A structure-based virtual screening identifies a novel MDM2 antagonist in the activation of the p53 signaling and inhibition of tumor growth

Vogelstein B, Lane D, Levine AJ. Surfing the p53 network. Nature. 2000;408:307–10.

Article  PubMed  CAS  Google Scholar 

Williams AB, Schumacher B. p53 in the DNA-damage-repair process. Cold Spring Harb Perspect Med. 2016;6:a026070.

Article  PubMed  PubMed Central  Google Scholar 

Kastenhuber ER, Lowe SW. Putting p53 in context. Cell. 2017;170:1062–78.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Momand J, Zambetti GP, Olson DC, George D, Levine AJ. The mdm-2 oncogene product forms a complex with the p53 protein and inhibits p53-mediated transactivation. Cell. 1992;69:1237–45.

Article  PubMed  CAS  Google Scholar 

Honda R, Tanaka H, Yasuda H. Oncoprotein MDM2 is a ubiquitin ligase E3 for tumor suppressor p53. FEBS Lett. 1997;420:25–7.

Article  PubMed  CAS  Google Scholar 

Haupt Y, Maya R, Kazaz A, Oren M. Mdm2 promotes the rapid degradation of p53. Nature. 1997;387:296–9.

Article  PubMed  CAS  Google Scholar 

Fakharzadeh SS, Rosenblum-Vos L, Murphy M, Hoffman EK, George DL. Structure and organization of amplified DNA on double minutes containing the mdm2 oncogene. Genomics. 1993;15:283–90.

Article  PubMed  CAS  Google Scholar 

Giacomelli AO, Yang X, Lintner RE, McFarland JM, Duby M, Kim J, et al. Mutational processes shape the landscape of TP53 mutations in human cancer. Nat Genet. 2018;50:1381–7.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Silva JL, Cino EA, Soares IN, Ferreira VF. G APdO. Targeting the prion-like aggregation of mutant p53 to combat cancer. Acc Chem Res. 2018;51:181–90.

Article  PubMed  CAS  Google Scholar 

Beroukhim R, Mermel CH, Porter D, Wei G, Raychaudhuri S, Donovan J, et al. The landscape of somatic copy-number alteration across human cancers. Nature. 2010;463:899–905.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Kussie PH, Gorina S, Marechal V, Elenbaas B, Moreau J, Levine AJ, et al. Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain. Science. 1996;274:948–53.

Article  PubMed  CAS  Google Scholar 

Popowicz GM, Domling A, Holak TA. The structure-based design of Mdm2/Mdmx-p53 inhibitors gets serious. Angew Chem Int Ed Engl. 2011;50:2680–8.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Daniele S, Barresi E, Zappelli E, Marinelli L, Novellino E, Da Settimo F, et al. Long lasting MDM2/Translocator protein modulator: a new strategy for irreversible apoptosis of human glioblastoma cells. Oncotarget. 2016;7:7866–84.

Article  PubMed  PubMed Central  Google Scholar 

Vassilev LT, Vu BT, Graves B, Carvajal D, Podlaski F, Filipovic Z, et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 2004;303:844–8.

Article  PubMed  CAS  Google Scholar 

Ding K, Lu Y, Nikolovska-Coleska Z, Qiu S, Ding Y, Gao W, et al. Structure-based design of potent non-peptide MDM2 inhibitors. J Am Chem Soc. 2005;127:10130–1.

Article  PubMed  CAS  Google Scholar 

Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013;56:5979–83.

Article  PubMed  CAS  Google Scholar 

Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, et al. Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. J Med Chem. 2014;57:1454–72.

Article  PubMed  CAS  Google Scholar 

Bill KL, Garnett J, Meaux I, Ma X, Creighton CJ, Bolshakov S, et al. SAR405838: a novel and potent inhibitor of the MDM2:p53 axis for the treatment of dedifferentiated liposarcoma. Clin Cancer Res. 2016;22:1150–60.

Article  PubMed  CAS  Google Scholar 

Yang X, Liu Y, Gan J, Xiao ZX, Cao Y. FitDock: protein-ligand docking by template fitting. Brief Bioinform. 2022;23:bbac087.

Article  PubMed  Google Scholar 

Allen JG, Bourbeau MP, Wohlhieter GE, Bartberger MD, Michelsen K, Hungate R, et al. Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction. J Med Chem. 2009;52:7044–53.

Article  PubMed  CAS  Google Scholar 

Anil B, Riedinger C, Endicott JA, Noble ME. The structure of an MDM2-Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant. Acta Crystallogr D Biol Crystallogr. 2013;69:1358–66.

Article  PubMed  CAS  Google Scholar 

Tovar C, Graves B, Packman K, Filipovic Z, Higgins B, Xia M, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013;73:2587–97.

Article  PubMed  CAS  Google Scholar 

Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, et al. The protein data bank. Nucleic Acids Res. 2000;28:235–42.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Trott O, Olson AJ. AutoDock Vina: improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading. J Comput Chem. 2010;31:455–61.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Cao Y, Li L. Improved protein-ligand binding affinity prediction by using a curvature-dependent surface-area model. Bioinformatics. 2014;30:1674–80.

Article  PubMed  CAS  Google Scholar 

Zhang H, Hu L, Qiu W, Deng T, Zhang Y, Bergholz J, et al. MDMX exerts its oncogenic activity via suppression of retinoblastoma protein. Oncogene. 2015;34:5560–9.

Article  PubMed  CAS  Google Scholar 

Arkin MR, Tang Y, Wells JA. Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. Chem Biol. 2014;21:1102–14.

Article  PubMed  PubMed Central  CAS  Google Scholar 

O’Boyle NM, Banck M, James CA, Morley C, Vandermeersch T, Hutchison GR. Open Babel: an open chemical toolbox. J Cheminform. 2011;3:33.

Article  PubMed  PubMed Central  Google Scholar 

Vitre BD, Cleveland DW. Centrosomes, chromosome instability (CIN) and aneuploidy. Curr Opin Cell Biol. 2012;24:809–15.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Wade M, Wang YV, Wahl GM. The p53 orchestra: Mdm2 and Mdmx set the tone. Trends Cell Biol. 2010;20:299–309.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Vassilev LT. MDM2 inhibitors for cancer therapy. Trends Mol Med. 2007;13:23–31.

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