Discovery of Carboranes as Inducers of 20S Proteasome Activity

被引：14

作者：

Ban, Hyun Seung ^{[1
]}

Minegishi, Hidemitsu ^{[1
]}

Shimizu, Kazuki ^{[1
]}

Maruyama, Minako ^{[1
]}

Yasui, Yuka ^{[1
]}

Nakamura, Hiroyuki ^{[1
]}

机构：

[1] Gakushuin Univ, Fac Sci, Dept Chem, Toshima Ku, Tokyo 1718588, Japan

来源：

CHEMMEDCHEM | 2010年 / 5卷 / 08期

关键词：

20S proteasome; activators; caspase-like activity; drug discovery; trypsin-like activity; MULTICATALYTIC PROTEINASE; BETULINIC ACID; INHIBITORS; ACTIVATION; UBIQUITIN; SYSTEM; POTENT; DEGRADATION; DERIVATIVES; PEPTIDES;

D O I：

10.1002/cmdc.201000112

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Chemical Equation Presented) 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. © 2010 Wiley-VCH Verlag GmbH& Co. KGaA.

引用

页码：1236 / 1241

页数：6

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