E1 Activating

Neddylation is essential for β-catenin degradation in Wnt signaling pathway

105 views | Apr 10 2022

Bojun Wang et al. highlighted the importance of reassessing previously identified ubiquitylation substrates. [Read the Full Post]

GRP78 blockade overcomes intrinsic resistance to UBA1 inhibitor TAK-243 in glioblastoma

106 views | Apr 10 2022

Xu Zhang et al. provided a new strategy for improving the sensitivity of GBM to TAK-243 treatment and experimental basis for further clinical trials to evaluate this combination therapy. [Read the Full Post]

Blocking neddylation elicits antiviral effect against hepatitis B virus replication

144 views | Nov 23 2021

Karima Abounouh et al. provided new tools interfering with HBV persistence as well as novel therapeutic strategies against chronic hepatitis B. [Read the Full Post]

Pevonedistat attenuates cisplatin-induced nephrotoxicity in mice by downregulating the release of inflammatory mediators

219 views | Sep 22 2021

Yousra M El-Far et al. found that pevonedistat alleviated CIS-induced nephrotoxicity that might be attributed to suppression of the inflammation induced in renal tissue. [Read the Full Post]

Direct Conjugation of NEDD8 to the N-Terminus of a Model Protein Can Induce Degradation

414 views | May 03 2021

Kartikeya Vijayasimha et al. suggested that under certain conditions, such as the model system described here, the covalent linkage of NEDD8 to a protein substrate might result in the target proteins degradation. [Read the Full Post]

SLFN11 inactivation induces proteotoxic stress and sensitizes cancer cells to ubiquitin activating enzyme inhibitor TAK-243

401 views | May 01 2021

Yasuhisa Murai et al. found that findings uncover a previously unknown function of SLFN11 as a regulator of protein quality control and attenuator of ER stress and UPR. Moreover, they suggest the potential value of TAK-243 in SLFN11-deficient tumors. [Read the Full Post]

Neddylation inhibitor MLN4924 has anti-HBV activity via modulating the ERK-HNF1α-C/EBPα-HNF4α axis

261 views | Dec 05 2020

Mingjie Xie et al. revealed that neddylation inhibitor MLN4924 had impressive anti-HBV activity by inhibiting HBV replication, thus providing sound rationale for future MLN4924 clinical trial as a novel anti-HBV therapy. [Read the Full Post]

Pevonedistat (MLN4924): mechanism of cell death induction and therapeutic potential in colorectal cancer

244 views | Sep 15 2020

Jennifer Ferris et al. suggested that this second-generation proteostasis-disrupting agent might have its most widespread activity in CRC, in combination with irinotecan-containing treatment regimens. [Read the Full Post]

Blocking PD1/PDL1 Interactions Together With MLN4924 Therapy Is a Potential Strategy for Glioma Treatment

332 views | Feb 26 2020

Natalia Filippova et al. concluded that i) PDL1 up-regulation in gliomas and the glioma microenvironment is an important chemotherapeutic target; ii) MLN4924 therapy, combined with a blockage of the PD1/PDL1 pathway, should be considered as a potential strategy for glioma treatment. [Read the Full Post]

Pevonedistat (MLN4924), a First-in-Class NEDD8-activating enzyme inhibitor, in patients with acute myeloid leukaemia and myelodysplastic syndromes: a phase 1 study

0 views | Dec 28 2019

Swords RT et al. indicated that administration of the first-in-class agent, pevonedistat, was feasible in patients with MDS and AML and modest clinical activity was observed. [Read the Full Post]