Androgen receptor: Past, present and future

Current Drug Targets

Volumn 14, Issue 4, 2013, Pages 401-407

  Schmidt, Lucy J ^a   Tindall, Donald J ^a,b  

^a MAYO CLINIC   (United States)

^b MAYO GRADUATE SCHOOL   (United States)

Author keywords

Androgen deprivation therapy; Androgen receptor; Castration recurrent prostate cancer

Indexed keywords

ANDROGEN; ANDROGEN RECEPTOR; E1A ASSOCIATED P300 PROTEIN; ENZALUTAMIDE; EPIDERMAL GROWTH FACTOR; GONADORELIN AGONIST; GONADORELIN ANTAGONIST; HEAT SHOCK PROTEIN 70; HEAT SHOCK PROTEIN 90; INTERLEUKIN 4; INTERLEUKIN 6; KERATINOCYTE GROWTH FACTOR; MESSENGER RNA; MINALRESTAT; MITOGEN ACTIVATED PROTEIN KINASE; SOMATOMEDIN; STEROID 5ALPHA REDUCTASE 1; TRANSCRIPTOME;

ANDROGEN DEPRIVATION THERAPY; ARTICLE; CANCER GROWTH; CANCER PREVENTION; CHROMATIN IMMUNOPRECIPITATION; COMPARATIVE GENOMIC HYBRIDIZATION; DISEASE COURSE; FLUORESCENCE IN SITU HYBRIDIZATION; GENE AMPLIFICATION; GENE DOSAGE; GENE EXPRESSION; GENETIC ASSOCIATION; HISTONE ACETYLATION; HUMAN; MICROARRAY ANALYSIS; MISSENSE MUTATION; PHOSPHORYLATION; PROSTATE CANCER; PROSTATE TUMOR; PROTEIN EXPRESSION; SINGLE NUCLEOTIDE POLYMORPHISM; SUMOYLATION; SURVIVAL TIME; TRANSACTIVATION; UBIQUITINATION; X RAY CRYSTALLOGRAPHY;

ANDROGEN ANTAGONISTS; ANDROGENS; ANIMALS; GENOME-WIDE ASSOCIATION STUDY; HUMANS; MALE; MUTATION; PROSTATIC NEOPLASMS; RECEPTORS, ANDROGEN; SIGNAL TRANSDUCTION;

EID: 84876699857     PISSN: 13894501     EISSN: 18735592     Source Type: Journal    
DOI: 10.2174/1389450111314040002     Document Type: Article

References (80)

