Discovery of Carboranes as Inducers of 20S Proteasome Activity

The carborane framework gives analogues able to induce 20S proteasome activities. A series of ortho‐carboranylphenoxy derivatives were synthesized as 20S proteasome agonists, and carborane derivatives 11 a and 11 b were found to be potent inducers of the β1 and β2 activities of the 20S proteasome. S...

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Veröffentlicht in:ChemMedChem 2010-08, Vol.5 (8), p.1236-1241
Hauptverfasser: Ban, Hyun Seung, Minegishi, Hidemitsu, Shimizu, Kazuki, Maruyama, Minako, Yasui, Yuka, Nakamura, Hiroyuki
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Sprache:eng
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Zusammenfassung:The carborane framework gives analogues able to induce 20S proteasome activities. A series of ortho‐carboranylphenoxy derivatives were synthesized as 20S proteasome agonists, and carborane derivatives 11 a and 11 b were found to be potent inducers of the β1 and β2 activities of the 20S proteasome. Since small‐molecule proteasome activators have not been developed, the carboranes described here have potential as chemical probes for the investigation of proteasome‐dependent degradation pathways.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201000112