ArticleInvestigational new drugs2017
Targeting the protein ubiquitination machinery in melanoma by the NEDD8-activating enzyme inhibitor pevonedistat (MLN4924).
Article in Investigational new drugs, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 21 citations in OpenAlex.
- HIV proviral transcription and infectivity are enhanced by neddylation.Journal of virology · 2025Article
- Pevonedistat, a first-in-class NEDD8-activating enzyme inhibitor, sensitizes cancer cells to VSVΔ51 oncolytic virotherapy.Molecular therapy : the journal of the American Society of Gene Therapy · 2023Article
- Article
- Targeting cullin neddylation for cancer and fibrotic diseases.Theranostics · 2023Review
- A new ferroptosis-related genetic mutation risk model predicts the prognosis of skin cutaneous melanoma.Frontiers in genetics · 2022Article
- Article
- Pevonedistat targeted therapy inhibits canine melanoma cell growth through induction of DNA re-replication and senescence.Veterinary and comparative oncology · 2020Article
- MiRNA-494 enhances M1 macrophage polarization via Nrdp1 in ICH mice model.Journal of inflammation (London, England) · 2020Article
- A patent review of the ubiquitin ligase system: 2015-2018.Expert opinion on therapeutic patents · 2018Review
- Analysis of MLN4924 (pevonedistat) as a potential therapeutic agent in malignant melanoma.Melanoma research · 2018Article
- Ceritinib Enhances the Efficacy of Trametinib inMolecular cancer therapeutics · 2018Article
- Ubiquitination in melanoma pathogenesis and treatment.Cancer medicine · 2017Review
- Whole-exome sequencing identifies recurrent SF3B1 R625 mutation and comutation of NF1 and KIT in mucosal melanoma.Melanoma research · 2017Article
- Systemic inhibition of neddylation by 3-day MLN4924 treatment regime does not impair autophagic flux in mouse hearts and brains.American journal of cardiovascular disease · 2017Article
Corrections and comments
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Authors and funding
14 authors at 4 institutions in 2 countries.
Funding
Abstract
Background The neddylation pathway conjugates NEDD8 to cullin-RING ligases and controls the proteasomal degradation of specific proteins involved in essential cell processes. Pevonedistat (MLN4924) is a selective small molecule targeting the NEDD8-activating enzyme (NAE) and inhibits an early step in neddylation, resulting in DNA re-replication, cell cycle arrest and death. We investigated the anti-tumor potential of pevonedistat in preclinical models of melanoma. Methods Melanoma cell lines and patient-derived tumor xenografts (PDTX) treated with pevonedistat were assessed for viability/apoptosis and tumor growth, respectively, to identify sensitive/resistant models. Gene expression microarray and gene set enrichment analyses were performed in cell lines to determine the expression profiles and pathways of sensitivity/resistance. Pharmacodynamic changes in treated-PDTX were also characterized. Results Pevonedistat effectively inhibited cell viability (IC
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