Development of Protein Phosphatases Inhibitors: A Focused Library Approach.
-
- Sodeoka Mikiko
- Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
-
- Baba Yoshiyasu
- Institute of Multidisciplinary Research for Advanced Materials, Tohoku University
書誌事項
- タイトル別名
-
- A ocused Library Approach
この論文をさがす
抄録
Selective inhibitors of protein phosphatases are expected to be useful tools for clarifying the biological functions of the phosphatases themselves, and also candidates for novel therapeutics. In terms of the catalytic site structure, protein phosphatases can be divided into two large groups: one is the protein serine/threonine phosphatases (PPs) group, and the other is the protein phosphatases (PTPs)/dual-specificity phosphatases (DSPs) group. We planned a library approach to the identification of PP- or PTP/DSP-selective inhibitors, in which unique structures derived from natural products are used as “core” phosphate mimics. In this paper we describe a synthesis and evaluation of a PTP/DSP inhibitor-oriented library. A series of novel tetronic acid derivatives were synthesized and evaluated as inhibitors of the dual-specificity protein phosphatases VHR and cdc25B, and tyrosine phosphatase PTP-S2. Several compounds were found to be potent inhibitors of cdc25B which is a key enzyme for cell-cycle progression.
収録刊行物
-
- 有機合成化学協会誌
-
有機合成化学協会誌 59 (11), 1095-1102, 2001
公益社団法人 有機合成化学協会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390282680253585664
-
- NII論文ID
- 10012286212
-
- NII書誌ID
- AN0024521X
-
- COI
- 1:CAS:528:DC%2BD3MXotlKmsrc%3D
-
- ISSN
- 18836526
- 00379980
-
- NDL書誌ID
- 5968871
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可