Literature DB >> 31528694

MLN4924: additional activities beyond neddylation inhibition.

Qiyin Zhou1,2, Yi Sun1,3.   

Abstract

MLN4924, a small molecular inhibitor of NEDD8 (neuronal precursor cell-expressed developmentally downregulated protein 8) activating enzyme (NAE), blocks cullin neddylation to inactivate cullin-RING ligase. We found that MLN4924 has additional activities: it triggers EGFR dimerization and activation of RAS/MAPK and PI3K/AKT1 signals to stimulate tumor sphere formation and inhibit ciliogenesis; and it triggers PKM2 tetramerization to promote glycolysis.

Entities:  

Keywords:  AKT1; EGFR; Neddylation; PKM2; ciliogenesis; dimerization; glycolysis; tetramerization; tumor-sphere

Year:  2019        PMID： 31528694      PMCID： PMC6736204          DOI： 10.1080/23723556.2019.1618174

Source DB:  PubMed          Journal:  Mol Cell Oncol        ISSN： 2372-3556


  10 in total

1.  Blockage of neddylation modification stimulates tumor sphere formation in vitro and stem cell differentiation and wound healing in vivo.

Authors:  Xiaochen Zhou; Mingjia Tan; Mukesh K Nyati; Yongchao Zhao; Gongxian Wang; Yi Sun
Journal:  Proc Natl Acad Sci U S A       Date:  2016-05-09       Impact factor: 11.205

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

Authors:  James E Brownell; Michael D Sintchak; James M Gavin; Hua Liao; Frank J Bruzzese; Nancy J Bump; Teresa A Soucy; Michael A Milhollen; Xiaofeng Yang; Anne L Burkhardt; Jingya Ma; Huay-Keng Loke; Trupti Lingaraj; Dongyun Wu; Kristin B Hamman; James J Spelman; Courtney A Cullis; Steven P Langston; Stepan Vyskocil; Todd B Sells; William D Mallender; Irache Visiers; Ping Li; Christopher F Claiborne; Mark Rolfe; Joseph B Bolen; Lawrence R Dick
Journal:  Mol Cell       Date:  2010-01-15       Impact factor: 17.970

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

Authors:  Teresa A Soucy; Peter G Smith; Michael A Milhollen; Allison J Berger; James M Gavin; Sharmila Adhikari; James E Brownell; Kristine E Burke; David P Cardin; Stephen Critchley; Courtney A Cullis; Amanda Doucette; James J Garnsey; Jeffrey L Gaulin; Rachel E Gershman; Anna R Lublinsky; Alice McDonald; Hirotake Mizutani; Usha Narayanan; Edward J Olhava; Stephane Peluso; Mansoureh Rezaei; Michael D Sintchak; Tina Talreja; Michael P Thomas; Tary Traore; Stepan Vyskocil; Gabriel S Weatherhead; Jie Yu; Julie Zhang; Lawrence R Dick; Christopher F Claiborne; Mark Rolfe; Joseph B Bolen; Steven P Langston
Journal:  Nature       Date:  2009-04-09       Impact factor: 49.962

Review 4.  Protein neddylation and its alterations in human cancers for targeted therapy.

Authors:  Lisha Zhou; Wenjuan Zhang; Yi Sun; Lijun Jia
Journal:  Cell Signal       Date:  2018-01-10       Impact factor: 4.315

5.  SAICAR stimulates pyruvate kinase isoform M2 and promotes cancer cell survival in glucose-limited conditions.

Authors:  Kirstie E Keller; Irene S Tan; Young-Sam Lee
Journal:  Science       Date:  2012-10-18       Impact factor: 47.728

6.  Inhibiting neddylation modification alters mitochondrial morphology and reprograms energy metabolism in cancer cells.

Authors:  Qiyin Zhou; Hua Li; Yuanyuan Li; Mingjia Tan; Shaohua Fan; Cong Cao; Feilong Meng; Ling Zhu; Lili Zhao; Min-Xin Guan; Hongchuan Jin; Yi Sun
Journal:  JCI Insight       Date:  2019-02-21

Review 7.  Protein neddylation: beyond cullin-RING ligases.

