Pevonedistat (MLN4924) is a selective NEDD8 inhibitor. [1] It is being investigated as a cancer treatment, e.g. for mantle cell lymphoma (MCL). [1]

2017年7月17日 · 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 that MLN4924...

2020年7月21日 · Pevonedistat (MLN4924), a selective inhibitor of the NEDD8-activating enzyme E1 regulatory subunit (NAE1), has demonstrated significant therapeutic potential in several malignancies.

2010年9月2日 · 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 rereplication, resulting in DNA damage and cell death.

2008年11月16日 · MLN4924 specifically inhibits Nedd8-cullin formation leading to increased steady state levels of direct CDL substrates by preventing their ubiquitination and degradation through the proteasome. Many of these CDL substrates are involved in cell cycle progression.

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 established that significant therapeutic benefit can be achieved …

2017年7月17日 · 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 cancer cells. In this study, we investigated the anti-tumor effect of MLN4924 in human clear cell renal carcinoma (ccRCC).

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 protein and cullin-RING ligases (CRL).

2020年1月20日 · Here, we show that the NAE inhibitor, Pevonedistat (MLN4924), potently inhibits RB1null and MYCNamp tumors. Intravitreal MLN4924 suppressed multiple human xenografts with EC80s from 20 ng to...