Leiden University Scholarly Publications

Persistent URL of this record https://hdl.handle.net/1887/3201320

In Collections

This item can be found in the following collections:

Plassche, M.A.T.; O'Neill, T.J.; Seeholzer, T.; Turk, B.; Krappmann, D.; Verhelst, S.H.L. (2020)

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

Article / Letter to editor
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.
All authors
Plassche, M.A.T.; O'Neill, T.J.; Seeholzer, T.; Turk, B.; Krappmann, D.; Verhelst, S.H.L.
Date
2020-05-23
Volume
63
Issue
8
Pages
3996 - 4004
DOI
doi:10.1021/acs.jmedchem.9b01879