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Therapeutic implications of p53 status on cancer cell fate following exposure to ionizing radiation and the DNA-PK inhibitor M3814.

Sun Q, Guo Y, Liu X, Czauderna F, Carr MI, Zenke FT, Blaukat A, Vassilev LT.

Mol Cancer Res. 2019 Sep 24. pii: molcanres.0362.2019. doi: 10.1158/1541-7786.MCR-19-0362. [Epub ahead of print]


Therapeutic Response to Non-genotoxic Activation of p53 by Nutlin3a Is Driven by PUMA-Mediated Apoptosis in Lymphoma Cells.

Valente LJ, Aubrey BJ, Herold MJ, Kelly GL, Happo L, Scott CL, Newbold A, Johnstone RW, Huang DC, Vassilev LT, Strasser A.

Cell Rep. 2016 Mar 1;14(8):1858-66. doi: 10.1016/j.celrep.2016.01.059. Epub 2016 Feb 18.


Constitutive autophagy contributes to resistance to TP53-mediated apoptosis in Epstein-Barr virus-positive latency III B-cell lymphoproliferations.

Pujals A, Favre L, Pioche-Durieu C, Robert A, Meurice G, Le Gentil M, Chelouah S, Martin-Garcia N, Le Cam E, Guettier C, Raphaël M, Vassilev LT, Gaulard P, Codogno P, Lipinski M, Wiels J.

Autophagy. 2015;11(12):2275-87. doi: 10.1080/15548627.2015.1115939.


Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.

Zhang Z, Ding Q, Liu JJ, Zhang J, Jiang N, Chu XJ, Bartkovitz D, Luk KC, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.

Bioorg Med Chem. 2014 Aug 1;22(15):4001-9. doi: 10.1016/j.bmc.2014.05.072. Epub 2014 Jun 11.


Endogenous c-Myc is essential for p53-induced apoptosis in response to DNA damage in vivo.

Phesse TJ, Myant KB, Cole AM, Ridgway RA, Pearson H, Muncan V, van den Brink GR, Vousden KH, Sears R, Vassilev LT, Clarke AR, Sansom OJ.

Cell Death Differ. 2014 Jun;21(6):956-66. doi: 10.1038/cdd.2014.15. Epub 2014 Feb 28.


Stapled α-helical peptide drug development: a potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy.

Chang YS, Graves B, Guerlavais V, Tovar C, Packman K, To KH, Olson KA, Kesavan K, Gangurde P, Mukherjee A, Baker T, Darlak K, Elkin C, Filipovic Z, Qureshi FZ, Cai H, Berry P, Feyfant E, Shi XE, Horstick J, Annis DA, Manning AM, Fotouhi N, Nash H, Vassilev LT, Sawyer TK.

Proc Natl Acad Sci U S A. 2013 Sep 3;110(36):E3445-54. doi: 10.1073/pnas.1303002110. Epub 2013 Aug 14.


Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.

Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.

J Med Chem. 2013 Jul 25;56(14):5979-83. doi: 10.1021/jm400487c. Epub 2013 Jul 16.


MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models.

Tovar C, Graves B, Packman K, Filipovic Z, Higgins B, Xia M, Tardell C, Garrido R, Lee E, Kolinsky K, To KH, Linn M, Podlaski F, Wovkulich P, Vu B, Vassilev LT.

Cancer Res. 2013 Apr 15;73(8):2587-97. doi: 10.1158/0008-5472.CAN-12-2807. Epub 2013 Feb 11.


Correlation of TP53 and MDM2 genotypes with response to therapy in sarcoma.

Ohnstad HO, Castro R, Sun J, Heintz KM, Vassilev LT, Bjerkehagen B, Kresse SH, Meza-Zepeda LA, Myklebost O.

Cancer. 2013 Mar 1;119(5):1013-22. doi: 10.1002/cncr.27837. Epub 2012 Nov 16.


Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study.

Ray-Coquard I, Blay JY, Italiano A, Le Cesne A, Penel N, Zhi J, Heil F, Rueger R, Graves B, Ding M, Geho D, Middleton SA, Vassilev LT, Nichols GL, Bui BN.

