Androgen Receptor Mutations in Carcinoma of the Prostate: Significance for Endocrine Therapy
Abstract
Endocrine therapy for advanced prostate cancer involves androgen ablation (orchiectomy or application of luteinizing hormone releasing hormone analogs) and/or blockade of the androgen receptor (AR) with either steroidal (cyproterone acetate) or nonsteroidal (hydroxyflutamide, bicalutamide and nilutamide) antiandrogens. These antagonists prevent androgen-induced conformational change and activation of the AR. During long term androgen ablation, the AR adapts to an environment with low androgen concentrations and becomes hypersensitive to low concentrations of androgens, either alone or in combination with various cellular regulators. Bicalutamide can switch from antagonist to agonist during long-term androgen withdrawal, as shown in prostate cancer LNCaP cells. AR point mutations were detected in metastatic lesions from human prostate cancer more frequently than in primary tumors. Although functional characterization of only some mutant AR detected in prostate cancer tissue has been performed, data available suggest that they are activated by dihydrotestosterone, its precursors and metabolites, synthetic androgens, estrogenic and progestagenic steroids and hydroxyflutamide. A direct association between AR mutations and endocrine withdrawal syndrome has been investigated in only one study thus far. There is no evidence at present that activation of any of the mutant AR genes detected in prostate cancer is enhanced in the presence of a nonsteroidal AR stimulator. Coactivators of the AR are proteins that associate with the receptor, possess histone acetylase activity and facilitate AR activation. The coregulatory proteins ARA70 and ARA160 differentially affected the activity of the mutated AR Glu(231)-->Gly, which was discovered in a mouse authochthonous prostate tumor. ARA70 enhanced receptor activation by both androgen and estradiol, whereas ARA160 augmented only androgen-induced AR activity. Novel experimental therapies that down-regulate AR expression have been developed; they include the application of ribozymes and antisense oligonucleotides.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Approximately 70 different missense mutations have been described in patient samples, with varying consequences upon androgen receptor activity.
“Approximately 70 different missense mutations have been described in patient samples, with varying consequences upon AR activity.”
From Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer (2011) · cites this paper as [72]
Cites
Huggins, C., & Hodges, C. V. (2002) · The Journal of Urology · doi:10.1016/s0022-5347(05)64820-3 · Cited by 3,856 · see citing works
LNCaP model of human prostatic carcinoma.
Horoszewicz, J. S., Leong, S. S., Kawinski, E., Karr, J. P., Rosenthal, H. E., Chu, T. M., MIRAND, E. A., & Murphy, G. P. (1983) · PubMed · Cited by 1,768 · see citing works
In vivo amplification of the androgen receptor gene and progression of human prostate cancer
Visakorpi, T., Hyytinen, E., Koivisto, P., Tanner, M., Keinänen, R., Palmberg, C., Palotie, A., Tammela, T., Isola, J., & Kallioniemi, O.-P. (1995) · Nature Genetics · doi:10.1038/ng0495-401 · Cited by 1,484 · see citing works
Mutation of the Androgen-Receptor Gene in Metastatic Androgen-Independent Prostate Cancer
Taplin, M., Bubley, G. J., Shuster, T. D., Frantz, M. E., Spooner, A. E., Ogata, G. K., Keer, H. N., & Balk, S. P. (1995) · New England Journal of Medicine · doi:10.1056/nejm199505253322101 · Cited by 1,243 · see citing works
A canonical structure for the ligand-binding domain of nuclear receptors
Wurtz, J., Bourguet, W., Renaud, J., Vivat, V., Chambon, P., Moras, D., & Gronemeyer, H. (1996) · Nature Structural Biology · doi:10.1038/nsb0196-87 · Cited by 986 · see citing works
Craft, N., Shostak, Y., Carey, M., & Sawyers, C. L. (1999) · Nature Medicine · doi:10.1038/6495 · Cited by 980 · see citing works
Veldscholte, J., Ris‐Stalpers, C., Kuiper, G. G. J. M., Jenster, G. W., Berrevoets, C., Claassen, E., van Rooij, H. C. J., Trapman, J., Brinkmann, A. O., & Mulder, E. (1990) · Biochemical and Biophysical Research Communications · doi:10.1016/s0006-291x(05)80067-1 · Cited by 945 · see citing works
Čulig, Z., Hobisch, A., Cronauer, M. V., Radmayr, C., Trapman, J., Hittmair, A., Bartsch, G., & Klocker, H. (1994) · PubMed · Cited by 938 · see citing works
Self-citationAmplification and overexpression of androgen receptor gene in hormone-refractory prostate cancer.
