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Items: 1 to 20 of 132

1.

Identification of novel androgen receptor antagonists using structure- and ligand-based methods.

Li H, Ren X, Leblanc E, Frewin K, Rennie PS, Cherkasov A.

J Chem Inf Model. 2013 Jan 28;53(1):123-30. doi: 10.1021/ci300514v. Epub 2013 Jan 16.

PMID:
23278403
2.

Identification and characterization of MEL-3, a novel AR antagonist that suppresses prostate cancer cell growth.

Helsen C, Marchand A, Chaltin P, Munck S, Voet A, Verstuyf A, Claessens F.

Mol Cancer Ther. 2012 Jun;11(6):1257-68. doi: 10.1158/1535-7163.MCT-11-0763. Epub 2012 Apr 10.

3.

Learning from estrogen receptor antagonism: structure-based identification of novel antiandrogens effective against multiple clinically relevant androgen receptor mutants.

Liu B, Geng G, Lin R, Ren C, Wu JH.

Chem Biol Drug Des. 2012 Mar;79(3):300-12. doi: 10.1111/j.1747-0285.2011.01290.x. Epub 2012 Jan 11.

PMID:
22151347
4.

Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor.

Li H, Ban F, Dalal K, Leblanc E, Frewin K, Ma D, Adomat H, Rennie PS, Cherkasov A.

J Med Chem. 2014 Aug 14;57(15):6458-67. doi: 10.1021/jm500802j. Epub 2014 Aug 4.

PMID:
25062331
5.

The discovery of novel human androgen receptor antagonist chemotypes using a combined pharmacophore screening procedure.

Voet A, Helsen C, Zhang KY, Claessens F.

ChemMedChem. 2013 Apr;8(4):644-51. doi: 10.1002/cmdc.201200549. Epub 2013 Feb 21.

PMID:
23436650
6.

Characterization of a new class of androgen receptor antagonists with potential therapeutic application in advanced prostate cancer.

Li H, Hassona MD, Lack NA, Axerio-Cilies P, Leblanc E, Tavassoli P, Kanaan N, Frewin K, Singh K, Adomat H, Böhm KJ, Prinz H, Guns ET, Rennie PS, Cherkasov A.

Mol Cancer Ther. 2013 Nov;12(11):2425-35. doi: 10.1158/1535-7163.MCT-13-0267. Epub 2013 Aug 12.

7.

Modeling androgen receptor flexibility: a binding mode hypothesis of CYP17 inhibitors/antiandrogens for prostate cancer therapy.

Gianti E, Zauhar RJ.

J Chem Inf Model. 2012 Oct 22;52(10):2670-83. doi: 10.1021/ci3002342. Epub 2012 Oct 1.

PMID:
22924551
9.

Steroid derivatives as pure antagonists of the androgen receptor.

Gauthier S, Martel C, Labrie F.

J Steroid Biochem Mol Biol. 2012 Oct;132(1-2):93-104. doi: 10.1016/j.jsbmb.2012.02.006. Epub 2012 Mar 23.

PMID:
22449547
10.

Discovery of novel androgen receptor antagonists: a hybrid approach of pharmacophore-based and docking-based virtual screening.

Liu J, Liu B, Guo G, Jing Y, Zhao G.

Anticancer Drugs. 2015 Aug;26(7):747-53. doi: 10.1097/CAD.0000000000000245.

PMID:
25933245
11.

Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening.

Axerio-Cilies P, Lack NA, Nayana MR, Chan KH, Yeung A, Leblanc E, Guns ES, Rennie PS, Cherkasov A.

J Med Chem. 2011 Sep 22;54(18):6197-205. doi: 10.1021/jm200532b. Epub 2011 Aug 29.

PMID:
21846139
12.

Identification of a group of brominated flame retardants as novel androgen receptor antagonists and potential neuronal and endocrine disrupters.

Kharlyngdoh JB, Pradhan A, Asnake S, Walstad A, Ivarsson P, Olsson PE.

Environ Int. 2015 Jan;74:60-70. doi: 10.1016/j.envint.2014.09.002. Epub 2014 Oct 20.

PMID:
25454221
13.

Structure-based virtual screening and identification of a novel androgen receptor antagonist.

Song CH, Yang SH, Park E, Cho SH, Gong EY, Khadka DB, Cho WJ, Lee K.

J Biol Chem. 2012 Aug 31;287(36):30769-80. doi: 10.1074/jbc.M112.379107. Epub 2012 Jul 13.

14.

Iminoenamine based novel androgen receptor antagonist exhibited anti-prostate cancer activity in androgen independent prostate cancer cells through inhibition of AKT pathway.

Divakar S, Saravanan K, Karthikeyan P, Elancheran R, Kabilan S, Balasubramanian KK, Devi R, Kotoky J, Ramanathan M.

Chem Biol Interact. 2017 Sep 25;275:22-34. doi: 10.1016/j.cbi.2017.07.023. Epub 2017 Jul 27.

PMID:
28757136
15.

Androgen receptor antagonists for prostate cancer therapy.

Helsen C, Van den Broeck T, Voet A, Prekovic S, Van Poppel H, Joniau S, Claessens F.

Endocr Relat Cancer. 2014 Aug;21(4):T105-18. doi: 10.1530/ERC-13-0545. Epub 2014 Mar 17. Review.

16.

A multi-parameter imaging assay identifies different stages of ligand-induced androgen receptor activation.

van Royen ME, van de Wijngaart DJ, Cunha SM, Trapman J, Houtsmuller AB.

Cytometry A. 2013 Sep;83(9):806-17. doi: 10.1002/cyto.a.22284. Epub 2013 Apr 12.

17.

Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.

Ivachtchenko AV, Ivanenkov YA, Mitkin OD, Vorobiev AA, Kuznetsova IV, Shevkun NA, Koryakova AG, Karapetian RN, Trifelenkov AS, Kravchenko DV, Veselov MS, Chufarova NV.

Eur J Med Chem. 2015 Jun 24;99:51-66. doi: 10.1016/j.ejmech.2015.05.039. Epub 2015 Jun 2.

PMID:
26046313
18.

Androgen receptor as a therapeutic target.

Gao W.

Adv Drug Deliv Rev. 2010 Oct 30;62(13):1277-84. doi: 10.1016/j.addr.2010.08.002. Epub 2010 Aug 12. Review.

PMID:
20708648
19.

Combined Ligand/Structure-Based Virtual Screening and Molecular Dynamics Simulations of Steroidal Androgen Receptor Antagonists.

Wang Y, Han R, Zhang H, Liu H, Li J, Liu H, Gramatica P.

Biomed Res Int. 2017;2017:3572394. doi: 10.1155/2017/3572394. Epub 2017 Feb 15.

20.

Inhibition of MAPK-signaling pathway promotes the interaction of the corepressor SMRT with the human androgen receptor and mediates repression of prostate cancer cell growth in the presence of antiandrogens.

Eisold M, Asim M, Eskelinen H, Linke T, Baniahmad A.

J Mol Endocrinol. 2009 May;42(5):429-35. doi: 10.1677/JME-08-0084. Epub 2009 Feb 17.

PMID:
19223455

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