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Open Access Green möglich sobald Postprint bei der ZB eingereicht worden ist.
Pharmacologic inhibition of MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL.
Cancer Cell 22, 825-837 (2012)
Proteolytic activity of the mucosa-associated lymphoid tissue lymphoma translocation protein-1 (MALT1) paracaspase is required for survival of the activated B cell subtype of diffuse large B cell lymphoma (ABC-DLBCL). We have identified distinct derivatives of medicinal active phenothiazines, namely mepazine, thioridazine, and promazine, as small molecule inhibitors of the MALT1 protease. These phenothiazines selectively inhibit cleavage activity of recombinant and cellular MALT1 by a noncompetitive mechanism. Consequently, the compounds inhibit anti-apoptotic NF-κB signaling and elicit toxic effects selectively on MALT1-dependent ABC-DLBCL cells in vitro and in vivo. Our data provide a conceptual proof for a clinical application of distinct phenothiazines in the treatment of ABC-DLBCL.
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Publikationstyp
Artikel: Journalartikel
Dokumenttyp
Wissenschaftlicher Artikel
Schlagwörter
B-CELL LYMPHOMA; PARACASPASE MALT1; RNA INTERFERENCE; ACTIVATION; THIORIDAZINE; SURVIVAL; CLEAVAGE; CANCER; PROLIFERATION; METACASPASES
ISSN (print) / ISBN
1535-6108
e-ISSN
1878-3686
Zeitschrift
Cancer Cell
Quellenangaben
Band: 22,
Heft: 6,
Seiten: 825-837
Verlag
Cell Press
Verlagsort
Cambridge, Mass.
Nichtpatentliteratur
Publikationen
Begutachtungsstatus
Peer reviewed
Institut(e)
Research Unit Signaling and Translation (SAT)
Institute of Molecular Immunology (IMI)
Institute of Molecular Toxicology and Pharmacology (TOXI)
Institute of Molecular Immunology (IMI)
Institute of Molecular Toxicology and Pharmacology (TOXI)