Linja, M. J., Savinainen, K., Saramäki, O. R., Tammela, T. L. J., Vessella, R. L., & Visakorpi, T. (2001) · PubMed · Cited by 762 · see citing works
Yeh, S., & Chang, C. (1996) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.93.11.5517 · Cited by 632 · see citing works
Gregory, C. W., He, B., Johnson, R. T., Ford, O. H., Mohler, J. L., French, F. S., & Wilson, E. (2001) · PubMed · Cited by 603 · see citing works
Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist.
Taplin, M., Bubley, G. J., Ko, Y., Small, E. J., Upton, M. P., Rajeshkumar, B. R., & Balk, S. P. (1999) · PubMed · Cited by 594 · see citing works
Zhao, X.-Y., Malloy, P. J., Krishnan, A. V., Swami, S., Navone, N. M., Peehl, D. M., & Feldman, D. (2000) · Nature Medicine · doi:10.1038/76287 · Cited by 536 · see citing works
(2001) · PubMed · Cited by 500 · see citing works
The Promoter of the Prostate-Specific Antigen Gene Contains a Functional Androgen Responsive Element
Riegman, P. H. J., Vlietstra, R. J., van der Korput, J. A. G. M., Brinkmann, A. O., & Trapman, J. (1991) · Molecular Endocrinology · doi:10.1210/mend-5-12-1921 · Cited by 448 · see citing works
Čulig, Z., Hobisch, A., Cronauer, M. V., Cato, A. C. B., Hittmair, A., Radmayr, C., Eberle, J., Bartsch, G., & Klocker, H. (1993) · Molecular Endocrinology · doi:10.1210/mend.7.12.8145761 · Cited by 440 · see citing works
Self-citationHobisch, A., Eder, I. E., Putz, T., Horninger, W., Bartsch, G. C., Klocker, H., & Čulig, Z. (1998) · PubMed · Cited by 437 · see citing works
Self-citationKemppainen, J., Lane, M. V., Sar, M., & Wilson, E. M. (1992) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)48380-9 · Cited by 430 · see citing works
Activation of the human androgen receptor through a protein kinase A signaling pathway.
Nazareth, L. V., & Weigel, N. L. (1996) · Journal of Biological Chemistry · doi:10.1074/jbc.271.33.19900 · Cited by 429 · see citing works
The AF1 and AF2 Domains of the Androgen Receptor Interact with Distinct Regions of SRC1
Bevan, C. L., Hoare, S., Claessens, F., Heery, D. M., & Parker, M. G. (1999) · Molecular and Cellular Biology · doi:10.1128/mcb.19.12.8383 · Cited by 424 · see citing works
Androgen receptor gene mutations in human prostate cancer.
Newmark, J., Hardy, D. O., Tonb, D. C., Carter, B. S., Epstein, J. I., Isaacs, W. B., Brown, T. R., & Barrack, E. R. (1992) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.89.14.6319 · Cited by 415 · see citing works
Čulig, Z., Hoffmann, J., Erdel, M., Eder, I. E., Hobisch, A., Hittmair, A., Bartsch, G., Utermann, G., Schneider, M. R., Parczyk, K., et al. (1999) · British Journal of Cancer · doi:10.1038/sj.bjc.6690684 · Cited by 410 · see citing works
Self-citationFlutamide withdrawal syndrome: its impact on clinical trials in hormone-refractory prostate cancer.
Scher, H. I., & Kelly, W. K. (1993) · Journal of Clinical Oncology · doi:10.1200/jco.1993.11.8.1566 · Cited by 405 · see citing works
Tilley, W. D., Buchanan, G., Hickey, T. E., & Bentel, J. M. (1996) · PubMed · Cited by 394 · see citing works
Androgen receptors in endocrine‐therapy‐resistant human prostate cancer
van der Kwast, T., Schalken, J. A., de Winter, J. A. R., van Vroonhoven, J. C. C., Mulder, E., Boersma, W. J. A., & Trapman, J. (1991) · International Journal of Cancer · doi:10.1002/ijc.2910480206 · Cited by 387 · see citing works
Cleutjens, K. B. J. M., van der Korput, H. A. G. M., Eekelen, C. C. E.-V., van Rooij, H. C. J., Faber, P. W., & Trapman, J. (1997) · Molecular Endocrinology · doi:10.1210/mend.11.2.9883 · Cited by 375 · see citing works
Tan, J.-A., Sharief, Y., Hamil, K. G., Gregory, C. W., Zang, D.-Y., Sar, M., Gumerlock, P. H., White, R. D., Pretlow, T. G., Harris, S. E., et al. (1997) · Molecular Endocrinology · doi:10.1210/mend.11.4.9906 · Cited by 375 · see citing works
Frequent detection of codon 877 mutation in the androgen receptor gene in advanced prostate cancers.
