Structural analysis of phenothiazine derivatives as allosteric inhibitors of the MALT1 paracaspase.
- Schlauderer, F.
- Lammens, K.
- Nagel, D.
- Vincendeau, M.
- Eitelhuber, A.C.
- Verhelst, S.H.
- Kling, D.
- Chrusciel, A.
- Ruland, J.
- Krappmann, D.
- Hopfner, K.-P.
DOIAbstract
Second site: In the crystal structure of human MALT1casp-Ig3 (mucosa-associated lymphoid tissue lymphoma translocation protein 1) in complex with the tricyclic phenothiazine derivative thioridazine (violet in the picture), the inhibitor is bound in a hydrophobic pocket far from the active site. This explains the action of phenothiazine derivatives as noncompetitive, reversible inhibitors
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