Lancet Oncol. 2012 Nov;13(11):1133-40. doi: 10.1016/S1470-2045(12)70474-6. Epub 2012 Oct 17.


Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization.

Graves B, Thompson T, Xia M, Janson C, Lukacs C, Deo D, Di Lello P, Fry D, Garvie C, Huang KS, Gao L, Tovar C, Lovey A, Wanner J, Vassilev LT.

Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93. doi: 10.1073/pnas.1203789109. Epub 2012 Jun 28.


Subtype and pathway specific responses to anticancer compounds in breast cancer.

Heiser LM, Sadanandam A, Kuo WL, Benz SC, Goldstein TC, Ng S, Gibb WJ, Wang NJ, Ziyad S, Tong F, Bayani N, Hu Z, Billig JI, Dueregger A, Lewis S, Jakkula L, Korkola JE, Durinck S, Pepin F, Guan Y, Purdom E, Neuvial P, Bengtsson H, Wood KW, Smith PG, Vassilev LT, Hennessy BT, Greshock J, Bachman KE, Hardwicke MA, Park JW, Marton LJ, Wolf DM, Collisson EA, Neve RM, Mills GB, Speed TP, Feiler HS, Wooster RF, Haussler D, Stuart JM, Gray JW, Spellman PT.

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2724-9. doi: 10.1073/pnas.1018854108. Epub 2011 Oct 14.


Stabilisation of p53 enhances reovirus-induced apoptosis and virus spread through p53-dependent NF-κB activation.

Pan D, Pan LZ, Hill R, Marcato P, Shmulevitz M, Vassilev LT, Lee PW.

Br J Cancer. 2011 Sep 27;105(7):1012-22. doi: 10.1038/bjc.2011.325. Epub 2011 Aug 23.


MDM2 antagonist Nutlin-3a potentiates antitumour activity of cytotoxic drugs in sarcoma cell lines.

Ohnstad HO, Paulsen EB, Noordhuis P, Berg M, Lothe RA, Vassilev LT, Myklebost O.

BMC Cancer. 2011 May 30;11:211:1-11. doi: 10.1186/1471-2407-11-211.


MDM2 antagonists boost antitumor effect of androgen withdrawal: implications for therapy of prostate cancer.

Tovar C, Higgins B, Kolinsky K, Xia M, Packman K, Heimbrook DC, Vassilev LT.

Mol Cancer. 2011 May 3;10:49. doi: 10.1186/1476-4598-10-49.


p21 does not protect cancer cells from apoptosis induced by nongenotoxic p53 activation.

Xia M, Knezevic D, Vassilev LT.

Oncogene. 2011 Jan 20;30(3):346-55. doi: 10.1038/onc.2010.413. Epub 2010 Sep 27.


Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.

Tovar C, Higgins B, Deo D, Kolinsky K, Liu JJ, Heimbrook DC, Vassilev LT.

Cell Cycle. 2010 Aug 15;9(16):3364-75. doi: 10.4161/cc.9.16.12732. Epub 2010 Aug 21.


1,25-dihydroxyvitamin D3 enhances the apoptotic activity of MDM2 antagonist nutlin-3a in acute myeloid leukemia cells expressing wild-type p53.

Thompson T, Andreeff M, Studzinski GP, Vassilev LT.

Mol Cancer Ther. 2010 May;9(5):1158-68. doi: 10.1158/1535-7163.MCT-09-1036. Epub 2010 Apr 20.


Simultaneous activation of p53 and inhibition of XIAP enhance the activation of apoptosis signaling pathways in AML.

Carter BZ, Mak DH, Schober WD, Koller E, Pinilla C, Vassilev LT, Reed JC, Andreeff M.

Blood. 2010 Jan 14;115(2):306-14. doi: 10.1182/blood-2009-03-212563. Epub 2009 Nov 6.


Pharmacologic p53 activation blocks cell cycle progression but fails to induce senescence in epithelial cancer cells.

Huang B, Deo D, Xia M, Vassilev LT.

Mol Cancer Res. 2009 Sep;7(9):1497-509. doi: 10.1158/1541-7786.MCR-09-0144. Epub 2009 Sep 8.


Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors.

