| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a compound that inhibits an E1 activating enzyme. <P>SOLUTION: The invention relates to a compound that inhibits an E1 activating enzyme, a pharmaceutical composition comprising the compound, and a method of using the compound. The compound is useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders, and for treating inflammation associated with infection and cachexia. The compound may be assayed for its ability to inhibit the E1 enzyme in vitro or in vivo, or in cells or an animal model. The compound may be assessed for its ability to bind or directly mediate E1 enzyme activity. Alternatively, the activity of the compound may be assessed through an indirect cellular assay or an assay measuring a downstream effect of E1 activation to assess inhibition of a downstream effect of E1 inhibition (e.g., inhibition of cullin-dependent ubiquitination and proteolysis). <P>COPYRIGHT: (C)2013,JPO&INPIT |
