissi,Baur, Regina,Le Chapelain, Camille,Dubiella, Christian,Heinemeyer, Wolfgang,Huber, Eva M.,Groll, Michael
, p. 523 - 526 (2017)
Selective inhibition of the immunoproteasome is a promising approach towards the development of immunomodulatory drugs. Recently, a class of substituted thiazole compounds that combine a nonpeptidic scaffold with the absence of an electrophile was reported in a patent. Here, we investigated the mode of action of the lead compound by using a sophisticated chimeric yeast model of the human immunoproteasome for structural studies. The inhibitor adopts a unique orientation perpendicular to the β5i substrate-binding channel. Distinct interactions between the inhibitor and the subpockets of the human immunoproteasome account for its isotype selectivity.
SUBSTITUTED THIAZOLE COMPOUNDS
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Page/Page column 36, (2014/06/24)
The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.
HETEROCYCLIC BIARYL DERIVATIVE AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT
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Page/Page column 28, (2011/08/04)
Novel heterocyclic biaryl derivatives were disclosed which are useful as pharmaceutical agents and which exhibit a phosphodiesterase-inhibitory action. The heterocyclic biaryl derivatives are represented by the following general formula (1): wherein the H
