The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity

被引:42
作者
Clerc, Jerome [1 ]
Li, Nan [2 ,3 ]
Krahn, Daniel [1 ]
Groll, Michael [4 ]
Bachmann, Andre S. [5 ]
Florea, Bogdan I. [2 ,3 ]
Overkleeft, Herman S. [2 ,3 ]
Kaiser, Markus [1 ]
机构
[1] Univ Duisburg Essen, Fak Biol & Geog, Zentrum Med Biotechnol, D-45117 Essen, Germany
[2] Leiden Inst Chem, NL-2333 CC Leiden, Netherlands
[3] Netherlands Prote Ctr, Gorlaeus Labs, NL-2333 CC Leiden, Netherlands
[4] Tech Univ Munich, Ctr Integrated Prot Sci, Dept Chem, D-85747 Garching, Germany
[5] Univ Hawaii Manao, Canc Res Ctr Hawaii, Honolulu, HI 96813 USA
关键词
20S PROTEASOME; IN-VIVO; THYMOPROTEASOME; CHEMISTRY; BACTERIUM; REVEALS; TMC-95A; YEAST;
D O I
10.1039/c0cc02238a
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The preparation of a Syringolin A/Glidobactin A hybrid (SylA-GlbA) consisting of a SylA macrocycle connected to the GlbA side chain and its potent proteasome targeting of all three proteasomal subsites is reported. The influence of the syrbactin macrocycle moiety on subsite selectivity is demonstrated.
引用
收藏
页码:385 / 387
页数:3
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