The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)- mepazine and one of its intermediates.
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(2015/01/16)
Structural analysis of phenothiazine derivatives as allosteric inhibitors of the MALT1 paracaspase
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. Copyright
Schlauderer, Florian,Lammens, Katja,Nagel, Daniel,Vincendeau, Michelle,Eitelhuber, Andrea C.,Verhelst, Steven H. L.,Kling, Dale,Chrusciel, Al,Ruland, Juergen,Krappmann, Daniel,Hopfner, Karl-Peter