ArticleDrug design, development and therapy2018
Identification of new inhibitors of Mdm2-p53 interaction via pharmacophore and structure-based virtual screening.
Article in Drug design, development and therapy, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Targeting p53-MDM2 pathway with novel triazole-oxazole hybrids: a fragment-based drug discovery approach for next-generation cancer therapies.Molecular diversity · 2026Article
- Target-Based Small Molecule Drug Discovery for Colorectal Cancer: A Review of Molecular Pathways and In Silico Studies.Biomolecules · 2022Review
- Predominance of Antioxidants in Some Edible Plant Oils in Ameliorating Oxidative Stress and Testicular Toxicity Induced by Malathion.Life (Basel, Switzerland) · 2022Article
- Morindone from Morinda citrifolia as a potential antiproliferative agent against colorectal cancer cell lines.PloS one · 2022Article
- Interaction of (+)-Strebloside and Its Derivatives with NaMolecules (Basel, Switzerland) · 2021Article
- Ubiquitination Regulators Discovered by Virtual Screening for the Treatment of Cancer.Frontiers in cell and developmental biology · 2021Review
- 7-Chloroquinoline-1,2,3-triazoyl carboxamides induce cell cycle arrest and apoptosis in human bladder carcinoma cells.Investigational new drugs · 2020Article
- MDM2 and MDMX promote ferroptosis by PPARα-mediated lipid remodeling.Genes & development · 2020Article
- Mimicking Strategy for Protein-Protein Interaction Inhibitor Discovery by Virtual Screening.Molecules (Basel, Switzerland) · 2019Review
- Discovery of new butyrylcholinesterase inhibitors via structure-based virtual screening.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Investigation of the In-Vivo Cytotoxicity and the In Silico-Prediction of MDM2-p53 Inhibitor Potential ofToxins · 2019Article
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Authors and funding
5 authors.
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Abstract
backgroundThe tumor suppressor protein p53 plays an important role in preventing tumor formation and progression through its involvement in cell division control and initiation of apoptosis. Mdm2 protein controls the activity of p53 protein through working as ubiquitin E3 ligase promoting p53 degradation through the proteasome degradation pathway. Inhibitors for Mdm2-p53 interaction have restored the activity of p53 protein and induced cancer fighting properties in the cell. PURPOSE: The objective of this study is to use computer-aided drug discovery techniques to search for new Mdm2-p53 interaction inhibitors.
methodsA set of pharmacophoric features were created based on a standard Mdm2 inhibitor and this was used to screen a commercial drug-like ligand library; then potential inhibitors were docked and ranked in a multi-step protocol using GLIDE. Top ranked ligands from docking were evaluated for their inhibition activity of Mdm2-p53 interaction using ELISA testing.
resultsSeveral compounds showed inhibition activity at the submicromolar level, which is comparable to the standard inhibitor Nutlin-3a. Furthermore, the discovered inhibitors were evaluated for their anticancer activities against different breast cancer cell lines, and they showed an interesting inhibition pattern.
conclusionThe reported inhibitors can represent a starting point for further SAR studies in the future and can help in the discovery of new anticancer agents.
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