1. Huggins C, Hodges C. Studies on Prostatic Cancer I. The effect of Castration, of Estrogen and of Androgen Injection on Serum Phosphatases in Metastatic Carcinoma of the Prostate. Cancer Res 1941; 1(4): 293-7.
2. Huggins C, Clark PJ. Quantitative Studies of Prostatic Secretion: II. The Effect of Castration and of Estrogen Injection on the Normal and on the Hyperplastic Prostate Glands of Dogs. J Exp Med 1940; 72(6): 747-62.
3. Huggins C. Effect of Orchiectomy and Irradiation on Cancer of the Prostate. Ann Surg 1942; 115(6): 1192-200.
4. Huggins C. Endocrine Control of Prostatic Cancer. Science 1943; 97(2529): 541-4.
5. Huggins C. The Diagnosis of Cancer of the Prostate Including the Interpretation of Serum Phosphatase Values. Bull N Y Acad Med 1943; 19(3): 195-200.
6. Huggins C. The Treatment of Cancer of the Prostate: (The 1943 Address in Surgery before the Royal College of Physicians and Surgeons of Canada). Can Med Assoc J 1944; 50(4): 301-7.
7. Huggins C. Control of cancers of man by endocrinologic methods; a review. Cancer Res 1956; 16(9): 825-30.
8. Lakey WH, Bruchovsky N, Callaway T, et al. Androgen receptors in benign and malignant prostatic tissue. Trans Am Assoc Genitourin Surg 1979; 71: 19-22.
9. Liao S, Witte D. Autoimmune anti-androgen-receptor antibodies in human serum. Proc Natl Acad Sci USA 1985; 82(24): 8345-8.
10. Young CY, Murthy LR, Prescott JL, et al. Monoclonal antibodies against the androgen receptor: recognition of human and other mammalian androgen receptors. Endocrinology 1988; 123(1): 601-10.
11. Chang CS, Kokontis J, Liao ST. Molecular cloning of human and rat complementary DNA encoding androgen receptors. Science 1988; 240(4850): 324-6.
12. Lubahn DB, Joseph DR, Sullivan PM, Willard HF, French FS, Wilson EM. Cloning of human androgen receptor complementary DNA and localization to the X chromosome. Science 1988; 240(4850): 327-30.
13. Isaacs JT, Coffey DS. Adaptation versus selection as the mechanism responsible for the relapse of prostatic cancer to androgen ablation therapy as studied in the Dunning R-3327-H adenocarcinoma. Cancer Res 1981; 41(12 Pt 1): 5070-5.
14. Scher HI, Sawyers CL. Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis. J Clin Oncol 2005; 23(32): 8253-61.
15. Dehm SM, Regan KM, Schmidt LJ, Tindall DJ. Selective role of an NH2-terminal WxxLF motif for aberrant androgen receptor activation in androgen depletion independent prostate cancer cells. Cancer Res 2007; 67(20): 10067-77.
16. Zhou ZX, Lane MV, Kemppainen JA, French FS, Wilson EM. Specificity of ligand-dependent androgen receptor stabilization: receptor domain interactions influence ligand dissociation and receptor stability. Mol Endocrinol 1995; 9(2): 208-18.
17. Debes JD, Comuzzi B, Schmidt LJ, Dehm SM, Culig Z, Tindall DJ. p300 regulates androgen receptor-independent expression of prostate-specific antigen in prostate cancer cells treated chronically with interleukin-6. Cancer Res 2005; 65(13): 5965-73.
18. Heemers HV, Sebo TJ, Debes JD, et al. Androgen deprivation increases p300 expression in prostate cancer cells. Cancer Res 2007; 67(7): 3422-30.
19. Heemers HV, Regan KM, Schmidt LJ, Anderson SK, Ballman KV, Tindall DJ. Androgen modulation of coregulator expression in prostate cancer cells. Mol Endocrinol 2009; 23(4): 572-83.
20. Zou JX, Guo L, Revenko AS, et al. Androgen-induced coactivator ANCCA mediates specific androgen receptor signaling in prostate cancer. Cancer Res 2009; 69(8): 3339-46.
21. Bouchal J, Santer FR, Hoschele PP, Tomastikova E, Neuwirt H, Culig Z. Transcriptional coactivators p300 and CBP stimulate estrogen receptor-beta signaling and regulate cellular events in prostate cancer. Prostate 2011; 71(4): 431-7.
22. Shiota M, Yokomizo A, Fujimoto N, Naito S. Androgen receptor cofactors in prostate cancer: potential therapeutic targets of castration-resistant prostate cancer. Curr Cancer Drug Targets 2011; 11(7): 870-81.
23. Debes JD, Sebo TJ, Lohse CM, Murphy LM, Haugen DA, Tindall DJ. p300 in prostate cancer proliferation and progression. Cancer Res 2003; 63(22): 7638-40.
24. Veldscholte J, Ris-Stalpers C, Kuiper GG, et al. A mutation in the ligand binding domain of the androgen receptor of human LNCaP cells affects steroid binding characteristics and response to antiandrogens. Biochem Biophys Res Commun 1990; 173(2): 534-40.
25. Gaddipati JP, McLeod DG, Heidenberg HB, et al. Frequent detection of codon 877 mutation in the androgen receptor gene in advanced prostate cancers. Cancer Res 1994; 54(11): 2861-4.
26. Elo JP, Kvist L, Leinonen K, et al. Mutated human androgen receptor gene detected in a prostatic cancer patient is also activated by estradiol. J Clin Endocrinol Metab 1995; 80(12): 3494-500.
