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Items: 1 to 50 of 77

1.

Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer.

Ponnusamy S, He Y, Hwang DJ, Thiyagarajan T, Houtman R, Bocharova V, Sumpter BG, Fernandez E, Johnson D, Du Z, Pfeffer LM, Getzenberg RH, McEwan IJ, Miller DD, Narayanan R.

Clin Cancer Res. 2019 Sep 3. doi: 10.1158/1078-0432.CCR-19-1458. [Epub ahead of print]

PMID:
31481513
2.

New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.

Hwang DJ, He Y, Ponnusamy S, Mohler ML, Thiyagarajan T, McEwan IJ, Narayanan R, Miller DD.

J Med Chem. 2019 Jan 24;62(2):491-511. doi: 10.1021/acs.jmedchem.8b00973. Epub 2018 Dec 26.

PMID:
30525603
3.

A reciprocal feedback between the PDZ binding kinase and androgen receptor drives prostate cancer.

Warren AY, Massie CE, Watt K, Luko K, Orafidiya F, Selth LA, Mohammed H, Chohan BS, Menon S, Baridi A, Zhao W, Escriu C, Pungsrinont T, D'Santos C, Yang X, Taylor C, Qureshi A, Zecchini VR, Shaw GL, Dehm SM, Mills IG, Carroll JS, Tilley WD, McEwan IJ, Baniahmad A, Neal DE, Asim M.

Oncogene. 2019 Feb;38(7):1136-1150. doi: 10.1038/s41388-018-0501-z. Epub 2018 Sep 20.

4.

Androgens and androgen receptor: Above and beyond.

Gibson DA, Saunders PTK, McEwan IJ.

Mol Cell Endocrinol. 2018 Apr 15;465:1-3. doi: 10.1016/j.mce.2018.02.013. Epub 2018 Feb 24. No abstract available.

PMID:
29481861
5.

Regulation of Androgen Receptor Activity by Transient Interactions of Its Transactivation Domain with General Transcription Regulators.

De Mol E, Szulc E, Di Sanza C, Martínez-Cristóbal P, Bertoncini CW, Fenwick RB, Frigolé-Vivas M, Masín M, Hunter I, Buzón V, Brun-Heath I, García J, De Fabritiis G, Estébanez-Perpiñá E, McEwan IJ, Nebreda ÁR, Salvatella X.

Structure. 2018 Jan 2;26(1):145-152.e3. doi: 10.1016/j.str.2017.11.007. Epub 2017 Dec 7.

6.

Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer.

Ponnusamy S, Coss CC, Thiyagarajan T, Watts K, Hwang DJ, He Y, Selth LA, McEwan IJ, Duke CB, Pagadala J, Singh G, Wake RW, Ledbetter C, Tilley WD, Moldoveanu T, Dalton JT, Miller DD, Narayanan R.

Cancer Res. 2017 Nov 15;77(22):6282-6298. doi: 10.1158/0008-5472.CAN-17-0976. Epub 2017 Oct 4.

7.

Tissue control of androgen action: The ups and downs of androgen receptor expression.

Hunter I, Hay CW, Esswein B, Watt K, McEwan IJ.

Mol Cell Endocrinol. 2018 Apr 15;465:27-35. doi: 10.1016/j.mce.2017.08.002. Epub 2017 Aug 5. Review.

PMID:
28789969
8.

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.

9.

Posttranslational Modifications of Steroid Receptors: Phosphorylation.

McGuinness D, McEwan IJ.

Methods Mol Biol. 2016;1443:105-17. doi: 10.1007/978-1-4939-3724-0_7.

PMID:
27246336
10.

The Nuclear Receptor Superfamily at Thirty.

McEwan IJ.

Methods Mol Biol. 2016;1443:3-9. doi: 10.1007/978-1-4939-3724-0_1.

PMID:
27246330
11.

A sting in the tail: the N-terminal domain of the androgen receptor as a drug target.

Monaghan AE, McEwan IJ.

Asian J Androl. 2016 Sep-Oct;18(5):687-94. doi: 10.4103/1008-682X.181081. Review.

12.

Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer.

Yang YC, Banuelos CA, Mawji NR, Wang J, Kato M, Haile S, McEwan IJ, Plymate S, Sadar MD.

Clin Cancer Res. 2016 Sep 1;22(17):4466-77. doi: 10.1158/1078-0432.CCR-15-2901. Epub 2016 May 2.

13.

Choline Kinase Alpha as an Androgen Receptor Chaperone and Prostate Cancer Therapeutic Target.

