Targeting NEDD8-activating enzyme for cancer therapy: developments, clinical trials, challenges and future research directions

DJ Fu, T Wang - Journal of Hematology & Oncology, 2023 - Springer
… Approach (3) is the discovery of novel NAE inhibitors … , and MLN4924 as a selective NAE
inhibitor exhibits anticancer … NAE inhibitor with broad-spectrum antitumor activity against a …

Nedd8-activating enzyme inhibitor MLN4924 (Pevonedistat), inhibits miR-1303 to suppress human breast cancer cell proliferation via targeting p27Kip1

Y Chen, M Du, S Yusuying, W Liu, Y Tan… - Experimental Cell …, 2020 - Elsevier
… 4j showed that MLN4924 enhanced the luciferase activity of … and targets to strengthen the
anti-cancer effect of MLN4924. … of MLN4924 combined with miR-1303 as a novel targeted …

[HTML][HTML] SOMCL-19-133, a novel, selective, and orally available inhibitor of NEDD8-activating enzyme (NAE) for cancer therapy

LN Zhou, C Xiong, YJ Cheng, SS Song, XB Bao… - Neoplasia, 2022 - Elsevier
… with improved anti-tumor potency than MLN4924. … with MLN4924, SOMCL-19-133 has
enhanced antitumor activity … -19-133 demonstrated substantial antitumor activity in the preclinical …

[HTML][HTML] The NEDD8 activating enzyme inhibitor MLN4924 mitigates doxorubicin-induced cardiotoxicity in mice

KH Chen, JM Sun, L Lin, JW Liu, XY Liu… - Free Radical Biology …, 2024 - Elsevier
… , MLN4924 exhibited a remarkable capacity to enhance cardiac contractile function and bolster
survival rates in mice. These cardioprotective effects of MLN4924 were … This novel finding …

NEDD8-activating enzyme inhibitor MLN4924 inhibits both the tumor stroma and angiogenesis in pancreatic cancer via Gli1 and REDD1

W Mao, L Zhang, Y Rong, T Kuang, D Wang… - Digestive Diseases and …, 2023 - Springer
inhibitor that exhibits anti-tumor activities toward pancreatic … that MLN4924 could have, we
ask what impact MLN4924 would … increases the understanding of the multi-facets of the effect

The Double-Edged Effects of MLN4924: Rethinking Anti-Cancer Drugs Targeting the Neddylation Pathway

H Tang, X Pang, S Li, L Tang - Biomolecules, 2024 - mdpi.com
… This means that the anti-cancer activity of MLN4924 can be … by the NEDD8-activating enzyme
inhibitor MLN4924 triggers … as novel non-sulfamide NEDD8 activating enzyme inhibitors

Development of potent NEDD8-activating enzyme inhibitors bearing a pyrimidotriazole scaffold

C Xiong, L Zhou, J Tan, S Song, X Bao… - Journal of Medicinal …, 2021 - ACS Publications
… clinical NAE inhibitor, pevonedistat (compound 1, MLN4924)… NAE inhibitor 26, we further
evaluated its antitumor activity in … found to inhibit the neddylation pathway and increase CRL …

Targeting protein neddylation for cancer therapy

L Zhou, L Jia - Cullin-RING Ligases and Protein Neddylation: Biology …, 2020 - Springer
… of the NEDD8-activating enzyme (NAE) inhibitor MLN4924 (also … inhibitor, significantly
enhances the anticancer effect of … of neddylation inhibitors (eg, MLN4924) as a novel class of anti-…

Advances in cancer treatment by targeting the neddylation pathway

W Gai, Z Peng, CH Liu, L Zhang… - Frontiers in Cell and …, 2021 - frontiersin.org
… , and MLN4924, which inhibits NEDD8-activating enzyme (… be a novel anti-cancer mechanism
for MLN4924 in cancer … shown the impressive antitumor activity of MLN4924, but single…

Effective targeting of the ubiquitin-like modifier NEDD8 for lung adenocarcinoma treatment

Y Jiang, W Cheng, L Li, L Zhou, Y Liang… - Cell Biology and …, 2020 - Springer
… showed MLN4924, an inhibitor of NEDD8 activating enzyme (E1)… new anticancer targets
and developing novel therapeutic … activated by an E1 enzyme (NEDD8 activating enzyme, NAE)…