| 摘要 |
Composition and methods for affecting cell proliferation, metabolism or sensitization, including the potentiation of proteasome inhibitor therapy for the treatment of disease caused by deregulation of ubiquitin-proteasome systems, in a cell or subject. The composition includes a compound in combination with a ubiquitin-proteasome inhibitor. In one embodiment, the compound has the formula C42H35N5O3 and the ubiquitin-protease inhibitor is a proteasome inhibitor or an inhibitor of another component of the ubiquitin-proteasome pathway such as an E3 ubiquitin ligase. In one embodiment of the method, the compound is administered to a cell or subject and a therapeutically effective amount of a ubiquitin-protease inhibitor is also administered. In another embodiment, the compound is administered to a cell or subject to inhibit cell proliferation. In yet another embodiment, the compound is administered to a cell or subject to increase, or augment, glucose utilization. |
| 主权项 |
1. A composition comprising a proteasome inhibitor and a compound having the following chemical formula: wherein R1 and R5 are each, independently, —H, a substituted or unsubstituted alkyl, a substituted or unsubstituted aryl, substituted or unsubstituted aralkyl or a substituted or unsubstituted heteroaralkyl; R2 is —H, a substituted or unsubstituted alkyl, a substituted or unsubstituted aryl, substituted or unsubstituted aralkyl or a substituted or unsubstituted heteroaralkyl; R3 is a substituted or unsubstituted alkyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaralkyl, or a substituted or unsubstituted heterocycloaralkyl; and R4 is unsubstituted alkyl, a substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted cycloalkylalkyl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted heteroaralkyl, or a substituted or unsubstituted benzophenonyl; or an active derivative thereof. |