Asim M, Massie CE, Orafidiya F, Pértega-Gomes N, Warren AY, Esmaeili M, Selth LA, Zecchini HI, Luko K, Qureshi A, Baridi A, Menon S, Madhu B, Escriu C, Lyons S, Vowler SL, Zecchini VR, Shaw G, Hessenkemper W, Russell R, Mohammed H, Stefanos N, Lynch AG, Grigorenko E, D'Santos C, Taylor C, Lamb A, Sriranjan R, Yang J, Stark R, Dehm SM, Rennie PS, Carroll JS, Griffiths JR, Tavaré S, Mills IG, McEwan IJ, Baniahmad A, Tilley WD, Neal DE.

J Natl Cancer Inst. 2015 Dec 11;108(5). doi: 10.1093/jnci/djv371. Print 2016 May.

14.

An Sp1 Modulated Regulatory Region Unique to Higher Primates Regulates Human Androgen Receptor Promoter Activity in Prostate Cancer Cells.

Hay CW, Hunter I, MacKenzie A, McEwan IJ.

PLoS One. 2015 Oct 8;10(10):e0139990. doi: 10.1371/journal.pone.0139990. eCollection 2015.

15.

Trinucleotide repeats and protein folding and disease: the perspective from studies with the androgen receptor.

Orafidiya FA, McEwan IJ.

Future Sci OA. 2015 Sep 1;1(2):FSO47. doi: 10.4155/fso.15.47. eCollection 2015 Sep. Review.

16.

Androgen Physiology: Receptor and Metabolic Disorders.

McEwan IJ, Brinkmann AO.

In: Feingold KR, Anawalt B, Boyce A, Chrousos G, Dungan K, Grossman A, Hershman JM, Kaltsas G, Koch C, Kopp P, Korbonits M, McLachlan R, Morley JE, New M, Perreault L, Purnell J, Rebar R, Singer F, Trence DL, Vinik A, Wilson DP, editors. Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc.; 2000-.
2016 Jun 12.

17.

Promoter-dependent activity on androgen receptor N-terminal domain mutations in androgen insensitivity syndrome.

Tadokoro-Cuccaro R, Davies J, Mongan NP, Bunch T, Brown RS, Audi L, Watt K, McEwan IJ, Hughes IA.

Sex Dev. 2014;8(6):339-49. doi: 10.1159/000369266. Epub 2014 Dec 6.

18.

Functional effects of polymorphisms on glucocorticoid receptor modulation of human anxiogenic substance-P gene promoter activity in primary amygdala neurones.

Hay CW, Shanley L, Davidson S, Cowie P, Lear M, McGuffin P, Riedel G, McEwan IJ, MacKenzie A.

Psychoneuroendocrinology. 2014 Sep;47:43-55. doi: 10.1016/j.psyneuen.2014.04.017. Epub 2014 May 2.

19.

Negative regulation of the androgen receptor gene through a primate-specific androgen response element present in the 5' UTR.

Hay CW, Watt K, Hunter I, Lavery DN, MacKenzie A, McEwan IJ.

Horm Cancer. 2014 Oct;5(5):299-311. doi: 10.1007/s12672-014-0185-y. Epub 2014 Jun 4.

20.

Androgen receptor modulators: a marriage of chemistry and biology.

McEwan IJ.

Future Med Chem. 2013 Jun;5(10):1109-20. doi: 10.4155/fmc.13.69. Review.

PMID:
23795968
21.

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.

22.

What lies beneath: natural products from marine organisms as nuclear receptor modulators.

McEwan IJ.

Biochem J. 2012 Aug 15;446(1):e1-3. doi: 10.1042/BJ20121018.

PMID:
22835216
23.

Allosteric modulators of steroid hormone receptors: structural dynamics and gene regulation.

Kumar R, McEwan IJ.

Endocr Rev. 2012 Apr;33(2):271-99. doi: 10.1210/er.2011-1033. Epub 2012 Mar 20. Review.

24.

Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100.

Richards J, Lim AC, Hay CW, Taylor AE, Wingate A, Nowakowska K, Pezaro C, Carreira S, Goodall J, Arlt W, McEwan IJ, de Bono JS, Attard G.

Cancer Res. 2012 May 1;72(9):2176-82. doi: 10.1158/0008-5472.CAN-11-3980. Epub 2012 Mar 12.

25.

The impact of point mutations in the human androgen receptor: classification of mutations on the basis of transcriptional activity.

