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Items: 1 to 20 of 108

1.

An androgen receptor N-terminal domain antagonist for treating prostate cancer.

Myung JK, Banuelos CA, Fernandez JG, Mawji NR, Wang J, Tien AH, Yang YC, Tavakoli I, Haile S, Watt K, McEwan IJ, Plymate S, Andersen RJ, Sadar MD.

J Clin Invest. 2013 Jul;123(7):2948-60. doi: 10.1172/JCI66398. Epub 2013 Jun 3.

2.

Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor.

Andersen RJ, Mawji NR, Wang J, Wang G, Haile S, Myung JK, Watt K, Tam T, Yang YC, Bañuelos CA, Williams DE, McEwan IJ, Wang Y, Sadar MD.

Cancer Cell. 2010 Jun 15;17(6):535-46. doi: 10.1016/j.ccr.2010.04.027.

3.

Sintokamide A Is a Novel Antagonist of Androgen Receptor That Uniquely Binds Activation Function-1 in Its Amino-terminal Domain.

Banuelos CA, Tavakoli I, Tien AH, Caley DP, Mawji NR, Li Z, Wang J, Yang YC, Imamura Y, Yan L, Wen JG, Andersen RJ, Sadar MD.

J Biol Chem. 2016 Oct 14;291(42):22231-22243. Epub 2016 Aug 30.

4.

EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer.

Brand LJ, Olson ME, Ravindranathan P, Guo H, Kempema AM, Andrews TE, Chen X, Raj GV, Harki DA, Dehm SM.

Oncotarget. 2015 Feb 28;6(6):3811-24.

5.

Characterization of niphatenones that inhibit androgen receptor N-terminal domain.

Banuelos CA, Lal A, Tien AH, Shah N, Yang YC, Mawji NR, Meimetis LG, Park J, Kunzhong J, Andersen RJ, Sadar MD.

PLoS One. 2014 Sep 30;9(9):e107991. doi: 10.1371/journal.pone.0107991. eCollection 2014.

6.
7.

Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer.

Dalal K, Roshan-Moniri M, Sharma A, Li H, Ban F, Hassona MD, Hsing M, Singh K, LeBlanc E, Dehm S, Tomlinson Guns ES, Cherkasov A, Rennie PS.

J Biol Chem. 2014 Sep 19;289(38):26417-29. doi: 10.1074/jbc.M114.553818. Epub 2014 Aug 1. Erratum in: J Biol Chem. 2015 Oct 23;290(43):25850. J Biol Chem. 2014 Dec 5;289(49):33877. Hessein, Mohamed [Corrected to Hassona, Mohamed D]. J Biol Chem. 2017 Mar 10;292(10 ):4359.

8.

In silico discovery of androgen receptor antagonists with activity in castration resistant prostate cancer.

Shen HC, Shanmugasundaram K, Simon NI, Cai C, Wang H, Chen S, Balk SP, Rigby AC.

Mol Endocrinol. 2012 Nov;26(11):1836-46. doi: 10.1210/me.2012-1222. Epub 2012 Sep 28.

9.

Lupeol, a novel androgen receptor inhibitor: implications in prostate cancer therapy.

Siddique HR, Mishra SK, Karnes RJ, Saleem M.

Clin Cancer Res. 2011 Aug 15;17(16):5379-91. doi: 10.1158/1078-0432.CCR-11-0916. Epub 2011 Jun 28.

10.

Targeting Binding Function-3 of the Androgen Receptor Blocks Its Co-Chaperone Interactions, Nuclear Translocation, and Activation.

Lallous N, Leblanc E, Munuganti RS, Hassona MD, Nakouzi NA, Awrey S, Morin H, Roshan-Moniri M, Singh K, Lawn S, Yamazaki T, Adomat HH, Andre C, Daugaard M, Young RN, Guns ES, Rennie PS, Cherkasov A.

Mol Cancer Ther. 2016 Dec;15(12):2936-2945. Epub 2016 Oct 7.