27. Culig Z, Hobisch A, Cronauer MV, et al. Mutant androgen receptor detected in an advanced-stage prostatic carcinoma is activated by adrenal androgens and progesterone. Mol Endocrinol 1993; 7(12): 1541-50.
28. Hyytinen ER, Haapala K, Thompson J, et al. Pattern of somatic androgen receptor gene mutations in patients with hormonerefractory prostate cancer. Lab Invest 2002; 82(11): 1591-8.
29. Sun S, Luo F, Zhou Z, Wu W. A novel androgen receptor gene mutation in a Chinese patient with complete androgen insensitivity syndrome. Eur J Obstet Gynecol Reprod Biol 2010; 153(2): 173-5.
30. Gottlieb B, Beitel LK, Wu JH, Trifiro M. The androgen receptor gene mutations database (ARDB): 2004 update. Hum Mutat 2004; 23(6): 527-33.
31. Beltran H, Yelensky R, Frampton GM, et al. Targeted nextgeneration sequencing of advanced prostate cancer identifies potential therapeutic targets and disease heterogeneity. Eur Urol 2012. [Epub ahead of print].
32. Taplin ME, Rajeshkumar B, Halabi S, et al. Androgen receptor mutations in androgen-in dependent prostate cancer: Cancer and Leukemia Group B Study 9663. J Clin Oncol 2003; 21(14): 2673-8.
33. Visakorpi T, Hyytinen E, Koivisto P, et al. In vivo amplification of the androgen receptor gene and progression of human prostate cancer. Nat Genet 1995; 9(4): 401-6.
34. Kaltz-Wittmer C, Klenk U, Glaessgen A, et al. FISH analysis of gene aberrations (MYC, CCND1, ERBB2, RB, and AR) in advanced prostatic carcinomas before and after androgen deprivation therapy. Lab Invest 2000; 80(9): 1455-64.
35. Miyoshi Y, Uemura H, Fujinami K, et al. Fluorescence in situ hybridization evaluation of c-myc and androgen receptor gene amplification and chromosomal anomalies in prostate cancer in Japanese patients. Prostate 2000; 43(3): 225-32.
36. Brown RS, Edwards J, Dogan A, et al. Amplification of the androgen receptor gene in bone metastases from hormonerefractory prostate cancer. J Pathol 2002; 198(2): 237-44.
37. Edwards J, Krishna NS, Grigor KM, Bartlett JM. Androgen receptor gene amplification and protein expression in hormone refractory prostate cancer. Br J Cancer 2003; 89(3): 552-6.
38. Holzbeierlein J, Lal P, LaTulippe E, et al. Gene expression analysis of human prostate carcinoma during hormonal therapy identifies androgen-responsive genes and mechanisms of therapy resistance. Am J Pathol 2004; 164(1): 217-27.
39. Stanbrough M, Bubley GJ, Ross K, et al. Increased expression of genes converting adrenal androgens to testosterone in androgenindependent prostate cancer. Cancer Res 2006; 66(5): 2815-25.
40. Chen CD, Welsbie DS, Tran C, et al. Molecular determinants of resistance to antiandrogen therapy. Nat Med 2004; 10(1): 33-9.
41. Gregory CW, Hamil KG, Kim D, et al. Androgen receptor expression in androgen-independent prostate cancer is associated with increased expression of androgen-regulated genes. Cancer Res 1998; 58(24): 5718-24.
42. Zegarra-Moro OL, Schmidt LJ, Huang H, Tindall DJ. Disruption of androgen receptor function inhibits proliferation of androgenrefractory prostate cancer cells. Cancer Res 2002; 62(4): 1008-13.
43. Mostaghel EA, Page ST, Lin DW, et al. Intraprostatic androgens and androgen-regulated gene expression persist after testosterone suppression: therapeutic implications for castration-resistant prostate cancer. Cancer Res 2007; 67(10): 5033-41.
44. 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): 5469-77.
45. Guo Z, Yang X, Sun F, 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): 2305-13.
46. Hu R, Dunn TA, Wei S, 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.
47. Sun S, Sprenger CC, Vessella RL, et al. Castration resistance in human prostate cancer is conferred by a frequently occurring androgen receptor splice variant. J Clin Invest 2010; 120(8): 2715-30.
48. Dehm SM, Tindall DJ. Alternatively spliced androgen receptor variants. Endocr Relat Cancer. 2011; 18(5): R183-96.
49. Haile S, Sadar MD. Androgen receptor and its splice variants in prostate cancer. Cell Mol Life Sci 2011; 68(24): 3971-81.
50. Hornberg E, Ylitalo EB, Crnalic S, 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.
51. Li Y, Alsagabi M, Fan D, Bova GS, Tewfik AH, Dehm SM. Intragenic rearrangement and altered RNA splicing of the androgen receptor in a cell-based model of prostate cancer progression. Cancer Res 2011; 71(6): 2108-17.
52. Zhang X, Morrissey C, Sun S, et al. Androgen receptor variants occur frequently in castration resistant prostate cancer metastases. PLoS One 2011; 6(11): e27970.
53. Chan SC, Li Y, Dehm SM. Androgen receptor splice variants activate androgen receptor target genes and support aberrant prostate cancer cell growth independent of canonical androgen receptor nuclear localization signal. J Biol Chem 2012; 287(23): 19736-49.