Gaddipati, J. P., McLeod, D. G. R., Heidenberg, H. B., Sesterhenn, I. A., Finger, M. J., Moul, J. W., & Srivastava, S. (1994) · PubMed · Cited by 363 · see citing works
Androgen-independent prostate cancer progression in the TRAMP model.
Gingrich, J. R., Barrios, R. J., Kattan, M. W., Nahm, H. S., Finegold, M. J., & Greenberg, N. M. (1997) · PubMed · Cited by 362 · see citing works
Wong, C.-I., KELCE, W. R., Sar, M., & Wilson, E. M. (1995) · Journal of Biological Chemistry · doi:10.1074/jbc.270.34.19998 · Cited by 337 · see citing works
de Winter, J. A. R., Janssen, P. J. A., Sleddens, H. M., Verleun-Mooijman, M. C. T., Trapman, J., Brinkmann, A. O., Santerse, A. B., Schröder, F. H., & van der Kwast, T. (1994) · PubMed Central · Cited by 333 · see citing works
FHL2, a novel tissue‐specific coactivator of the androgen receptor
Müller, J. M., Isele, U., Metzger, E., Rempel, A., Moser, M., Pscherer, A., Breyer, T., Holubarsch, C., Buettner, R., & Schüle, R. (2000) · The EMBO Journal · doi:10.1093/emboj/19.3.359 · Cited by 326 · see citing works
Androgen receptor mutations in prostate cancer.
Barrack, E. R. (1996) · PubMed · Cited by 301 · see citing works
Distant metastases from prostatic carcinoma express androgen receptor protein.
Hobisch, A., CULIG, Z., Radmayr, C., Bartsch, G., Klocker, H., & Hittmair, A. (1995) · PubMed · Cited by 283 · see citing works
Self-citationGregory, C. W., Hamil, K. G., Kim, D., Hall, S. H., Pretlow, T. G., Mohler, J. L., & French, F. S. (1998) · PubMed · Cited by 273 · see citing works
From estrogen to androgen receptor: A new pathway for sex hormones in prostate
Yeh, S., Miyamoto, H., Shima, H., & Chang, C. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.10.5527 · Cited by 267 · see citing works
Establishment of two human prostate cancer cell lines derived from a single bone metastasis.
Navone, N. M., Olivé, M., Özen, M., Davis, R., Troncoso, P., Tu, S., Johnston, D., Pollack, A. S., Pathak, S., von Eschenbach, A. C., et al. (1997) · PubMed · Cited by 265 · see citing works
Chen, T., Wang, L. H., & Farrar, W. L. (2000) · PubMed · Cited by 258 · see citing works
Young, C. Y. F., Montgomery, B. T., Andrews, P. E., Qui, S., Bilhartz, D. L., & Tindall, D. J. (1991) · PubMed · Cited by 257 · see citing works
CREB-binding protein in androgen receptor-mediated signaling
Aarnisalo, P., Palvimo, J. J., & Jänne, O. A. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.5.2122 · Cited by 255 · see citing works
Tip60 Is a Nuclear Hormone Receptor Coactivator
Brady, M. E., Ozanne, D. M., Gaughan, L., Waite, I. S., Cook, S., Neal, D. E., & Robson, C. N. (1999) · Journal of Biological Chemistry · doi:10.1074/jbc.274.25.17599 · Cited by 254 · see citing works
Kokontis, J. M., Hay, N., & Liao, S. (1998) · Molecular Endocrinology · doi:10.1210/mend.12.7.0136 · Cited by 250 · see citing works
Kokontis, J. M., Takakura, K., Hay, N., & Liao, S. (1994) · PubMed · Cited by 248 · see citing works
Kang, H., Yeh, S., Fujimoto, N., & Chang, C. (1999) · Journal of Biological Chemistry · doi:10.1074/jbc.274.13.8570 · Cited by 230 · see citing works
Androgen receptor gene mutations in human prostate cancer
Suzuki, H., Sato, N., Watabe, Y., Masai, M., Seino, S., & Shimazaki, J. (1993) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/0960-0760(93)90316-o · Cited by 226 · see citing works
