MRK003, a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma

Notch-stimulated signaling cascade results in transcriptional regulation of genes involved in cell fate decision, apoptosis and proliferation and has been implicated in various malignancies. Here, we investigated the impact of MRK003, an inhibitor of this pathway, on myeloma and lymphoma cells. We f...

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Veröffentlicht in:	Leukemia 2012-02, Vol.26 (2), p.340-348
Hauptverfasser:	Ramakrishnan, V, Ansell, S, Haug, J, Grote, D, Kimlinger, T, Stenson, M, Timm, M, Wellik, L, Halling, T, Rajkumar, S V, Kumar, S
Format:	Artikel
Sprache:	eng
Schlagworte:	1-Phosphatidylinositol 3-kinase AKT protein AKT1 protein Amyloid Precursor Protein Secretases - antagonists & inhibitors Apoptosis Apoptosis - drug effects Base Sequence Bcl-2 protein Bcl-x protein Biological and medical sciences c-Myc protein Cancer Research Caspase Cell fate Cell Line, Tumor Cell lines Cell proliferation Critical Care Medicine Crosstalk Cyclic S-Oxides - pharmacology Cyclic S-Oxides - therapeutic use Cyclin D1 Diagnosis DNA Primers Drug Screening Assays, Antitumor Drug therapy Enzyme inhibitors Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Gene expression Gene regulation Genetic aspects Health services Hematologic and hematopoietic diseases Hematology Humans Immunodeficiencies. Immunoglobulinopathies Immunoglobulinopathies Immunopathology Intensive Internal Medicine Kinases Leukemias. Malignant lymphomas. Malignant reticulosis. Myelofibrosis Ligands Lymphoma Lymphoma, Non-Hodgkin - drug therapy Lymphoma, Non-Hodgkin - pathology Medical sciences Medicine Medicine & Public Health Multiple myeloma Multiple Myeloma - drug therapy Multiple Myeloma - pathology Myc protein Non-Hodgkin's lymphoma Non-Hodgkin's lymphomas Notch protein Oncology original-article Receptors Reverse Transcriptase Polymerase Chain Reaction Secretase Signal transduction Signaling Thiadiazoles - pharmacology Thiadiazoles - therapeutic use Transcription Tumor cell lines XIAP protein
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