An imaging agent to detect androgen receptor and its active splice variants in prostate cancer

JCI Insight

Volumn 1, Issue 11, 2016, Pages

  Imamura, Yusuke ^a   Tien, Amy H ^a   Pan, Jinhe ^a   Leung, Jacky K ^a   Banuelos, Carmen A ^a   Jian, Kunzhong ^b   Wang, Jun ^a   Mawji, Nasrin R ^a   Fernandez, Javier Garcia ^b   Lin, Kuo Shyan ^a   Andersen, Raymond J ^b   Sadar, Marianne D ^a  

^a BRITISH COLUMBIA CANCER AGENCY   (Canada)

^b UNIVERSITY OF BRITISH COLUMBIA   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 85019817851     PISSN: None     EISSN: 23793708     Source Type: Journal    
DOI: 10.1172/jci.insight.87850     Document Type: Article

References (38)

1. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet. 2010;375(9724):1437–1446.
2. Scher HI, et al. Increased survival with enzalutamide in prostate cancer after chemotherapy. N Engl J Med. 2012;367(13):1187–1197.
3. de Bono JS, et al. Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med. 2011;364(21):1995–2005.
4. Ryan CJ, et al. Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med. 2013;368(2):138–148.
5. Antonarakis ES, et al. AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer. N Engl J Med. 2014;371(11):1028–1038.
6. Nadiminty N, et al. NF-kappaB2/p52 induces resistance to enzalutamide in prostate cancer: role of androgen receptor and its variants. Mol Cancer Ther. 2013;12(8):1629–1637.
7. Mostaghel EA, et al. Resistance to CYP17A1 inhibition with abiraterone in castration-resistant prostate cancer: induction of steroidogenesis and androgen receptor splice variants. Clin Cancer Res. 2011;17(18):5913–5925.
8. Jenster G, van der Korput HA, van Vroonhoven C, van der Kwast TH, Trapman J, Brinkmann AO. Domains of the human androgen receptor involved in steroid binding, transcriptional activation, and subcellular localization. Mol Endocrinol. 1991;5(10):1396–1404.
9. Rundlett SE, Wu XP, Miesfeld RL. Functional characterizations of the androgen receptor confirm that the molecular basis of androgen action is transcriptional regulation. Mol Endocrinol. 1990;4(5):708–714.
10. Simental JA, Sar M, Lane MV, French FS, Wilson EM. Transcriptional activation and nuclear targeting signals of the human androgen receptor. J Biol Chem. 1991;266(1):510–518.
11. Guo Z, et al. A novel androgen receptor splice variant is up-regulated during prostate cancer progression and promotes androgen depletion-resistant growth. Cancer Res. 2009;69(6):2305–2313.
12. Hu R, et al. Distinct transcriptional programs mediated by the ligand-dependent full-length androgen receptor and its splice variants in castration-resistant prostate cancer. Cancer Res. 2012;72(14):3457–3462.
13. Li Y, Chan CS, Brand LJ, Hwang TH, Silverstein KA, Dehm SM. Androgen receptor splice variants mediate enzalutamide resistance in castration-resistant prostate cancer cell lines. Cancer Res. 2013;73(2):483–489.
14. Hu R, et al. Ligand-independent androgen receptor variants derived from splicing of cryptic exons signify hormone-refractory prostate cancer. Cancer Res. 2009;69(1):16–22.
15. Dehm SM, Schmidt LJ, Heemers HV, Vessella RL, Tindall DJ. Splicing of a novel androgen receptor exon generates a constitutively active androgen receptor that mediates prostate cancer therapy resistance. Cancer Res. 2008;68(13):5469–5477.
16. Hörnberg E, et al. Expression of androgen receptor splice variants in prostate cancer bone metastases is associated with castration-resistance and short survival. PLoS ONE. 2011;6(4):e19059.
17. Haile S, Sadar MD. Androgen receptor and its splice variants in prostate cancer. Cell Mol Life Sci. 2011;68(24):3971–3981.
