MLN4924: a novel first-in-class inhibitor of NEDD8-activating enzyme for cancer therapy (Q38026589)

27 August 2017

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

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27 August 2017

Steffan T Nawrocki

1

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27 August 2017

Patrick Griffin

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2

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27 August 2017

Kevin R Kelly

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3

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27 August 2017

Jennifer S Carew

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4

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27 August 2017

language of work or name

English

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publication date

16 July 2012

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Expert Opinion on Investigational Drugs

27 August 2017

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27 August 2017

21

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27 August 2017

10

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27 August 2017

1563-1573

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Narrative review: protein degradation and human diseases: the ubiquitin connection

27 August 2017

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Intracellular protein degradation: from a vague idea thru the lysosome and the ubiquitin-proteasome system and onto human diseases and drug targeting

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The ubiquitin system for protein degradation and some of its roles in the control of the cell division cycle

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Targeting proteins for destruction by the ubiquitin system: implications for human pathobiology

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Proteasome inhibitors in cancer therapy: lessons from the first decade

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The ubiquitin-proteasome pathway: on protein death and cell life

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The ubiquitin-proteasome pathway: the complexity and myriad functions of proteins death

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Bortezomib as an antitumor agent.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Bortezomib for the treatment of mantle cell lymphoma

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

A phase 2 study of bortezomib in relapsed, refractory myeloma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Bortezomib or high-dose dexamethasone for relapsed multiple myeloma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Bortezomib plus melphalan and prednisone for initial treatment of multiple myeloma

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Novel proteasome inhibitors to overcome bortezomib resistance

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Treatment options for relapsed and refractory multiple myeloma

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Latest advances and current challenges in the treatment of multiple myeloma

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Bortezomib in the front-line treatment of multiple myeloma

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Drug discovery in the ubiquitin-proteasome system.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

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

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Modification of proteins by ubiquitin and ubiquitin-like proteins

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Concepts in sumoylation: a decade on

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The interferon regulated ubiquitin-like protein, ISG15, in tumorigenesis: friend or foe?

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Function and regulation of cullin-RING ubiquitin ligases

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Ubiquitin-binding proteins: decoders of ubiquitin-mediated cellular functions

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Origin and function of ubiquitin-like proteins

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Diversity of degradation signals in the ubiquitin-proteasome system

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Characterization of NEDD8, a developmentally down-regulated ubiquitin-like protein

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Nedd8 on cullin: building an expressway to protein destruction.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Crystal structure of the human ubiquitin-like protein NEDD8 and interactions with ubiquitin pathway enzymes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Conservation in the Mechanism of Nedd8 Activation by the Human AppBp1-Uba3 Heterodimer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The amyloid precursor protein-binding protein APP-BP1 drives the cell cycle through the S-M checkpoint and causes apoptosis in neurons

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The structure of the APPBP1-UBA3-NEDD8-ATP complex reveals the basis for selective ubiquitin-like protein activation by an E1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Identification of the activating and conjugating enzymes of the NEDD8 conjugation pathway

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

E2-RING expansion of the NEDD8 cascade confers specificity to cullin modification

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Dcn1 functions as a scaffold-type E3 ligase for cullin neddylation

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

SCCRO (DCUN1D1) is an essential component of the E3 complex for neddylation

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Cullin-based ubiquitin ligase and its control by NEDD8-conjugating system

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Structure of the Cul1-Rbx1-Skp1-F boxSkp2 SCF ubiquitin ligase complex

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

An intact NEDD8 pathway is required for Cullin-dependent ubiquitylation in mammalian cells

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Covalent modification of all members of human cullin family proteins by NEDD8

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

A targeted proteomic analysis of the ubiquitin-like modifier nedd8 and associated proteins.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Identification of NEDD8-conjugation site in human cullin-2

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Direct interactions between NEDD8 and ubiquitin E2 conjugating enzymes upregulate cullin-based E3 ligase activity.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

NEDD8 recruits E2-ubiquitin to SCF E3 ligase.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Multimodal activation of the ubiquitin ligase SCF by Nedd8 conjugation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

CAND1 binds to unneddylated CUL1 and regulates the formation of SCF ubiquitin E3 ligase complex

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Structural insights into NEDD8 activation of cullin-RING ligases: conformational control of conjugation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

NEDD8 modification of CUL1 dissociates p120(CAND1), an inhibitor of CUL1-SKP1 binding and SCF ligases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The ubiquitin system, disease, and drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

A Nedd8 conjugation pathway is essential for proteolytic targeting of p27Kip1 by ubiquitination

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Regulation of neddylation and deneddylation of cullin1 in SCFSkp2 ubiquitin ligase by F-box protein and substrate

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

In vitro reconstitution of SCF substrate ubiquitination with purified proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The NEDD8 pathway is required for proteasome-mediated degradation of human estrogen receptor (ER)-alpha and essential for the antiproliferative activity of ICI 182,780 in ERalpha-positive breast cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Control of cell proliferation via elevated NEDD8 conjugation in oral squamous cell carcinoma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Altered pattern of Cul-1 protein expression and neddylation in human lung tumours: relationships with CAND1 and cyclin E protein levels.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

TRIM40 promotes neddylation of IKKγ and is downregulated in gastrointestinal cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Nedd8 modification of cul-1 activates SCF(beta(TrCP))-dependent ubiquitination of IkappaBalpha

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

NEDD8-targeting drug MLN4924 elicits DNA rereplication by stabilizing Cdt1 in S phase, triggering checkpoint activation, apoptosis, and senescence in cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Inhibition of NEDD8-activating enzyme induces rereplication and apoptosis in human tumor cells consistent with deregulating CDT1 turnover

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Distinct types of diffuse large B-cell lymphoma identified by gene expression profiling

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Radiosensitization of human pancreatic cancer cells by MLN4924, an investigational NEDD8-activating enzyme inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

The p21-dependent radiosensitization of human breast cancer cells by MLN4924, an investigational inhibitor of NEDD8 activating enzyme

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Inhibition of the Nedd8 system sensitizes cells to DNA interstrand cross-linking agents.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Molecular and cellular effects of NEDD8-activating enzyme inhibition in myeloma.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

A gatekeeper residue for NEDD8-activating enzyme inhibition by MLN4924.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Treatment-emergent mutations in NAEβ confer resistance to the NEDD8-activating enzyme inhibitor MLN4924.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

Age and acute myeloid leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.707192

10.1517/13543784.2012.707192

21 January 2018

Identifiers

DOI

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27 August 2017

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