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Discovery of Carboranes as Inducers of 20S Proteasome Activity
Author(s) -
Ban Hyun Seung,
Minegishi Hidemitsu,
Shimizu Kazuki,
Maruyama Minako,
Yasui Yuka,
Nakamura Hiroyuki
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000112
Subject(s) - proteasome , carborane , chemistry , small molecule , inducer , computational biology , biochemistry , combinatorial chemistry , stereochemistry , biology , gene
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.