Synergistic anti-AML effects of the LSD1 inhibitor T-3775440 and the NEDD8-activating enzyme inhibitor pevonedistat via transdifferentiation and DNA rereplication

The NAE inhibitor pevonedistat interacts with the HDAC inhibitor belinostat to target AML cells by disrupting the DDR

(2016) L. Zhou et al.   BLOOD

Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes

(2016) John P. McGrath et al.   CANCER RESEARCH

A Novel LSD1 Inhibitor T-3775440 Disrupts GFI1B-Containing Complex Leading to Transdifferentiation and Impaired Growth of AML Cells

(2016) Yoshinori Ishikawa et al.   MOLECULAR CANCER THERAPEUTICS

Pevonedistat (MLN4924), a First-in-Class NEDD8-activating enzyme inhibitor, in patients with acute myeloid leukaemia and myelodysplastic syndromes: a phase 1 study

(2015) Ronan T. Swords et al.   BRITISH JOURNAL OF HAEMATOLOGY

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

(2015) Helai P. Mohammad et al.   CANCER CELL

Phase I Study of the Investigational NEDD8-Activating Enzyme Inhibitor Pevonedistat (TAK-924/MLN4924) in Patients with Advanced Solid Tumors

(2015) J. Sarantopoulos et al.   CLINICAL CANCER RESEARCH

Pharmacological targeting of miR-155 via the NEDD8-activating enzyme inhibitor MLN4924 (Pevonedistat) in FLT3-ITD acute myeloid leukemia

(2015) J Khalife et al.   LEUKEMIA

Lysine-specific demethylase 1 (LSD1) in hematopoietic and lymphoid neoplasms

(2014) D. Niebel et al.   BLOOD

Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells

(2014) W Fiskus et al.   LEUKEMIA

Nedd8-Activating Enzyme Inhibitor MLN4924 Provides Synergy with Mitomycin C through Interactions with ATR, BRCA1/BRCA2, and Chromatin Dynamics Pathways

(2014) K. Garcia et al.   MOLECULAR CANCER THERAPEUTICS

SCF ubiquitin ligase-targeted therapies

(2014) Jeffrey R. Skaar et al.   NATURE REVIEWS DRUG DISCOVERY

The histone demethylase LSD1/KDM1A promotes the DNA damage response

(2013) Nima Mosammaparast et al.   JOURNAL OF CELL BIOLOGY

The Histone Demethylase KDM1A Sustains the Oncogenic Potential of MLL-AF9 Leukemia Stem Cells

(2012) William J. Harris et al.   CANCER CELL

Novel DNA Damage Checkpoints Mediating Cell Death Induced by the NEDD8-Activating Enzyme Inhibitor MLN4924

(2012) J. L. Blank et al.   CANCER RESEARCH

MLN4924: a novel first-in-class inhibitor of NEDD8-activating enzyme for cancer therapy

(2012) Steffan T Nawrocki et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

LSD1 inhibition: a therapeutic strategy in cancer?

(2012) James T Lynch et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Inhibition of the Nedd8 System Sensitizes Cells to DNA Interstrand Cross-linking Agents

(2012) Y. Kee et al.   MOLECULAR CANCER RESEARCH

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

(2012) Tino Schenk et al.   NATURE MEDICINE

Inhibition of NEDD8-Activating Enzyme Induces Rereplication and Apoptosis in Human Tumor Cells Consistent with Deregulating CDT1 Turnover

(2011) M. A. Milhollen et al.   CANCER RESEARCH

Densely Interconnected Transcriptional Circuits Control Cell States in Human Hematopoiesis

(2011) Noa Novershtern et al.   CELL

Quantitative Proteomic Analysis of Cellular Protein Modulation upon Inhibition of the NEDD8-Activating Enzyme by MLN4924

(2011) Hua Liao et al.   MOLECULAR & CELLULAR PROTEOMICS

Inactivation of SAG E3 Ubiquitin Ligase Blocks Embryonic Stem Cell Differentiation and Sensitizes Leukemia Cells to Retinoid Acid

(2011) Mingjia Tan et al.   PLoS One

Inhibition of NEDD8-activating enzyme: a novel approach for the treatment of acute myeloid leukemia

(2010) R. T. Swords et al.   BLOOD

NEDD8-Targeting Drug MLN4924 Elicits DNA Rereplication by Stabilizing Cdt1 in S Phase, Triggering Checkpoint Activation, Apoptosis, and Senescence in Cancer Cells

(2010) J. J. Lin et al.   CANCER RESEARCH

The role of PU.1 and GATA-1 transcription factors during normal and leukemogenic hematopoiesis

(2010) P Burda et al.   LEUKEMIA

PU.1 Activation Relieves GATA-1-Mediated Repression of Cebpa and Cbfb during Leukemia Differentiation

(2009) P. Burda et al.   MOLECULAR CANCER RESEARCH

An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

(2009) Teresa A. Soucy et al.   NATURE