Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma

Inhibition of the bromodomain and extra-terminal (BET) proteins is a promising therapeutic strategy for various hematologic cancers. Previous studies suggest that BET inhibitors constrain tumor cell proliferation and survival mainly through the suppression of MYC transcription and activity. However,...

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Veröffentlicht in:	Leukemia 2017-08, Vol.31 (8), p.1760-1769
Hauptverfasser:	Siu, K T, Ramachandran, J, Yee, A J, Eda, H, Santo, L, Panaroni, C, Mertz, J A, Sims III, R J, Cooper, M R, Raje, N
Format:	Artikel
Sprache:	eng
Schlagworte:	13/2 13/31 38/39 38/77 38/89 45/22 631/67/1059/153 631/67/1990/804 631/92/436/108 64/60 692/308/2778 692/700/565/1436/1437 96/106 96/109 Animals Anticancer properties Antimitotic agents Antineoplastic agents Antitumor activity Apoptosis Benzazepines - pharmacology Binding proteins Biocompatibility Biotechnology Bone marrow Cancer Research Caspase Cell cycle Cell proliferation Cell survival Critical Care Medicine Cytokines Cytotoxicity Degradation Drug therapy Drug therapy, Combination Drugs G1 Phase Cell Cycle Checkpoints Genetic aspects Health aspects Hematology Humans Ikaros protein Ikaros Transcription Factor - analysis Ikaros Transcription Factor - genetics Immunomodulation In vitro methods and tests In vivo methods and tests Inhibition Inhibitors Intensive Interferon regulatory factor 4 Interferon Regulatory Factors - analysis Interferon Regulatory Factors - genetics Internal Medicine Isoxazoles - pharmacology Medicine Medicine & Public Health Mice Multiple myeloma Multiple Myeloma - drug therapy Multiple Myeloma - pathology Myc protein Nuclear Proteins - antagonists & inhibitors Oncology original-article Patients Protein-Serine-Threonine Kinases - antagonists & inhibitors Proteins Proto-Oncogene Proteins c-myc - analysis Proto-Oncogene Proteins c-myc - genetics Rodents Stromal cells Synergism Terminal protein Testing Toxicity Transcription Transcription Factors - antagonists & inhibitors Tumors Xenografts Xenotransplantation
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