54. Li Y, Hwang TH, Oseth LA, et al. AR intragenic deletions linked to androgen receptor splice variant expression and activity in models of prostate cancer progression. Oncogene 2012; 31(45): 4759-67.
55. Dehm SM, Tindall DJ. Molecular regulation of androgen action in prostate cancer. J Cell Biochem. 2006; 99(2): 333-44.
56. Takayama K, Tsutsumi S, Katayama S, et al. Integration of cap analysis of gene expression and chromatin immunoprecipitation analysis on array reveals genome-wide androgen receptor signaling in prostate cancer cells. Oncogene 2011; 30(5): 619-30.
57. Heemers HV, Tindall DJ. Androgen receptor (AR) coregulators: a diversity of functions converging on and regulating the AR transcriptional complex. Endocr Rev 2007; 28(7): 778-808.
58. Lee SO, Chun JY, Nadiminty N, Lou W, Feng S, Gao AC. Interleukin-4 activates androgen receptor through CBP/p300. Prostate 2009; 69(2): 126-32.
59. Grosdidier S, Carbo LR, Buzon V, et al. Allosteric conversation in the androgen receptor ligand-binding domain surfaces. Mol Endocrinol. 2012; 26(7): 1078-90.
60. Soulitzis N, Karyotis I, Delakas D, Spandidos DA. Expression analysis of peptide growth factors VEGF, FGF2, TGFB1, EGF and IGF1 in prostate cancer and benign prostatic hyperplasia. Int J Oncol 2006; 29(2): 305-14.
61. Wu Y, Zhao W, Zhao J, et al. Identification of androgen response elements in the insulin-like growth factor I upstream promoter. Endocrinology 2007; 148(6): 2984-93.
62. Huang YW, Wang LS, Chang HL, et al. Effect of keratinocyte growth factor on cell viability in primary cultured human prostate cancer stromal cells. J Steroid Biochem Mol Biol 2006; 100(1-3): 24-33.
63. Hobisch A, Eder IE, Putz T, et al. Interleukin-6 regulates prostatespecific protein expression in prostate carcinoma cells by activation of the androgen receptor. Cancer Res. 1998; 58(20): 4640-5.
64. Debes JD, Schmidt LJ, Huang H, Tindall DJ. p300 mediates androgen-independent transactivation of the androgen receptor by interleukin 6. Cancer Res 2002; 62(20): 5632-6.
65. Foradori CD, Weiser MJ, Handa RJ. Non-genomic actions of androgens. Front Neuroendocrinol 2008; 29(2): 169-81.
66. Sharifi N, Auchus RJ. Steroid biosynthesis and prostate cancer. Steroids 2012; 77(7): 719-26.
67. Chang KH, Li R, Papari-Zareei M, et al. Dihydrotestosterone synthesis bypasses testosterone to drive castration-resistant prostate cancer. Proc Natl Acad Sci USA 2011; 108(33): 13728-33.
68. Mohler JL, Titus MA, Bai S, et al. Activation of the androgen receptor by intratumoral bioconversion of androstanediol to dihydrotestosterone in prostate cancer. Cancer Res 2011; 71(4): 1486-96.
69. Garcia JA, Rini BI. Castration-resistant prostate cancer: many treatments, many options, many challenges ahead. Cancer 2012; 118(10): 2583-93.
70. Haapala K, Hyytinen ER, Roiha M, et al. Androgen receptor alterations in prostate cancer relapsed during a combined androgen blockade by orchiectomy and bicalutamide. Lab Invest 2001; 81(12): 1647-51.
71. Hara T, Miyazaki J, Araki H, et al. Novel mutations of androgen receptor: a possible mechanism of bicalutamide withdrawal syndrome. Cancer Res 2003; 63(1): 149-53.
72. Attard G, Reid AH, Auchus RJ, et al. Clinical and biochemical consequences of CYP17A1 inhibition with abiraterone given with and without exogenous glucocorticoids in castrate men with advanced prostate cancer. J Clin Endocrinol Metab 2012; 97(2): 507-16.
73. Sadar MD. Advances in small molecule inhibitors of androgen receptor for the treatment of advanced prostate cancer. World J Urol 2012; 30(3): 311-8.
74. Sadar MD. Small molecule inhibitors targeting the "achilles' heel" of androgen receptor activity. Cancer Res 2011; 71(4): 1208-13.
75. Hindorff LA, Gillanders EM, Manolio TA. Genetic architecture of cancer and other complex diseases: lessons learned and future directions. Carcinogenesis 2011; 32(7): 945-54.
76. Kader AK, Sun J, Isaacs SD, et al. Individual and cumulative effect of prostate cancer risk-associated variants on clinicopathologic variables in 5,895 prostate cancer patients. Prostate 2009; 69(11): 1195-205.
77. Penney KL, Pyne S, Schumacher FR, et al. Genome-wide association study of prostate cancer mortality. Cancer Epidemiol Biomarkers Prev 2010; 19(11): 2869-76.
78. Xu J, Zheng SL, Isaacs SD, et al. Inherited genetic variant predisposes to aggressive but not indolent prostate cancer. Proc Natl Acad Sci USA 2010; 107(5): 2136-40.
79. Feng J, Sun J, Kim ST, et al. A genome-wide survey over the ChIP-on-chip identified androgen receptor-binding genomic regions identifies a novel prostate cancer susceptibility locus at 12q13.13. Cancer Epidemiol Biomarkers Prev 2011; 20(11): 2396-403.
80. Wu C, Wyatt AW, Lapuk AV, et al. Integrated genome and transcriptome sequencing identifies a novel form of hybrid and aggressive prostate cancer. J Pathol 2012; 227(1): 53-61.