CREB Binding Protein Is a Coactivator for the Androgen Receptor and Mediates Cross-talk with AP-1
Frønsdal, K. B., Engedal, N., Slagsvold, T., & Saatcioglu, F. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.48.31853 · Cited by 223 · see citing works
Kaplan, P. J., Mohan, S., Cohen, P., Foster, B. A., & Greenberg, N. M. (1999) · PubMed · Cited by 215 · see citing works
Aberrant response in vitro of hormone‐responsive prostate cancer cells to antiandrogens
Wilding, G., Chen, M. J., & Gelmann, E. P. (1989) · The Prostate · doi:10.1002/pros.2990140204 · Cited by 205 · see citing works
Miyamoto, H., Yeh, S., Wilding, G., & Chang, C. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.13.7379 · Cited by 203 · see citing works
Montgomery, B. T., Young, C. Y. F., Bilhartz, D. L., Andrews, P. E., THOMPSON, N., Tindall, D. J., & Prescott, J. L. (1992) · The Prostate · doi:10.1002/pros.2990210107 · Cited by 177 · see citing works
Small, E. J., & Carroll, P. R. (1994) · Urology · doi:10.1016/0090-4295(94)90092-2 · Cited by 174 · see citing works
Veldscholte, J., Voorhorst‐Ogink, M. M., Vries, J. B., van Rooij, H. C. J., Trapman, J., & Mulder, E. (1990) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/0167-4889(90)90075-o · Cited by 160 · see citing works
Inhibition of LNCaP prostate cancer cells by means of androgen receptor antisense oligonucleotides
Eder, I. E., Čulig, Z., Ramoner, R. E., Thurnher, M., Putz, T., Nessler‐Menardi, C., Tiefenthaler, M., Bartsch, G. H., & Klocker, H. (2000) · Cancer Gene Therapy · doi:10.1038/sj.cgt.7700202 · Cited by 152 · see citing works
Self-citationAndrogen receptor status of lymph node metastases from prostate cancer
Hobisch, A., Čulig, Z., Radmayr, C., Bartsch, G., Klocker, H., & Hittmair, A. (1996) · The Prostate · doi:10.1002/(sici)1097-0045(199602)28:2 · Cited by 146 · see citing works
Self-citationYuan, S., Trachtenberg, J., Mills, G. B., Brown, T. J., Xu, F., & Keating, A. (1993) · PubMed · Cited by 145 · see citing works
Elo, J. P., Kvist, L. J., Leinonen, K. A., ISOMAA, V. V., Henttu, P. M. A., Lukkarinen, O. A., & Vihko, P. (1995) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jcem.80.12.8530589 · Cited by 143 · see citing works
Veldscholte, J., Berrevoets, C. A., Zegers, N. D., Van der Kwast, T. H., Grootegoed, J. A., & Mulder, E. (1992) · Biochemistry · doi:10.1021/bi00147a029 · Cited by 139 · see citing works
Schmitt, B. P., Wilt, T. J., Schellhammer, P. F., DeMasi, V., Sartor, O. A., Crawford, E. D., & Bennett, C. L. (2001) · Urology · doi:10.1016/s0090-4295(00)01086-4 · Cited by 131 · see citing works
Han, G., Foster, B. A., Mistry, S. G., Buchanan, G., Harris, J. M., Tilley, W. D., & Greenberg, N. M. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m008207200 · Cited by 123 · see citing works
Dawson, N. A., & McLeod, D. G. (1995) · The Journal of Urology · doi:10.1016/s0022-5347(01)67365-8 · Cited by 122 · see citing works
Alen, P., Claessens, F., Schoenmakers, E., Swinnen, J. V., Verhoeven, G., Rombauts, W., & Peeters, B. (1999) · Molecular Endocrinology · doi:10.1210/mend.13.1.0214 · Cited by 120 · see citing works
Čulig, Z., Klocker, H., Eberle, J., Kaspar, F., Hobisch, A., Cronauer, M. V., & Bartsch, G. H. (1993) · The Prostate · doi:10.1002/pros.2990220103 · Cited by 115 · see citing works
Self-citationZhao, X.-Y., BOYLE, B., Krishnan, A. V., Navone, N. M., Peehl, D. M., & Feldman, D. (1999) · The Journal of Urology · doi:10.1016/s0022-5347(05)68158-x · Cited by 110 · see citing works