Hay CW, McEwan IJ.

PLoS One. 2012;7(3):e32514. doi: 10.1371/journal.pone.0032514. Epub 2012 Mar 5.

26.

Nuclear hormone receptors: allosteric switches.

McEwan IJ.

Mol Cell Endocrinol. 2012 Jan 30;348(2):345-7. doi: 10.1016/j.mce.2011.08.035. Epub 2011 Sep 1. No abstract available.

PMID:
21906655
27.

Intrinsic disorder in the androgen receptor: identification, characterisation and drugability.

McEwan IJ.

Mol Biosyst. 2012 Jan;8(1):82-90. doi: 10.1039/c1mb05249g. Epub 2011 Aug 5. Review.

PMID:
21822504
28.

Long-range regulatory synergy is required to allow control of the TAC1 locus by MEK/ERK signalling in sensory neurones.

Shanley L, Davidson S, Lear M, Thotakura AK, McEwan IJ, Ross RA, MacKenzie A.

Neurosignals. 2010;18(3):173-85. doi: 10.1159/000322010. Epub 2010 Dec 16.

29.

Regulation of the androgen receptor by SET9-mediated methylation.

Gaughan L, Stockley J, Wang N, McCracken SR, Treumann A, Armstrong K, Shaheen F, Watt K, McEwan IJ, Wang C, Pestell RG, Robson CN.

Nucleic Acids Res. 2011 Mar;39(4):1266-79. doi: 10.1093/nar/gkq861. Epub 2010 Oct 19. Erratum in: Nucleic Acids Res. 2013 Jul;41(13):6783.

30.

Conformation of the mineralocorticoid receptor N-terminal domain: evidence for induced and stable structure.

Fischer K, Kelly SM, Watt K, Price NC, McEwan IJ.

Mol Endocrinol. 2010 Oct;24(10):1935-48. doi: 10.1210/me.2010-0005. Epub 2010 Aug 4.

31.

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.

32.

Identification of androgen receptor phosphorylation in the primate ovary in vivo.

McEwan IJ, McGuinness D, Hay CW, Millar RP, Saunders PT, Fraser HM.

Reproduction. 2010 Jul;140(1):93-104. doi: 10.1530/REP-10-0140. Epub 2010 Apr 20.

33.
34.

Using intrinsic fluorescence emission spectroscopy to study steroid receptor and coactivator protein conformation dynamics.

Watt K, McEwan IJ.

Methods Mol Biol. 2009;505:205-18. doi: 10.1007/978-1-60327-575-0_12.

PMID:
19117147
35.

Nuclear receptors: one big family.

McEwan IJ.

Methods Mol Biol. 2009;505:3-18. doi: 10.1007/978-1-60327-575-0_1. Review.

PMID:
19117136
36.

Consequences of poly-glutamine repeat length for the conformation and folding of the androgen receptor amino-terminal domain.

Davies P, Watt K, Kelly SM, Clark C, Price NC, McEwan IJ.

J Mol Endocrinol. 2008 Nov;41(5):301-14. doi: 10.1677/JME-08-0042. Epub 2008 Sep 1.

PMID:
18762554
37.
39.
40.

Structural dynamics of the human androgen receptor: implications for prostate cancer and neurodegenerative disease.

Duff J, Davies P, Watt K, McEwan IJ.

Biochem Soc Trans. 2006 Dec;34(Pt 6):1098-102.

PMID:
17073759
42.

The role of the general transcription factor IIF in androgen receptor-dependent transcription.

Choudhry MA, Ball A, McEwan IJ.

Mol Endocrinol. 2006 Sep;20(9):2052-61. Epub 2006 Apr 27.

PMID:
16645039
43.
44.
46.

Induced alpha-helix structure in the aryl hydrocarbon receptor transactivation domain modulates protein-protein interactions.

Watt K, Jess TJ, Kelly SM, Price NC, McEwan IJ.

Biochemistry. 2005 Jan 18;44(2):734-43.

PMID:
15641800
47.

In vitro regulation of reporter gene transcription by the androgen receptor AF1 domain.

Choudhry MA, McEwan IJ.

Biochem Soc Trans. 2004 Dec;32(Pt 6):1103-6.

PMID:
15506979
48.
49.
50.

Induced alpha-helix structure in AF1 of the androgen receptor upon binding transcription factor TFIIF.

Kumar R, Betney R, Li J, Thompson EB, McEwan IJ.

Biochemistry. 2004 Mar 23;43(11):3008-13.

PMID:
15023052

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