Nutlins are cis-imidazoline analogs which inhibit the interaction between mdm2 and tumor suppressor p53, and which were discovered by screening a chemical library by Vassilev et al. Nutlin-1, nutlin-2, and nutlin-3 were all identified in the same screen; [1] however, Nutlin-3 is the compound most commonly used in anti-cancer studies. [2]

Nutlin-3 is a potent and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-clinical studies. This review will highlight recent advances in the development of small-molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on …

Jun 29, 2010 · Nutlin-3 is a small-molecule inhibitor that binds preferentially to the p53-binding pocket of MDM2, leading to stabilisation of p53 and activation of the p53 pathway.

Mar 19, 2013 · Induction of cellular senescence through activation of the p53 tumor suppressor protein is a new option for treating proliferative disorders. Nutlins prevent the ubiquitin ligase MDM2 (murine double minute 2), a negative p53 regulator, from interacting with p53.

Treatment with nutlin-3 results in a rapid accumulation of p53 protein, within 1–2 h of treatment, and in a robust induction of p53 target gene expression in neuroblastoma cells with wild-type p53, regardless of their differentiation status [50,51].

Oct 17, 2013 · Nutlin-3 is a potent enhancer of D269H/E195R-induced apoptosis in wild-type p53-expressing cancer cells. Addition of DNA-damaging agents such as cisplatin further...

Oct 11, 2022 · Nutlin-3 DrugBank Accession Number DB17039 Background. Nutlin-3 is a small molecule inhibitor that targets p53-Mdm2 interaction. 1. Type Small Molecule Groups Experimental Structure

Nutlin-3 is a small molecule inhibitor of the MDM2/p53 interaction, which leads to the non-genotoxic p53 stabilization, activation of cell cycle arrest and apoptosis pathways. A series of recent studies have strengthened the concept that selective, non-genotoxic p53 activation by Nutlin-3 might repr …

Nutlin-3, a small molecule inhibitor that specifically targets p53-Mdm2 interaction offers new therapeutic opportunities by enhancing cancer cell growth arrest and apoptosis through the restoration of the p53-mediated tumor suppression pathway while producing minimal cytotoxicity and side effects.

Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10 μM) stabilizes p53 and p21 WAF levels and is toxic to WTp53-22RV1 cells (IC 50, 4.3 μM) but has minimal toxicity toward p53-deficient cells (IC 50, >10 μM).