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]

Nutlins are cis-imidazoline analogs that inhibit the interaction between MDM2 and tumor suppressor p53. Nutlin-3 is the compound that is most commonly used in anti-cancer studies in nutlins [110]. Nutlin-3 induces ER/mitochondria stress and contributed to paraptosis.

Jun 29, 2010 · One drug that targets the p53-binding pocket of MDM2 and thus acts to inhibit p53/MDM2 interaction is Nutlin-3, developed by Roche (Nutley, NJ, USA) (Vassilev, 2004; Vassilev et al, 2004;...

Mar 11, 2011 · Nutlin-3a is a small molecule that activates the p53 pathway by disrupting p53–MDM2 interaction. We show that nutlin-3a activates p53 in DLBCL cells associated with t (14;18) (q32;q21), BCL2...

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.

Nutlins are a class of highly substituted 2-imidazolines that block the binding of the p53 tumor suppressing gene and a protein called MDM2, thereby showing potential as anti-cancer therapies. You might find these chapters and articles relevant to this topic. K. Samanta, ... C. Schmuck, in Comprehensive Supramolecular Chemistry II, 2017.

MDM2 (mouse double minute 2) inhibitors that activate p53 and induce apoptosis in a non-genotoxic manner are in clinical development for treatment of leukemias. P53 can modulate other programmed cell death pathways including autophagy both transcriptionally and non-transcriptionally.

Nutlin-3, a small molecule inhibitor that specifi-cally 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 pro-ducing minimal cytotoxicity and side effects.

Induces the transcription of long intergenic non-coding RNA p21 (lincRNA-p21) and lincRNA-Mkln1.

Nutlin-3a (Nutlin) is a preclinical drug that binds MDM2 and prevents the interaction between MDM2 and p53, leading to p53 stabilization and activation of p53 signaling events. Previous studies have reported that Nutlin promotes growth arrest and/or apoptosis in cancer cells that express wild-type p53.