Development and biological evaluation of acyl protein thioesterase 1 (APT1) inhibitors

被引:19
作者
Deck, P
Pendzialek, D
Biel, M
Wagner, M
Popkirova, B
Ludolph, B
Kragol, G
Kuhlmann, J [1 ]
Giannis, A
Waldmann, H
机构
[1] Max Planck Inst Mol Physiol, Dept Biol Struct, Otto Hahn Str 11, D-44227 Dortmund, Germany
[2] Univ Leipzig, Inst Organ Chem, D-04103 Leipzig, Germany
[3] Max Planck Inst Mol Physiol, Dept Biol Chem, D-44227 Dortmund, Germany
[4] Univ Dortmund, Fachbereich Chem, Dortmund, Germany
关键词
biological activity; enzyme inhibitors; esterases; peptidomimetics; proteins;
D O I
10.1002/anie.200462625
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
It works both ways: The development of potent peptidomimetic acyl protein thioesterase 1 (APT1) inhibitors, such as Raspalin 3 (see structure), and their use in biological and biochemical investigations are reported. The results show that the enzyme can deacylate and acylate Ras proteins. (Chemical Equation Presented). © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:4975 / 4980
页数:6
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