Jul 17, 2017 · MLN4924 is a neddylation inhibitor currently under investigation in multiple phase I studies on various malignancies, and its clincal name is Pevonedistat. It has been documented …

Jul 21, 2020 · Pevonedistat (MLN4924), a selective inhibitor of the NEDD8-activating enzyme E1 regulatory subunit (NAE1), has demonstrated significant therapeutic potential in several …

Sep 2, 2010 · MLN4924 is a potent and selective small molecule NEDD8-activating enzyme (NAE) inhibitor. In most cancer cells tested, inhibition of NAE leads to induction of DNA …

Pevonedistat (MLN4924) is a potent inhibitor of NAE, and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC 50 =1.5, 8.2, 1.8 and >10 μM, respectively) …

Nov 16, 2008 · MLN4924 specifically inhibits Nedd8-cullin formation leading to increased steady state levels of direct CDL substrates by preventing their ubiquitination and degradation through …

Jan 20, 2020 · Here, we show that the NAE inhibitor, Pevonedistat (MLN4924), potently inhibits RB1null and MYCNamp tumors. Intravitreal MLN4924 suppressed multiple human xenografts …

MLN4924 is a first-in-class inhibitor of the proximal regulator of the NEDD8 system (NEDD8-activating enzyme, NAE) that has entered Phase-I trials for cancer therapy and has …

Jul 17, 2017 · It has been documented that MLN4924 blocks Cullins neddylation and inactivates CRLs and, in turn, triggers cell-cycle arrest, apoptosis, senescence and autophagy in many …

MLN4924 (Pevonedistat) is a potent and selective inhibitor of NEDD8-activating enzyme (NAE) (1). The NAE is part of the NEDD8 conjugation pathway that involves the ubiquitin-like NEDD8 …