期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 8, 页码 3996-4004出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01879
关键词
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资金
- Research Foundation Flanders FWO [G0D8617N]
- Ministerium fur Kultur und Wissenschaft des Landes Nordrhein-Westfalen
- Regierende Burgermeister von Berlin-inkl. Wissenschaft und Forschung
- Bundesministerium fur Bildung und Forschung
- Deutsche Forschungsgemeinschaft [SFB 1054]
- Slovene Research Agency [P1-0140]
- Hercules Foundation of the Flemish Government [20100225-7]
Constitutive proteolytic activity of MALT1 is associated with highly aggressive B-cell lymphomas. Chemical tools that detect active MALT1 have been reported, but suffer from poor cell permeability and/or cross-reactivity with the cysteine protease cathepsin B. Here, we report that the non-natural amino acid pipecolinic acid in the P2 position of substrates and chemical probes leads to improved selectivity toward MALT1 and results in cell-permeable fluorescent probes.
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