Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation (Q88080886)

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20 March 2020

title

Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation (English)

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20 March 2020

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R. Kiplin Guy

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Jared T Hammill

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author name string

Deepak Bhasin

2

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20 March 2020

Daniel C Scott

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Jaeki Min

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Yizhe Chen

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Yan Lu

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20 March 2020

Lei Yang

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Ho Shin Kim

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20 March 2020

Michele C Connelly

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20 March 2020

Courtney Hammill

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20 March 2020

Gloria Holbrook

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Cynthia Jeffries

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Bhuvanesh Singh

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publication date

26 March 2018

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Journal of Medicinal Chemistry

20 March 2020

published in

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volume

61

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issue

7

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20 March 2020

page(s)

2694-2706

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Antihypertensive ureidopiperidines

20 March 2020

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1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels

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Direct Reductive Amination of Aldehydes and Ketones Using Phenylsilane: Catalysis by Dibutyltin Dichloride

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The role of novel oncogenes squamous cell carcinoma-related oncogene and phosphatidylinositol 3-kinase p110alpha in squamous cell carcinoma of the oral tongue.

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Squamous cell carcinoma related oncogene regulates angiogenesis through vascular endothelial growth factor-A.

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Function and regulation of cullin-RING ubiquitin ligases

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Squamous cell carcinoma related oncogene/DCUN1D1 is highly conserved and activated by amplification in squamous cell carcinomas

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

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12 December 2020

SCCRO (DCUN1D1) induces extracellular matrix invasion by activating matrix metalloproteinase 2.

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12 December 2020

Prediction of activation energies for aromatic oxidation by cytochrome P450.

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12 December 2020

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

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RING domain E3 ubiquitin ligases

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Targeting NEDD8-activated cullin-RING ligases for the treatment of cancer.

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12 December 2020

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

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12 December 2020

Potent and selective inhibition of human cytochrome P450 3A4 by seco-pancratistatin structural analogs

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12 December 2020

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

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12 December 2020

SCCRO promotes glioma formation and malignant progression in mice

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Inhibitors for E3 ubiquitin ligases

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A natural product-like inhibitor of NEDD8-activating enzyme

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12 December 2020

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

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12 December 2020

Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design

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12 December 2020

N-Terminal Acetylation Acts as an Avidity Enhancer Within an Interconnected Multiprotein Complex

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12 December 2020

Inhibition of NEDD8-conjugation pathway by novel molecules: potential approaches to anticancer therapy

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12 December 2020

Immunohistochemical Expression of DCUN1D1 in Non-small Cell Lung Carcinoma: Its Relation to Brain Metastasis

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12 December 2020

Evaluation of hepatic clearance prediction using in vitro data: emphasis on fraction unbound in plasma and drug ionisation using a database of 107 drugs

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12 December 2020

Discovery of a natural product inhibitor targeting protein neddylation by structure-based virtual screening

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12 December 2020

Potent small molecule Hedgehog agonists induce VEGF expression in vitro

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12 December 2020

A metal-based inhibitor of NEDD8-activating enzyme

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12 December 2020

The ubiquitin proteasome system - implications for cell cycle control and the targeted treatment of cancer

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12 December 2020

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

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12 December 2020

Clinical and marketed proteasome inhibitors for cancer treatment

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12 December 2020

Integrative genomics analysis identifies candidate drivers at 3q26-29 amplicon in squamous cell carcinoma of the lung

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12 December 2020

Coamplification and cooperation: toward identifying biologically relevant oncogenes

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12 December 2020

Building and remodelling Cullin-RING E3 ubiquitin ligases

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12 December 2020

QSAR modeling: where have you been? Where are you going to?

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12 December 2020

Emerging therapies targeting the ubiquitin proteasome system in cancer

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12 December 2020

A CULLINary ride across the secretory pathway: more than just secretion

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12 December 2020

Effective virtual screening strategy toward covalent ligands: identification of novel NEDD8-activating enzyme inhibitors

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12 December 2020

Identification of druggable cancer driver genes amplified across TCGA datasets

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12 December 2020

Structure of a RING E3 trapped in action reveals ligation mechanism for the ubiquitin-like protein NEDD8

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12 December 2020

Regulation of cancer-related pathways by protein NEDDylation and strategies for the use of NEDD8 inhibitors in the clinic

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12 December 2020

Protein neddylation: beyond cullin-RING ligases

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12 December 2020

E3 ubiquitin ligases as drug targets and prognostic biomarkers in melanoma

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12 December 2020

Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation

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12 December 2020

Drugging the undruggables: exploring the ubiquitin system for drug development

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12 December 2020

Discovery of a novel NEDD8 Activating Enzyme Inhibitor with Piperidin-4-amine Scaffold by Structure-Based Virtual Screening

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12 December 2020

Cullin-RING ligases in regulation of autophagy

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12 December 2020

Targeted inhibition of the COP9 signalosome for treatment of cancer

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12 December 2020

Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity

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12 December 2020

A Rhodium(III) Complex as an Inhibitor of Neural Precursor Cell Expressed, Developmentally Down-Regulated 8-Activating Enzyme with in Vivo Activity against Inflammatory Bowel Disease

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12 December 2020

Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase.

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12 December 2020

Squamous cell carcinoma-related oncogene (SCCRO) neddylates Cul3 protein to selectively promote midbody localization and activity of Cul3KLHL21 protein complex during abscission.

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12 December 2020

A potent small-molecule inhibitor of the DCN1-UBC12 interaction that selectively blocks cullin 3 neddylation

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12 December 2020

High-Affinity Peptidomimetic Inhibitors of the DCN1-UBC12 Protein-Protein Interaction.

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12 December 2020

Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation

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12 December 2020

10.1021/ACS.JMEDCHEM.7B01282

Identifiers

DOI

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20 March 2020

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20 March 2020

PubMed publication ID

29547693

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