Nazareth, L. V., Stenoien, D. L., Bingman, W. E., James, A. J., Wu, C. A., Zhang, Y., Edwards, D. P., Mancini, M. A., Marcelli, M., Lamb, D. J., et al. (1999) · Molecular Endocrinology · doi:10.1210/mend.13.12.0382 · Cited by 100 · see citing works
Sex determination and the Y chromosome
McElreavey, K., & Fellous, M. (1999) · American Journal of Medical Genetics · doi:10.1002/(sici)1096-8628(19991229)89:4 · Cited by 93 · see citing works
Evans, B. A. J., Harper, M. E., Daniells, C., Watts, C. E., Matenhelia, S. S., Green, J., & Griffiths, K. (1996) · The Prostate · doi:10.1002/(sici)1097-0045(199603)28:3 · Cited by 89 · see citing works
Gao, M., Ossowski, L., & Ferrari, A. C. (1999) · Journal of Cellular Physiology · doi:10.1002/(sici)1097-4652(199906)179:3 · Cited by 86 · see citing works
Mononen, N., Syrjäkoski, K., Matikainen, M. P., Tammela, T. L. J., Schleutker, J., Kallioniemi, O., Trapman, J., & Koivisto, P. A. (2000) · PubMed · Cited by 78 · see citing works
Peterziel, H., Čulig, Z., Stober, J., Hobisch, A., Radmayr, C., Bartsch, G. H., Klocker, H., & Cato, A. C. B. (1995) · International Journal of Cancer · doi:10.1002/ijc.2910630415 · Cited by 75 · see citing works
Self-citationSadar, M. D., & Gleave, M. E. (2000) · PubMed · Cited by 74 · see citing works
Čulig, Z., Hobisch, A., Hittmair, A., Cronauer, M. V., Radmayr, C., Zhang, J., Bartsch, G. H., & Klocker, H. (1997) · The Prostate · doi:10.1002/(sici)1097-0045(19970701)32:2 · Cited by 74 · see citing works
Self-citationRaghow, S., Kuliyev, E., Steakley, M., Greenberg, N. M., & Steiner, M. S. (2000) · PubMed · Cited by 68 · see citing works
Use of the Nonsteroidal Anti-androgen Casodex in Advanced Prostatic Carcinoma
Kennealey, G. T., & Furr, B. J. A. (1991) · Urologic Clinics of North America · doi:10.1016/s0094-0143(21)01397-5 · Cited by 65 · see citing works
Case Reports: Withdrawal Phenomenon With the Antiandrogen Casodex
Nieh, P. T., Crawford, E. D., Scher, H. I., & Kelly, W. K. (1995) · The Journal of Urology · doi:10.1016/s0022-5347(01)67644-4 · Cited by 65 · see citing works
Nieh, P. T., Crawford, E. D., Scher, H. I., & Kelly, W. K. (1995) · The Journal of Urology · doi:10.1097/00005392-199503001-00048 · Cited by 65 · see citing works
Thyroid Receptor Activator Molecule, TRAM-1, Is an Androgen Receptor Coactivator
Tan, J.-A., Hall, S. H., Petrusz, P., & French, F. S. (2000) · Endocrinology · doi:10.1210/endo.141.9.7680 · Cited by 60 · see citing works
Kallio, P. J., Jänne, O. A., & Palvimo, J. J. (1994) · Endocrinology · doi:10.1210/endo.134.2.8299593 · Cited by 59 · see citing works
Gao, T., Brantley, K., Bolu, E., & McPhaul, M. J. (1999) · Molecular Endocrinology · doi:10.1210/mend.13.10.0352 · Cited by 59 · see citing works
Phorbol ester causes ligand‐independent activation of the androgen receptor
Darné, C., VEYSSIERE, G., & Jean, C. (1998) · European Journal of Biochemistry · doi:10.1046/j.1432-1327.1998.2560541.x · Cited by 54 · see citing works
Matrilysin Expression in the Involuting Rat Ventral Prostate
Powell, W. C., Domann, F. E., MITCHEN, J. M., Matrisian, L. M., Nagle, R. B., & Bowden, G. T. (1996) · The Prostate · doi:10.1002/1097-0045(199609)29:3 · Cited by 48 · see citing works
[Androgen receptor gene mutations and p53 gene analysis in advanced prostate cancer].
