Total Synthesis and Biological Activity of Lactacystin, Omuralide and Analogs
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概要
- 論文の詳細を見る
Lactacystin (1) and the related β-lactone omuralide (2) are remarkably selective and potent irreversible inhibitors of the 20S proteasome, a large polymolecular protein machine which is responsible for the degradation of ubiquitin-labeled proteins. Because of this fact 1 and 2 have emerged as important tools in biochemistry and cell biology. The challenge of synthesis has been accepted by several research groups with the result that 1 and 2 and their analogs can now be synthesized by a variety of synthetic approaches. This review summarizes the synthetic processes which have been developed to date for the production of such compounds. The study of biological activity of analogs of 1 and 2 has clearly defined the structural features which are responsible for the potency of 1 and 2,as described in the closing section of this account. It is concluded that 1 and 2 are nearly optimal for the irreversible inactivation of the 20S proteasome.
- 公益社団法人日本薬学会の論文
- 1999-01-15
著者
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Li Wei-dong
Department Of Chemistry And Chemical Biology Harvard University Cambridge
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Corey E.
Department Of Chemistry And Chemical Biology Harvard University Cambridge
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Corey E.J.
Department of Chemistry and Chemical Biology, Harvard University, Cambridge