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

MLN4924, an investigational NEDD8-activating enzyme (NAE) inhibitor, in patients (pts) with advanced solid tumors: Phase I study of multiple treatment schedules.

(2017) J. S. Kauh et al.   JOURNAL OF CLINICAL ONCOLOGY

Ubiquitin-Binding Proteins: Decoders of Ubiquitin-Mediated Cellular Functions

(2012) Koraljka Husnjak et al.   Annual Review of Biochemistry

Treatment-Emergent Mutations in NAEβ Confer Resistance to the NEDD8-Activating Enzyme Inhibitor MLN4924

(2012) Michael A. Milhollen et al.   CANCER CELL

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

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

Molecular and Cellular Effects of NEDD8-Activating Enzyme Inhibition in Myeloma

(2012) D. W. McMillin et al.   MOLECULAR CANCER THERAPEUTICS

Latest advances and current challenges in the treatment of multiple myeloma

(2012) Anuj Mahindra et al.   Nature Reviews Clinical Oncology

Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib

(2012) Jeffrey A. Sosman et al.   NEW ENGLAND JOURNAL OF MEDICINE

The p21-Dependent Radiosensitization of Human Breast Cancer Cells by MLN4924, an Investigational Inhibitor of NEDD8 Activating Enzyme

(2012) Dong Yang et al.   PLoS One

A Gatekeeper Residue for NEDD8-Activating Enzyme Inhibition by MLN4924

(2012) Julia I. Toth et al.   Cell Reports

Radiosensitization of Human Pancreatic Cancer Cells by MLN4924, an Investigational NEDD8-Activating Enzyme Inhibitor

(2011) D. Wei et al.   CANCER RESEARCH

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

TRIM40 promotes neddylation of IKK  and is downregulated in gastrointestinal cancers

(2011) K. Noguchi et al.   CARCINOGENESIS

Treatment Options for Relapsed and Refractory Multiple Myeloma

(2011) Sagar Lonial et al.   CLINICAL CANCER RESEARCH

Novel Proteasome Inhibitors to Overcome Bortezomib Resistance

(2011) Amy M. Ruschak et al.   JNCI-Journal of the National Cancer Institute

Initial testing of the investigational NEDD8-activating enzyme inhibitor MLN4924 by the pediatric preclinical testing program

(2011) Malcolm A. Smith et al.   PEDIATRIC BLOOD & CANCER

MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF- B-dependent lymphoma

(2010) M. A. Milhollen et al.   BLOOD

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

Substrate-Assisted Inhibition of Ubiquitin-like Protein-Activating Enzymes: The NEDD8 E1 Inhibitor MLN4924 Forms a NEDD8-AMP Mimetic In Situ

(2010) James E. Brownell et al.   MOLECULAR CELL

Clinical challenges associated with bortezomib therapy in multiple myeloma and Waldenströms Macroglobulinemia

(2009) Jacob P. Laubach et al.   LEUKEMIA & LYMPHOMA

E2-RING Expansion of the NEDD8 Cascade Confers Specificity to Cullin Modification

(2009) Danny T. Huang et al.   MOLECULAR CELL

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

(2009) Teresa A. Soucy et al.   NATURE

Origin and function of ubiquitin-like proteins

(2009) Mark Hochstrasser   NATURE

Ubiquitin-like protein activation by E1 enzymes: the apex for downstream signalling pathways

(2009) Brenda A. Schulman et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Targeting Proteins for Destruction by the Ubiquitin System: Implications for Human Pathobiology

(2008) Alan L. Schwartz et al.   Annual Review of Pharmacology and Toxicology

The ubiquitin system, disease, and drug discovery

(2008) Matthew D Petroski   BMC BIOCHEMISTRY

Structural Insights into NEDD8 Activation of Cullin-RING Ligases: Conformational Control of Conjugation

(2008) David M. Duda et al.   CELL

Proteasome Inhibitors in Cancer Therapy: Lessons from the First Decade

(2008) R. Z. Orlowski et al.   CLINICAL CANCER RESEARCH

Bortezomib in the front-line treatment of multiple myeloma

(2008) Paul G Richardson et al.   Expert Review of Anticancer Therapy

SCCRO (DCUN1D1) Is an Essential Component of the E3 Complex for Neddylation

(2008) Alexander Y. Kim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Targeted Proteomic Analysis of the Ubiquitin-Like Modifier Nedd8 and Associated Proteins

(2008) Jeffrey Jones et al.   JOURNAL OF PROTEOME RESEARCH

Dcn1 Functions as a Scaffold-Type E3 Ligase for Cullin Neddylation

(2008) Thimo Kurz et al.   MOLECULAR CELL

Multimodal Activation of the Ubiquitin Ligase SCF by Nedd8 Conjugation

(2008) Anjanabha Saha et al.   MOLECULAR CELL

Diversity of degradation signals in the ubiquitin–proteasome system

(2008) Tommer Ravid et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Bortezomib plus Melphalan and Prednisone for Initial Treatment of Multiple Myeloma

(2008) Jesús F. San Miguel et al.   NEW ENGLAND JOURNAL OF MEDICINE