Zhao C, Tovar C, Yin X, Xu Q, Todorov IT, Vassilev LT, Chen L.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):319-23. doi: 10.1016/j.bmcl.2008.11.093. Epub 2008 Nov 27.


Differentiation of trophoblast stem cells into giant cells is triggered by p57/Kip2 inhibition of CDK1 activity.

Ullah Z, Kohn MJ, Yagi R, Vassilev LT, DePamphilis ML.

Genes Dev. 2008 Nov 1;22(21):3024-36. doi: 10.1101/gad.1718108.


p53-mediated apoptosis of CLL cells: evidence for a transcription-independent mechanism.

Steele AJ, Prentice AG, Hoffbrand AV, Yogashangary BC, Hart SM, Nacheva EP, Howard-Reeves JD, Duke VM, Kottaridis PD, Cwynarski K, Vassilev LT, Wickremasinghe RG.

Blood. 2008 Nov 1;112(9):3827-34. doi: 10.1182/blood-2008-05-156380. Epub 2008 Aug 5.


Elevated MDM2 boosts the apoptotic activity of p53-MDM2 binding inhibitors by facilitating MDMX degradation.

Xia M, Knezevic D, Tovar C, Huang B, Heimbrook DC, Vassilev LT.

Cell Cycle. 2008 Jun 1;7(11):1604-12. Epub 2008 Mar 17.


Triptolide sensitizes AML cells to TRAIL-induced apoptosis via decrease of XIAP and p53-mediated increase of DR5.

Carter BZ, Mak DH, Schober WD, Dietrich MF, Pinilla C, Vassilev LT, Reed JC, Andreeff M.

Blood. 2008 Apr 1;111(7):3742-50. doi: 10.1182/blood-2007-05-091504. Epub 2008 Jan 10.


Induction of p53-dependent senescence by the MDM2 antagonist nutlin-3a in mouse cells of fibroblast origin.

Efeyan A, Ortega-Molina A, Velasco-Miguel S, Herranz D, Vassilev LT, Serrano M.

Cancer Res. 2007 Aug 1;67(15):7350-7.


Enhanced tumor cell kill by combined treatment with a small-molecule antagonist of mouse double minute 2 and adenoviruses encoding p53.

Graat HC, Carette JE, Schagen FH, Vassilev LT, Gerritsen WR, Kaspers GJ, Wuisman PI, van Beusechem VW.

Mol Cancer Ther. 2007 May;6(5):1552-61.


Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.

Chen S, Chen L, Le NT, Zhao C, Sidduri A, Lou JP, Michoud C, Portland L, Jackson N, Liu JJ, Konzelmann F, Chi F, Tovar C, Xiang Q, Chen Y, Wen Y, Vassilev LT.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2134-8. Epub 2007 Jan 31.


Pharmacologic activation of p53-dependent and p53-independent apoptotic pathways in Hodgkin/Reed-Sternberg cells.

Janz M, Stühmer T, Vassilev LT, Bargou RC.

Leukemia. 2007 Apr;21(4):772-9. Epub 2007 Feb 1.


Cell cycle synchronization at the G2/M phase border by reversible inhibition of CDK1.

Vassilev LT.

Cell Cycle. 2006 Nov;5(22):2555-6. Epub 2006 Nov 15.


Mouse double minute antagonist Nutlin-3a enhances chemotherapy-induced apoptosis in cancer cells with mutant p53 by activating E2F1.

Ambrosini G, Sambol EB, Carvajal D, Vassilev LT, Singer S, Schwartz GK.

Oncogene. 2007 May 24;26(24):3473-81. Epub 2006 Dec 4.


MDM2 inhibitors for cancer therapy.

Vassilev LT.

Trends Mol Med. 2007 Jan;13(1):23-31. Epub 2006 Nov 28. Review.


Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.

Vassilev LT, Tovar C, Chen S, Knezevic D, Zhao X, Sun H, Heimbrook DC, Chen L.

Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10660-5. Epub 2006 Jul 3.


Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy.

Tovar C, Rosinski J, Filipovic Z, Higgins B, Kolinsky K, Hilton H, Zhao X, Vu BT, Qing W, Packman K, Myklebost O, Heimbrook DC, Vassilev LT.