Castagnaro, M., Yandell, D. W., Dockhorn‐Dworniczak, B., Wolfe, H. J., & Poremba, C. (1993) · PubMed · Cited by 46 · see citing works
Lim, J. T. S., Ghadessy, F. J., Abdullah, A. A. R., Pinsky, L., Trifiro, M. A., & Yong, E. (2000) · Molecular Endocrinology · doi:10.1210/mend.14.8.0499 · Cited by 45 · see citing works
Chen, S., Song, C. S., Lavrovsky, Y., Bi, B., Vellanoweth, R. L., Chatterjee, B., & Roy, A. K. (1998) · Molecular Endocrinology · doi:10.1210/mend.12.10.0186 · Cited by 45 · see citing works
Freeman, S., Mainwaring, W., & Furr, B. J. A. (1989) · British Journal of Cancer · doi:10.1038/bjc.1989.336 · Cited by 41 · see citing works
Akakura, K., Akimoto, S., Ohki, T., & Shimazaki, J. (1995) · Urology · doi:10.1016/s0090-4295(99)80070-3 · Cited by 35 · see citing works
Blackledge, G. R. P., Cockshott, I. D., & Furr, B. J. A. (1997) · European Urology · doi:10.1159/000474547 · Cited by 31 · see citing works
Antiandrogen Withdrawal Syndrome With Nilutamide
Gomella, L. G., Ismail, M., & Nathan, F. E. (1997) · The Journal of Urology · doi:10.1016/s0022-5347(01)64984-x · Cited by 30 · see citing works
Antiandrogen withdrawal syndrome with cyproterone acetate
Sella, A., Flex, D., Sulkes, A., & Baniel, J. (1998) · Urology · doi:10.1016/s0090-4295(98)00354-9 · Cited by 26 · see citing works
Bélanger, A., Giasson, M., Couture, J., Dupont, A., Cusan, L., & Labrie, F. (1988) · The Prostate · doi:10.1002/pros.2990120110 · Cited by 25 · see citing works
Apparent coactivation due to interference of expression constructs with nuclear receptor expression
Hofman, K., Swinnen, J. V., Claessens, F., Verhoeven, G., & Heyns, W. (2000) · Molecular and Cellular Endocrinology · doi:10.1016/s0303-7207(00)00311-7 · Cited by 20 · see citing works
Surprises with Antiprogestins: Novel Mechanisms of Progesterone Receptor Action
Horwitz, K. B., Sartorius, C. A., Hovland, A. R., Jackson, T. A., Groshong, S. D., Tung, L. W., & Takimoto, G. S. (2007) · Novartis Foundation symposium · doi:10.1002/9780470514757.ch14 · Cited by 15 · see citing works
Relative potency of bicalutamide (Casodex) and flutamide (Eulexin)
Schellhammer, P., & Fabozzi, S. (1999) · PubMed · Cited by 14 · see citing works
Estimated potency of Casodex: a problematic design.
Labrie, F., Simard, J., Singh, S. M., & Candas, B. (1997) · PubMed · Cited by 9 · see citing works
Laufer, M., Sinibaldi, V. J., Carducci, M. A., & Eisenberger, M. A. (1999) · Urology · doi:10.1016/s0090-4295(99)00268-x · Cited by 8 · see citing works
(1999) · Urology · doi:10.1016/s0090-4295(98)00474-9 · Cited by 2 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Inorganic Arsenic and Human Prostate Cancer
Benbrahim‐Tallaa, L., & Waalkes, M. P. (2007) · Environmental Health Perspectives · doi:10.1289/ehp.10423 · Cited by 194 · see citing works
Recent advances in androgen receptor action
Lee, H.-J., & Chang, C. (2003) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-003-2309-3 · Cited by 162 · see citing works
Minireview: Alternative Activation Pathways for the Androgen Receptor in Prostate Cancer
Lamont, K. R., & Tindall, D. J. (2011) · Molecular Endocrinology · doi:10.1210/me.2010-0469 · Cited by 150 · see citing works
Expression and function of androgen receptor coactivators in prostate cancer
Čulig, Z., Comuzzi, B., Steiner, H., Bartsch, G. H., & Hobisch, A. (2004) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2004.10.003 · Cited by 133 · see citing works
Self-citationShiota, M., Yokomizo, A., & Naito, S. (2011) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2011.07.011 · Cited by 124 · see citing works
Signal transduction in prostate cancer progression
Gioeli, D. G. (2005) · Clinical Science · doi:10.1042/cs20040329 · Cited by 116 · see citing works
The hallmarks of castration-resistant prostate cancers
Katsogiannou, M., Ziouziou, H., Karaki, S., Andrieu, C., de Villeneuve, M. H., & Rocchi, P. (2015) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2015.05.003 · Cited by 107 · see citing works
Molecular Mechanisms of Prostate Cancer
Porkka, K. P., & Visakorpi, T. (2004) · European Urology · doi:10.1016/j.eururo.2004.01.012 · Cited by 93 · see citing works