18. Antonarakis ES, et al. Androgen Receptor Splice Variant 7 and Efficacy of Taxane Chemotherapy in Patients With Metastatic Castration-Resistant Prostate Cancer. JAMA Oncol. 2015;1(5):582–591.
19. Dawson SJ, et al. Analysis of circulating tumor DNA to monitor metastatic breast cancer. N Engl J Med. 2013;368(13):1199–1209.
20. Haber DA, Velculescu VE. Blood-based analyses of cancer: circulating tumor cells and circulating tumor DNA. Cancer Discov. 2014;4(6):650–661.
21. Hu DG, et al. Identification of androgen receptor splice variant transcripts in breast cancer cell lines and human tissues. Horm Cancer. 2014;5(2):61–71.
22. Andersen RJ, et al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010;17(6):535–546.
23. Myung JK, et al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest. 2013;123(7):2948–2960.
24. De Mol E, et al. EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor [published online ahead of print June 29, 2016]. ACS Chem Biol. doi:10.1021/acschembio.6b00182.
25. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009;324(5928):787–790.
26. Sun S, et al. Castration resistance in human prostate cancer is conferred by a frequently occurring androgen receptor splice variant. J Clin Invest. 2010;120(8):2715–2730.
27. Zhang X, et al. Androgen receptor variants occur frequently in castration resistant prostate cancer metastases. PLoS ONE. 2011;6(11):e27970.
28. Yang YC, et al. Targeting androgen receptor activation function-1 with EPI to overcome resistance mechanisms in castration-resistant prostate cancer [published online ahead of print May 2, 2016]. Clin Cancer Res. doi:10.1158/1078-0432.CCR-15-2901.
29. Banuelos CA, et al. Characterization of niphatenones that inhibit androgen receptor N-terminal domain. PLoS ONE. 2014;9(9):e107991.
30. Liu A, Dence CS, Welch MJ, Katzenellenbogen JA. Fluorine-18-labeled androgens: radiochemical synthesis and tissue distribution studies on six fluorine-substituted androgens, potential imaging agents for prostatic cancer. J Nucl Med. 1992;33(5):724–734.
31. Bonasera TA, et al. Preclinical evaluation of fluorine-18-labeled androgen receptor ligands in baboons. J Nucl Med. 1996;37(6):1009–1015.
32. Pond GR, Sonpavde G, de Wit R, Eisenberger MA, Tannock IF, Armstrong AJ. The prognostic importance of metastatic site in men with metastatic castration-resistant prostate cancer. Eur Urol. 2014;65(1):3–6.
33. Goodman OB Jr, et al. Exploratory analysis of the visceral disease subgroup in a phase III study of abiraterone acetate in metastatic castration-resistant prostate cancer. Prostate Cancer Prostatic Dis. 2014;17(1):34–39.
34. Evans CP, et al. The PREVAIL Study: Primary Outcomes by Site Extent of Baseline Disease for Enzalutamide-treated Men with Chemotherapy-naive Metastatic Castration-resistant Prostate Cancer [published online ahead of print March 19, 2016]. Eur Urol. 2016;S0302-2838(16):00274–00278. doi:10.1016/j.eururo.2016.03.017.
35. Larson SM, et al. Tumor localization of 16beta-18F-fluoro-5alpha-dihydrotestosterone versus 18F-FDG in patients with progressive, metastatic prostate cancer. J Nucl Med. 2004;45(3):366–373.
36. Liu LL, Xie N, Sun S, Plymate S, Mostaghel E, Dong X. Mechanisms of the androgen receptor splicing in prostate cancer cells. Oncogene. 2014;33(24):3140–3150.
37. Yang YC, et al. Spongian diterpenoids inhibit androgen receptor activity. Mol Cancer Ther. 2013;12(5):621–631.
38. Reid J, Kelly SM, Watt K, Price NC, McEwan IJ. Conformational analysis of the androgen receptor amino-terminal domain involved in transactivation. Influence of structure-stabilizing solutes and protein-protein interactions. J Biol Chem. 2002;277(22):20079–20086.