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
NEDDylation, a post-translational modification through three-step enzymatic cascades,
plays crucial roles in the regulation of diverse biological processes. NEDD8-activating …

[HTML][HTML] Targeting cullin neddylation for cancer and fibrotic diseases

ZX He, W Yang, D Zengyangzong, G Gao, Q Zhang… - Theranostics, 2023 - ncbi.nlm.nih.gov
Protein neddylation is a post-translational modification, and its best recognized substrates
are cullin family proteins, which are the core component of Cullin-RING ligases (CRLs) …

A small molecule inhibitor of the UBE2F-CRL5 axis induces apoptosis and radiosensitization in lung cancer

T Xu, Q Ma, Y Li, Q Yu, P Pan, Y Zheng, Z Li… - … and Targeted Therapy, 2022 - nature.com
Protein neddylation is catalyzed by a neddylation activating enzyme (NAE, E1), an E2
conjugating enzyme, and an E3 ligase. In various types of human cancers, the neddylation …

Protein neddylation and its role in health and diseases

S Zhang, Q Yu, Z Li, Y Zhao, Y Sun - Signal Transduction and Targeted …, 2024 - nature.com
NEDD8 (Neural precursor cell expressed developmentally downregulated protein 8) is an
ubiquitin-like protein that is covalently attached to a lysine residue of a protein substrate …

Precision oncology with drugs targeting the replication stress, ATR, and Schlafen 11

U Jo, Y Murai, N Takebe, A Thomas, Y Pommier - Cancers, 2021 - mdpi.com
Simple Summary Chemotherapeutic DNA-damaging agents targeting replication are widely
used but predictive rationales for drug combinations and patient selection still need clinical …

[HTML][HTML] Discovery of small molecule inhibitors of neddylation catalyzing enzymes for anticancer therapy

X Qin, X Han, Y Sun - Biomedicine & Pharmacotherapy, 2024 - Elsevier
Protein neddylation, a type of post-translational modifications, involves the transfer of the
ubiquitin-like protein NEDD8 to the lysine residues of a target substrate, which is catalyzed …

The NF-κB pharmacopeia: Novel strategies to subdue an intractable target

D Verzella, J Cornice, P Arboretto, D Vecchiotti… - Biomedicines, 2022 - mdpi.com
NF-κB transcription factors are major drivers of tumor initiation and progression. NF-κB
signaling is constitutively activated by genetic alterations or environmental signals in many …

Loss of NEDD8 in cancer cells causes vulnerability to immune checkpoint blockade in triple-negative breast cancer

I Papakyriacou, G Kutkaite, M Rúbies Bedós… - Nature …, 2024 - nature.com
Immune checkpoint blockade therapy aims to activate the immune system to eliminate
cancer cells. However, clinical benefits are only recorded in a subset of patients. Here, we …

[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
Inhibition of the NEDD8-activating enzyme (NAE), the key E1 enzyme in the neddylation
cascade, has been considered an attractive anticancer strategy with the discovery of the first …

Diabetic sensory neuropathy and insulin resistance are induced by loss of UCHL1 in Drosophila

D Lee, E Yoon, SJ Ham, K Lee, H Jang, D Woo… - Nature …, 2024 - nature.com
Diabetic sensory neuropathy (DSN) is one of the most common complications of type 2
diabetes (T2D), however the molecular mechanistic association between T2D and DSN …