PMID:
27765852
11.

Small molecule inhibitors targeting the "achilles' heel" of androgen receptor activity.

Sadar MD.

Cancer Res. 2011 Feb 15;71(4):1208-13. doi: 10.1158/0008-5472.CAN_10-3398. Epub 2011 Feb 1. Review.

12.

Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer.

Long BJ, Grigoryev DN, Nnane IP, Liu Y, Ling YZ, Brodie AM.

Cancer Res. 2000 Dec 1;60(23):6630-40.

13.

Reduced expression of the androgen receptor by third generation of antisense shows antitumor activity in models of prostate cancer.

Zhang Y, Castaneda S, Dumble M, Wang M, Mileski M, Qu Z, Kim S, Shi V, Kraft P, Gao Y, Pak J, Sapra P, Bandaru R, Zhao H, Vessella RL, Horak ID, Greenberger LM.

Mol Cancer Ther. 2011 Dec;10(12):2309-19. doi: 10.1158/1535-7163.MCT-11-0329. Epub 2011 Oct 25.

14.

Distinct transcriptional programs mediated by the ligand-dependent full-length androgen receptor and its splice variants in castration-resistant prostate cancer.

Hu R, Lu C, Mostaghel EA, Yegnasubramanian S, Gurel M, Tannahill C, Edwards J, Isaacs WB, Nelson PS, Bluemn E, Plymate SR, Luo J.

Cancer Res. 2012 Jul 15;72(14):3457-62. doi: 10.1158/0008-5472.CAN-11-3892. Epub 2012 Jun 18.

15.

EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor.

De Mol E, Fenwick RB, Phang CT, Buzón V, Szulc E, de la Fuente A, Escobedo A, García J, Bertoncini CW, Estébanez-Perpiñá E, McEwan IJ, Riera A, Salvatella X.

ACS Chem Biol. 2016 Sep 16;11(9):2499-505. doi: 10.1021/acschembio.6b00182. Epub 2016 Jul 14.

16.

Emodin down-regulates androgen receptor and inhibits prostate cancer cell growth.

Cha TL, Qiu L, Chen CT, Wen Y, Hung MC.

Cancer Res. 2005 Mar 15;65(6):2287-95.

17.

Effect of small molecules modulating androgen receptor (SARMs) in human prostate cancer models.

Tesei A, Leonetti C, Di Donato M, Gabucci E, Porru M, Varchi G, Guerrini A, Amadori D, Arienti C, Pignatta S, Paganelli G, Caraglia M, Castoria G, Zoli W.

PLoS One. 2013 May 8;8(5):e62657. doi: 10.1371/journal.pone.0062657. Print 2013.

18.

Inhibition of the androgen receptor as a novel mechanism of taxol chemotherapy in prostate cancer.

Gan L, Chen S, Wang Y, Watahiki A, Bohrer L, Sun Z, Wang Y, Huang H.

Cancer Res. 2009 Nov 1;69(21):8386-94. doi: 10.1158/0008-5472.CAN-09-1504. Epub 2009 Oct 13.

19.

Discovery and biological characterization of a novel series of androgen receptor modulators.

Zhou C, Wu G, Feng Y, Li Q, Su H, Mais DE, Zhu Y, Li N, Deng Y, Yang D, Wang MW.

Br J Pharmacol. 2008 May;154(2):440-50. doi: 10.1038/bjp.2008.107. Epub 2008 Apr 14. Erratum in: Br J Pharmacol. 2008 Jul;154(5):1161.

20.

A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides.

Guerrini A, Tesei A, Ferroni C, Paganelli G, Zamagni A, Carloni S, Di Donato M, Castoria G, Leonetti C, Porru M, De Cesare M, Zaffaroni N, Beretta GL, Del Rio A, Varchi G.

J Med Chem. 2014 Sep 11;57(17):7263-79. doi: 10.1021/jm5005122. Epub 2014 Aug 28.

PMID:
25121586

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