Comuzzi, B., Lambrinidis, L., Rogatsch, H., Godoy‐Tundidor, S., Knežević, N., Krhen, I., Mareković, Z., Bartsch, G. H., Klocker, H., Hobisch, A., et al. (2003) · American Journal Of Pathology · doi:10.1016/s0002-9440(10)63814-x · Cited by 76 · see citing works
Self-citationVertebrate Sex Steroid Receptors: Evolution, Ligands, and Neurodistribution
Guerriero, G. (2009) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.2009.04460.x · Cited by 68 · see citing works
Inorganic arsenic and human prostate cancer
Benbrahim‐Tallaa, L., & Waalkes, M. P. (2009) · Ciência & Saúde Coletiva · doi:10.1590/s1413-81232009000100037 · Cited by 65 · see citing works
Novel therapeutic approaches for the treatment of castration-resistant prostate cancer
Heidegger, I. M., Massoner, P., Eder, I. E., Pircher, A., Pichler, R., Aigner, F., Bektić, J., Horninger, W., & Klocker, H. (2013) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2013.06.002 · Cited by 43 · see citing works
Self-citationBicalutamide failure in prostate cancer treatment: Involvement of Multi Drug Resistance proteins
Colabufo, N. A., Pagliarulo, V., Berardi, F., Contino, M., Inglese, C., Niso, M., Ancona, P., Albo, G., Pagliarulo, A., & Perrone, R. (2008) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2008.10.038 · Cited by 43 · see citing works
Cholesterol as a Potential Target for Castration-Resistant Prostate Cancer
Twiddy, A. L., Leon, C. G., & Wasan, K. M. (2010) · Pharmaceutical Research · doi:10.1007/s11095-010-0210-y · Cited by 39 · see citing works
Liu, G., Wang, H., & Wang, Z. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m212229200 · Cited by 31 · see citing works
Oh, W. K., Manola, J. B., Bittmann, L., Brufsky, A., Kaplan, I. D., Smith, M. R., Kaufman, D. S., & Kantoff, P. W. (2003) · Urology · doi:10.1016/s0090-4295(03)00145-6 · Cited by 29 · see citing works
Genetic changes and DNA damage responses in the prostate
af Hällström, T., & Laiho, M. (2008) · The Prostate · doi:10.1002/pros.20746 · Cited by 27 · see citing works
Voet, A. R. D., Helsen, C., Zhang, K. Y. J., & Claessens, F. (2013) · ChemMedChem · doi:10.1002/cmdc.201200549 · Cited by 27 · see citing works
Androgens and androgen receptor in prostate and ovarian malignancies
Sadar, M. D. (2003) · Frontiers in bioscience · doi:10.2741/1063 · Cited by 26 · see citing works
Livin‐α promotes cell proliferation by regulating G1‐S cell cycle transition in prostate cancer
Ye, L., Song, X., Li, S., Yang, D., Zhang, J., Che, X., Chen, X., Wang, J., & Zhang, Z. (2010) · The Prostate · doi:10.1002/pros.21220 · Cited by 22 · see citing works
Saito, S., Fujimaki, T., Panbangred, W., Igarashi, Y., & Imoto, M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201510079 · Cited by 18 · see citing works
Krishnan, A. V., Peehl, D. M., & Feldman, D. (2005) · Elsevier eBooks · doi:10.1016/b978-012252687-9/50098-x · Cited by 18 · see citing works
Lotfy, K. (2015) · Journal of Biophysical Chemistry · doi:10.4236/jbpc.2015.64010 · Cited by 15 · see citing works
Prosaposin is a novel androgen‐regulated gene in prostate cancer cell line LNCaP
Koochekpour, S., Lee, T. ‐., Wang, R., Sun, Y., Delorme, N., Hiraiwa, M., Grabowski, G. A., Čulig, Z., & Minokadeh, A. (2006) · Journal of Cellular Biochemistry · doi:10.1002/jcb.21207 · Cited by 15 · see citing works
Helsen, C., Marchand, A., Chaltin, P., Munck, S., Voet, A. R. D., Verstuyf, A., & Claessens, F. (2012) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-11-0763 · Cited by 13 · see citing works
The androgen receptor: molecular biology
Klocker, H., Gromoll, J., & Cato, A. C. B. (2001) · Cambridge University Press eBooks · doi:10.1017/cbo9780511545221.003 · Cited by 12 · see citing works
Self-citationWang, Z., Xu, D., Gao, Y., Liu, Y., Ren, J., Yao, Y., Yin, L., Chen, J., Gan, S., & Cui, X.-G. (2015) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/cbr.2014.1728 · Cited by 10 · see citing works
RetractedCyproterone acetate acts as a disruptor of the aryl hydrocarbon receptor
Cheng, C., Gao, G.-L., Ho, D., Lin, C.-Y. G., Chou, Y.-T., Chen, S.-C., Huang, M., Kao, W.-Y., & Su, J.-G. J. (2021) · Scientific Reports · doi:10.1038/s41598-021-84769-7 · Cited by 8 · see citing works
Molecular markers in prostate cancer. Part I: predicting lethality
