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Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors.

Rai G, Vyjayanti VN, Dorjsuren D, Simeonov A, Jadhav A, Wilson DM 3rd, Maloney DJ.

J Med Chem. 2012 Apr 12;55(7):3101-12. doi: 10.1021/jm201537d. Epub 2012 Mar 28.


The apurinic/apyrimidinic endonuclease activity of Ape1/Ref-1 contributes to human glioma cell resistance to alkylating agents and is elevated by oxidative stress.

Silber JR, Bobola MS, Blank A, Schoeler KD, Haroldson PD, Huynh MB, Kolstoe DD.

Clin Cancer Res. 2002 Sep;8(9):3008-18. Erratum in: Clin Cancer Res. 2003 Jul;9(7):2877.


Diverse small molecule inhibitors of human apurinic/apyrimidinic endonuclease APE1 identified from a screen of a large public collection.

Dorjsuren D, Kim D, Vyjayanti VN, Maloney DJ, Jadhav A, Wilson DM 3rd, Simeonov A.

PLoS One. 2012;7(10):e47974. doi: 10.1371/journal.pone.0047974. Epub 2012 Oct 23.


Novel small-molecule inhibitor of apurinic/apyrimidinic endonuclease 1 blocks proliferation and reduces viability of glioblastoma cells.

Bapat A, Glass LS, Luo M, Fishel ML, Long EC, Georgiadis MM, Kelley MR.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):988-98. doi: 10.1124/jpet.110.169128. Epub 2010 May 26.


Small Molecule Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1).

Rai G, Vyjayanti VN, Dorjsuren D, Simeonov A, Jadhav A, Wilson DM, Maloney DJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 29 [updated 2013 Feb 28].


Isolation of a small molecule inhibitor of DNA base excision repair.

Madhusudan S, Smart F, Shrimpton P, Parsons JL, Gardiner L, Houlbrook S, Talbot DC, Hammonds T, Freemont PA, Sternberg MJ, Dianov GL, Hickson ID.

Nucleic Acids Res. 2005 Aug 19;33(15):4711-24. Print 2005.


Human AP endonuclease 1 (APE1): from mechanistic insights to druggable target in cancer.

Abbotts R, Madhusudan S.

Cancer Treat Rev. 2010 Aug;36(5):425-35. doi: 10.1016/j.ctrv.2009.12.006. Epub 2010 Jan 6. Review.


Development and evaluation of human AP endonuclease inhibitors in melanoma and glioma cell lines.

Mohammed MZ, Vyjayanti VN, Laughton CA, Dekker LV, Fischer PM, Wilson DM 3rd, Abbotts R, Shah S, Patel PM, Hickson ID, Madhusudan S.

Br J Cancer. 2011 Feb 15;104(4):653-63. doi: 10.1038/sj.bjc.6606058. Epub 2011 Jan 25.


Identification of a novel potential antitumor activity of gossypol as an APE1/Ref-1 inhibitor.

Qian C, Li M, Sui J, Ren T, Li Z, Zhang L, Zhou L, Cheng Y, Wang D.

Drug Des Devel Ther. 2014 May 9;8:485-96. doi: 10.2147/DDDT.S62963. eCollection 2014.


Design and synthesis of 3-carbamoylbenzoic acid derivatives as inhibitors of human apurinic/apyrimidinic endonuclease 1 (APE1).

Aiello F, Shabaik Y, Esqueda A, Sanchez TW, Grande F, Garofalo A, Neamati N.

ChemMedChem. 2012 Oct;7(10):1825-39. doi: 10.1002/cmdc.201200334. Epub 2012 Sep 5.


Functional analysis of the involvement of apurinic/apyrimidinic endonuclease 1 in the resistance to melphalan in multiple myeloma.

Xie J, Zhang L, Li M, Du J, Zhou L, Yang S, Zeng L, Li Z, Wang G, Wang D.

BMC Cancer. 2014 Jan 8;14:11. doi: 10.1186/1471-2407-14-11.


Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors.

Zawahir Z, Dayam R, Deng J, Pereira C, Neamati N.

J Med Chem. 2009 Jan 8;52(1):20-32. doi: 10.1021/jm800739m.


Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1.

Simeonov A, Kulkarni A, Dorjsuren D, Jadhav A, Shen M, McNeill DR, Austin CP, Wilson DM 3rd.

PLoS One. 2009 Jun 1;4(6):e5740. doi: 10.1371/journal.pone.0005740.


Combined treatment with temozolomide and methoxyamine: blocking apurininc/pyrimidinic site repair coupled with targeting topoisomerase IIalpha.

Yan L, Bulgar A, Miao Y, Mahajan V, Donze JR, Gerson SL, Liu L.

Clin Cancer Res. 2007 Mar 1;13(5):1532-9.


A novel inhibitor of DNA polymerase beta enhances the ability of temozolomide to impair the growth of colon cancer cells.

Jaiswal AS, Banerjee S, Panda H, Bulkin CD, Izumi T, Sarkar FH, Ostrov DA, Narayan S.

Mol Cancer Res. 2009 Dec;7(12):1973-83. doi: 10.1158/1541-7786.MCR-09-0309. Epub 2009 Dec 8.


Receptor-based virtual screening and biological characterization of human apurinic/apyrimidinic endonuclease (Ape1) inhibitors.

Ruiz FM, Francis SM, Tintoré M, Ferreira R, Gil-Redondo R, Morreale A, Ortiz ÁR, Eritja R, Fàbrega C.

ChemMedChem. 2012 Dec;7(12):2168-78. doi: 10.1002/cmdc.201200372. Epub 2012 Oct 25.


Genetic and biochemical characterization of human AP endonuclease 1 mutants deficient in nucleotide incision repair activity.

Gelin A, Redrejo-Rodríguez M, Laval J, Fedorova OS, Saparbaev M, Ishchenko AA.

PLoS One. 2010 Aug 17;5(8):e12241. doi: 10.1371/journal.pone.0012241.


Small-molecule inhibitors of APE1 DNA repair function: an overview.

Al-Safi RI, Odde S, Shabaik Y, Neamati N.

Curr Mol Pharmacol. 2012 Jan;5(1):14-35. Review.

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