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Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe

Tijdschriftbijdrage - Tijdschriftartikel

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.
Tijdschrift: Journal of Medicinal Chemistry
ISSN: 0022-2623
Issue: 8
Volume: 63
Pagina's: 3996 - 4004
Jaar van publicatie:2020
BOF-keylabel:ja
IOF-keylabel:ja
BOF-publication weight:10
CSS-citation score:1
Auteurs:International
Authors from:Higher Education
Toegankelijkheid:Closed