Proc Natl Acad Sci U S A. 2006 Feb 7;103(6):1888-93. Epub 2006 Jan 27.


MDM2 antagonists activate p53 and synergize with genotoxic drugs in B-cell chronic lymphocytic leukemia cells.

Coll-Mulet L, Iglesias-Serret D, Santidrián AF, Cosialls AM, de Frias M, Castaño E, Campàs C, Barragán M, de Sevilla AF, Domingo A, Vassilev LT, Pons G, Gil J.

Blood. 2006 May 15;107(10):4109-14. Epub 2006 Jan 26.


High-throughput screening for inhibitors of the Cks1-Skp2 interaction.

Huang KS, Vassilev LT.

Methods Enzymol. 2005;399:717-28.


Development of E3-substrate (MDM2-p53)-binding inhibitors: structural aspects.

Fry DC, Graves B, Vassilev LT.

Methods Enzymol. 2005;399:622-33.


Targeting protein-protein interactions for cancer therapy.

Fry DC, Vassilev LT.

J Mol Med (Berl). 2005 Dec;83(12):955-63. Epub 2005 Nov 11. Review.


Depletion of mutant p53 and cytotoxicity of histone deacetylase inhibitors.

Blagosklonny MV, Trostel S, Kayastha G, Demidenko ZN, Vassilev LT, Romanova LY, Bates S, Fojo T.

Cancer Res. 2005 Aug 15;65(16):7386-92.


Nongenotoxic activation of the p53 pathway as a therapeutic strategy for multiple myeloma.

Stühmer T, Chatterjee M, Hildebrandt M, Herrmann P, Gollasch H, Gerecke C, Theurich S, Cigliano L, Manz RA, Daniel PT, Bommert K, Vassilev LT, Bargou RC.

Blood. 2005 Nov 15;106(10):3609-17. Epub 2005 Aug 4.


MDM2 antagonists induce p53-dependent apoptosis in AML: implications for leukemia therapy.

Kojima K, Konopleva M, Samudio IJ, Shikami M, Cabreira-Hansen M, McQueen T, Ruvolo V, Tsao T, Zeng Z, Vassilev LT, Andreeff M.

Blood. 2005 Nov 1;106(9):3150-9. Epub 2005 Jul 12.


p53 Activation by small molecules: application in oncology.

Vassilev LT.

J Med Chem. 2005 Jul 14;48(14):4491-9. Review. No abstract available.


Activation of p53 by MDM2 antagonists can protect proliferating cells from mitotic inhibitors.

Carvajal D, Tovar C, Yang H, Vu BT, Heimbrook DC, Vassilev LT.

Cancer Res. 2005 Mar 1;65(5):1918-24.


Phosphorylation of p53 on key serines is dispensable for transcriptional activation and apoptosis.

Thompson T, Tovar C, Yang H, Carvajal D, Vu BT, Xu Q, Wahl GM, Heimbrook DC, Vassilev LT.

J Biol Chem. 2004 Dec 17;279(51):53015-22. Epub 2004 Oct 6.


Targeting the p53-MDM2 interaction to treat cancer.

Klein C, Vassilev LT.

Br J Cancer. 2004 Oct 18;91(8):1415-9. Review.


Small-molecule antagonists of p53-MDM2 binding: research tools and potential therapeutics.

Vassilev LT.

Cell Cycle. 2004 Apr;3(4):419-21. Epub 2004 Apr 1.


In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.

Vassilev LT, Vu BT, Graves B, Carvajal D, Podlaski F, Filipovic Z, Kong N, Kammlott U, Lukacs C, Klein C, Fotouhi N, Liu EA.

Science. 2004 Feb 6;303(5659):844-8. Epub 2004 Jan 2.


Macrophage inhibitory cytokine-1: a novel biomarker for p53 pathway activation.

Yang H, Filipovic Z, Brown D, Breit SN, Vassilev LT.

Mol Cancer Ther. 2003 Oct;2(10):1023-9.


A generic time-resolved fluorescence assay for serine/threonine kinase activity: application to Cdc7/Dbf4.

Xu K, Stern AS, Levin W, Chua A, Vassilev LT.

J Biochem Mol Biol. 2003 Jul 31;36(4):421-5.


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