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Bipolar androgen therapy in men with metastatic castration-resistant prostate cancer after progression on enzalutamide: an open-label, phase 2, multicohort study.

Teply BA, Wang H, Luber B, Sullivan R, Rifkind I, Bruns A, Spitz A, DeCarli M, Sinibaldi V, Pratz CF, Lu C, Silberstein JL, Luo J, Schweizer MT, Drake CG, Carducci MA, Paller CJ, Antonarakis ES, Eisenberger MA, Denmeade SR.

Lancet Oncol. 2018 Jan;19(1):76-86. doi: 10.1016/S1470-2045(17)30906-3. Epub 2017 Dec 14.


Anticancer activities of emetine prodrugs that are proteolytically activated by the prostate specific antigen (PSA) and evaluation of in vivo toxicity of emetine derivatives.

Akinboye ES, Rosen MD, Bakare O, Denmeade SR.

Bioorg Med Chem. 2017 Dec 15;25(24):6707-6717. doi: 10.1016/j.bmc.2017.11.015. Epub 2017 Nov 10.


Muscadine Grape Skin Extract (MPX) in Men with Biochemically Recurrent Prostate Cancer: A Randomized, Multicenter, Placebo-Controlled Clinical Trial.

Paller CJ, Zhou XC, Heath EI, Taplin ME, Mayer T, Stein MN, Bubley GJ, Pili R, Hudson T, Kakarla R, Abbas MM, Anders NM, Dowling D, King S, Bruns AB, Wagner WD, Drake CG, Antonarakis ES, Eisenberger MA, Denmeade SR, Rudek MA, Rosner GL, Carducci MA.

Clin Cancer Res. 2018 Jan 15;24(2):306-315. doi: 10.1158/1078-0432.CCR-17-1100. Epub 2017 Nov 7.


Rationale for bipolar androgen therapy (BAT) for metastatic prostate cancer.

Isaacs JT, Brennen WN, Denmeade SR.

Cell Cycle. 2017 Sep 17;16(18):1639-1640. doi: 10.1080/15384101.2017.1360645. Epub 2017 Aug 18. No abstract available.


Mesenchymal stem cell infiltration during neoplastic transformation of the human prostate.

Brennen WN, Zhang B, Kulac I, Kisteman LN, Antony L, Wang H, Meeker AK, De Marzo AM, Garraway IP, Denmeade SR, Isaacs JT.

Oncotarget. 2017 Jul 18;8(29):46710-46727. doi: 10.18632/oncotarget.17362.


Clinical Significance of Androgen Receptor Splice Variant-7 mRNA Detection in Circulating Tumor Cells of Men With Metastatic Castration-Resistant Prostate Cancer Treated With First- and Second-Line Abiraterone and Enzalutamide.

Antonarakis ES, Lu C, Luber B, Wang H, Chen Y, Zhu Y, Silberstein JL, Taylor MN, Maughan BL, Denmeade SR, Pienta KJ, Paller CJ, Carducci MA, Eisenberger MA, Luo J.

J Clin Oncol. 2017 Jul 1;35(19):2149-2156. doi: 10.1200/JCO.2016.70.1961. Epub 2017 Apr 6.


Bipolar Androgen Therapy: A Paradoxical Approach for the Treatment of Castration-resistant Prostate Cancer.

Schweizer MT, Antonarakis ES, Denmeade SR.

Eur Urol. 2017 Sep;72(3):323-325. doi: 10.1016/j.eururo.2017.03.022. Epub 2017 Mar 29.


Clinical Applications of Molecular Imaging in the Management of Prostate Cancer.

Gorin MA, Rowe SP, Denmeade SR.

PET Clin. 2017 Apr;12(2):185-192. doi: 10.1016/j.cpet.2016.11.001. Epub 2017 Jan 16. Review.


Androgen Receptor Splice Variants Are Not Substrates of Nonsense-Mediated Decay.

Ajiboye AS, Esopi D, Yegnasubramanian S, Denmeade SR.

Prostate. 2017 Jun;77(8):829-837. doi: 10.1002/pros.23323. Epub 2017 Feb 22.


Detection fidelity of AR mutations in plasma derived cell-free DNA.

Goldstein A, Toro PV, Lee J, Silberstein JL, Nakazawa M, Waters I, Cravero K, Chu D, Cochran RL, Kim M, Shinn D, Torquato S, Hughes RM, Pallavajjala A, Carducci MA, Paller CJ, Denmeade SR, Kressel B, Trock BJ, Eisenberger MA, Antonarakis ES, Park BH, Hurley PJ.

Oncotarget. 2017 Feb 28;8(9):15651-15662. doi: 10.18632/oncotarget.14926.


Germline Mutations in ATM and BRCA1/2 Distinguish Risk for Lethal and Indolent Prostate Cancer and are Associated with Early Age at Death.

