Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe.
Basic Information
ID: ALA4354872
Journal: J Med Chem
Title: Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe.
Authors: van de Plassche MAT, O'Neill TJ, Seeholzer T, Turk B, Krappmann D, Verhelst SHL.
Abstract: 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.
CiteXplore: 32227886
DOI: 10.1021/acs.jmedchem.9b01879
Patent ID: ┄