Agrawal, S., & Dunsmuir, W. D. (2008) · Asian Journal of Andrology · doi:10.1038/aja.2008.20 · Cited by 8 · see citing works
Molecular Genetics and Cancer Biology
Gonzalgo, M. L., & Meeker, A. K. (2012) · Elsevier eBooks · doi:10.1016/b978-1-4160-6911-9.00018-9 · Cited by 5 · see citing works
Non-androgen Signaling Pathways in Castration-Resistant Prostate Cancer
Sittadjody, S., Thangasamy, T., NickKolgh, B., & Balaji, K. C. (2016) · Springer eBooks · doi:10.1007/978-3-319-31341-2_4 · Cited by 4 · see citing works
Krishnan, A. V., & Feldman, D. (2011) · Elsevier eBooks · doi:10.1016/b978-0-12-381978-9.10086-1 · Cited by 4 · see citing works
Cell Biology of Prostate Cancer and Molecular Targets
Gleave, M. E., Cox, M., & Wang, Y. Z. (2010) · Springer eBooks · doi:10.1007/978-1-60327-829-4_1 · Cited by 3 · see citing works
Signal Transduction by the Ras–MAP Kinase Pathway in Prostate Cancer Progression
Gioeli, D. G., Kraus, S. R., & Weber, M. J. (2008) · Humana Press eBooks · doi:10.1007/978-1-60327-079-3_11 · Cited by 3 · see citing works
Saito, S., Fujimaki, T., Panbangred, W., Igarashi, Y., & Imoto, M. (2016) · Angewandte Chemie · doi:10.1002/ange.201510079 · Cited by 2 · see citing works
Murti, K., Butler, L. M., Sakko, A. J., Ricciardelli, C., Mitto, T. B., Octnick, A., Stahl, J., & Tilley, W. D. (2010) · Medical Journal of Indonesia · doi:10.13181/mji.v19i1.376 · Cited by 2 · see citing works
Mathematical modeling of intracrine androgen metabolism in prostate cancer: Methodological aspects
Cook, S. F., Fiandalo, M. V., Watt, D. S., Wu, Y., Mohler, J. L., & Bies, R. R. (2018) · The Prostate · doi:10.1002/pros.23665 · Cited by 2 · see citing works
Somatic Molecular Genetics of Prostate Cancer
Humbert, L., & Chevrette, M. (2009) · Springer eBooks · doi:10.1007/978-1-4419-0449-2_5 · Cited by 2 · see citing works
Genetic Alterations in Prostate Cancer
Yu, E. Y., & Hahn, W. C. (2005) · Clinical Prostate Cancer · doi:10.3816/cgc.2005.n.003 · Cited by 1 · see citing works
The role of ER stress in the pathogenesis of Kennedy’s Disease
Montague-Cardoso, K. (2012) · UCL Discovery (University College London)
p53 and DNA damage checkpoint responses in the human prostate
af Hällström, T. (2007)
Overexpression of Androgen Receptor in Prostate Cancer
Urbanucci, A. (2012) · Tampere University Institutional Repository (Tampere University)
Effects of the androgen receptor overexpression in prostate cancer
Vartiainen, P. (2007) · Tampere University Institutional Repository (Tampere University)
Effect of Geldanamycin Binding on the Thr90 Phosphorylation Site of Hsp90
Shcherbakov, K. A., Shcherbinin, D. S., & Veselovsky, A. V. (2021) · Biomedical Chemistry Research and Methods · doi:10.18097/bmcrm00145
Somatic Alterations in Prostate Cancer Progression
Porkka, K. P., & Visakorpi, T. (2007) · Humana Press eBooks · doi:10.1007/978-1-59745-224-3_15
Characterization of Pten and Trp53 deficient prostatic tumors in mice
Bizri, R. E. (2018) · theses.fr (ABES) · doi:10.70675/887a45dbz93f0z4790z9840z71a317de4d2f
Guo, J., Wu, K., Zheng, M., Guo, S., Wang, F., & Lu, L. (2026) · Frontiers in Immunology · doi:10.3389/fimmu.2026.1852294
- Authors
- Culig, Z., Klocker, H., Bartsch, G., & Hobisch, A.
- Affiliations
- Innsbruck Medical University (AT)
- ORCID
- Klocker, Helmut
- Venue
- American Journal of PharmacoGenomics
- Published
- 2001
- Volume
- 1
- Issue
- 4
- Pages
- 241-249
- ISSN
- 1175-2203 (ISSN-L)
- OpenAlex
- W2216139737
- Semantic Scholar
- f001db8f71408be711edcfd2f3473e5c6dd95108
- Cited by
- 50
- References
- 96
- Citations by year
- 2026: 1 · 2021: 2 · 2018: 2 · 2016: 3 · 2015: 3 · 2013: 3 · 2012: 4
- FWCI
- 2.31
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- American Journal of PharmacoGenomics (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
- Keywords
- androgen receptor mutations, prostate cancer, androgen receptor antagonists, androgen withdrawal, endocrine therapy, bicalutamide, hydroxyflutamide, dihydrotestosterone, transcriptional coactivator, ribozymes, antisense oligonucleotides, metastatic prostate cancer
- MeSH terms
- Androgen Antagonists, Humans, Male, Mutation, Prostatic Neoplasms, Receptors, Androgen, Tumor Cells, Cultured, Point Mutation
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