Authors:  Radoslav I Enchev; Brenda A Schulman; Matthias Peter
Journal:  Nat Rev Mol Cell Biol       Date:  2015-01       Impact factor: 94.444

8.  Primary Cilia Mediate Diverse Kinase Inhibitor Resistance Mechanisms in Cancer.

Authors:  Andrew D Jenks; Simon Vyse; Jocelyn P Wong; Eleftherios Kostaras; Deborah Keller; Thomas Burgoyne; Amelia Shoemark; Athanasios Tsalikis; Maike de la Roche; Martin Michaelis; Jindrich Cinatl; Paul H Huang; Barbara E Tanos
Journal:  Cell Rep       Date:  2018-06-05       Impact factor: 9.423

Review 9.  Neddylation: a novel modulator of the tumor microenvironment.

Authors:  Lisha Zhou; Yanyu Jiang; Qin Luo; Lihui Li; Lijun Jia
Journal:  Mol Cancer       Date:  2019-04-03       Impact factor: 27.401

10.  Neddylation inhibitor MLN4924 suppresses cilia formation by modulating AKT1.

Authors:  Hongmei Mao; Zaiming Tang; Hua Li; Bo Sun; Mingjia Tan; Shaohua Fan; Yuan Zhu; Yi Sun
Journal:  Protein Cell       Date:  2019-03-09       Impact factor: 14.870
  10 in total
  8 in total

1.  Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells.

Authors:  Xian Wang; Yi Sun; Qiyin Zhou; Wenyu Lin; Chaoqun Wang; Fei Sun; Siwei Ju; Qian Chen; Yi Wang; Yongxia Chen; Haomin Li; Linbo Wang; Zeping Hu; Hongchuan Jin
Journal:  Nat Commun       Date:  2022-05-31       Impact factor: 17.694

2.  Decreased KLHL3 expression is involved in the activation of WNK-OSR1/SPAK-NCC cascade in type 1 diabetic mice.

Authors:  Qin Guo; Ya Zhang; Geng-Ru Jiang; Chong Zhang
Journal:  Pflugers Arch       Date:  2021-01-11       Impact factor: 3.657

3.  Overexpressed NEDD8 as a potential therapeutic target in esophageal squamous cell carcinoma.

Authors:  Jingrong Xian; Shiwen Wang; Yanyu Jiang; Lihui Li; Lili Cai; Ping Chen; Yue Liu; Xiaofei Zeng; Guoan Chen; Chen Ding; Robert M Hoffman; Lijun Jia; Hu Zhao; Yanmei Zhang
Journal:  Cancer Biol Med       Date:  2021-03-18       Impact factor: 5.347

Review 4.  Neddylation regulation of mitochondrial structure and functions.

Authors:  Qiyin Zhou; Yawen Zheng; Yi Sun
Journal:  Cell Biosci       Date:  2021-03-17       Impact factor: 7.133

5.  The Effect of Neddylation Inhibition on Inflammation-Induced MMP9 Gene Expression in Esophageal Squamous Cell Carcinoma.

Authors:  Anita Hryniewicz-Jankowska; Jaroslaw Wierzbicki; Renata Tabola; Kamilla Stach; Khalid Sossey-Alaoui; Katarzyna Augoff
Journal:  Int J Mol Sci       Date:  2021-02-09       Impact factor: 5.923

6.  Celecoxib Synergistically Enhances MLN4924-Induced Cytotoxicity and EMT Inhibition Via AKT and ERK Pathways in Human Urothelial Carcinoma.

Authors:  Shida Xiong; Wei Huang; Xiaoqiang Liu; Qian Chen; Yi Ding; Haoxuan Huang; Ru Zhang; Ju Guo
Journal:  Cell Transplant       Date:  2022 Jan-Dec       Impact factor: 4.064

7.  Astaxanthin Inhibits Oxidative Stress-Induced Ku Protein Degradation and Apoptosis in Gastric Epithelial Cells.

Authors:  Jaeeun Lee; Joo Weon Lim; Hyeyoung Kim
Journal:  Nutrients       Date:  2022-09-22       Impact factor: 6.706

Review 8.  [Targeting Cullin-RING E3 ligases for anti-cancer therapy: efforts on drug discovery].

Authors:  Qing Yu; Xiufang Xiong; Yi Sun
Journal:  Zhejiang Da Xue Xue Bao Yi Xue Ban       Date:  2020-05-25
  8 in total

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