jm9b01879_si_002.pdb (243.97 kB)

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

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posted on 09.04.2020, 19:05 by Merel A. T. van de Plassche, Thomas J. O’Neill, Thomas Seeholzer, Boris Turk, Daniel Krappmann, Steven H. L. Verhelst
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.