Na R, Zheng SL, Han M, Yu H, Jiang D, Shah S, Ewing CM, Zhang L, Novakovic K, Petkewicz J, Gulukota K, Helseth DL Jr, Quinn M, Humphries E, Wiley KE, Isaacs SD, Wu Y, Liu X, Zhang N, Wang CH, Khandekar J, Hulick PJ, Shevrin DH, Cooney KA, Shen Z, Partin AW, Carter HB, Carducci MA, Eisenberger MA, Denmeade SR, McGuire M, Walsh PC, Helfand BT, Brendler CB, Ding Q, Xu J, Isaacs WB.

Eur Urol. 2017 May;71(5):740-747. doi: 10.1016/j.eururo.2016.11.033. Epub 2016 Dec 15.


Extreme Response to High-dose Testosterone in BRCA2- and ATM-mutated Prostate Cancer.

Teply BA, Kachhap S, Eisenberger MA, Denmeade SR.

Eur Urol. 2017 Mar;71(3):499. doi: 10.1016/j.eururo.2016.09.020. Epub 2016 Sep 29. No abstract available.


Challenges of conducting clinical trials of natural products to combat cancer.

Paller CJ, Denmeade SR, Carducci MA.

Clin Adv Hematol Oncol. 2016 Jun;14(6):447-55. Review.


Bipolar Androgen Therapy for Men With Androgen Ablation Naïve Prostate Cancer: Results From the Phase II BATMAN Study.

Schweizer MT, Wang H, Luber B, Nadal R, Spitz A, Rosen DM, Cao H, Antonarakis ES, Eisenberger MA, Carducci MA, Paller C, Denmeade SR.

Prostate. 2016 Sep;76(13):1218-26. doi: 10.1002/pros.23209. Epub 2016 Jun 24.


Mutational Analysis of Prostate-Specific Antigen Defines the Intrinsic Proteolytic Activity of the proPSA Zymogen.

Sangster-Guity N, Tu-Sekine B, Raben DM, Denmeade SR, Williams SA.

Prostate. 2016 Sep;76(13):1203-17. doi: 10.1002/pros.23216. Epub 2016 Jun 8.


A prodrug-doped cellular Trojan Horse for the potential treatment of prostate cancer.

Levy O, Brennen WN, Han E, Rosen DM, Musabeyezu J, Safaee H, Ranganath S, Ngai J, Heinelt M, Milton Y, Wang H, Bhagchandani SH, Joshi N, Bhowmick N, Denmeade SR, Isaacs JT, Karp JM.

Biomaterials. 2016 Jun;91:140-150. doi: 10.1016/j.biomaterials.2016.03.023. Epub 2016 Mar 17.


The influence of prednisone on the efficacy of docetaxel in men with metastatic castration-resistant prostate cancer.

Teply BA, Luber B, Denmeade SR, Antonarakis ES.

Prostate Cancer Prostatic Dis. 2016 Mar;19(1):72-8. doi: 10.1038/pcan.2015.53. Epub 2015 Nov 17.


Iterative design of emetine-based prodrug targeting fibroblast activation protein (FAP) and dipeptidyl peptidase IV DPPIV using a tandem enzymatic activation strategy.

Akinboye ES, Brennen WN, Rosen DM, Bakare O, Denmeade SR.

Prostate. 2016 Jun;76(8):703-14. doi: 10.1002/pros.23162. Epub 2016 Feb 2.


Prognostic factors for clinical outcomes in patients with metastatic castration resistant prostate cancer treated with sequential novel androgen receptor-directed therapies.

Nadal R, Tsai HL, Sinibaldi VJ, Paller CJ, Antonarakis ES, Denmeade SR, Carducci MA, Eisenberger MA.

Prostate. 2016 Apr;76(5):512-20. doi: 10.1002/pros.23141. Epub 2015 Dec 22.


Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines.

Akinboye ES, Bamji ZD, Kwabi-Addo B, Ejeh D, Copeland RL, Denmeade SR, Bakare O.

Bioorg Med Chem. 2015 Sep 1;23(17):5839-45. doi: 10.1016/j.bmc.2015.06.072. Epub 2015 Jul 4.


Androgen Receptor Splice Variant 7 and Efficacy of Taxane Chemotherapy in Patients With Metastatic Castration-Resistant Prostate Cancer.

Antonarakis ES, Lu C, Luber B, Wang H, Chen Y, Nakazawa M, Nadal R, Paller CJ, Denmeade SR, Carducci MA, Eisenberger MA, Luo J.

JAMA Oncol. 2015 Aug;1(5):582-91. doi: 10.1001/jamaoncol.2015.1341.


A phase I study of muscadine grape skin extract in men with biochemically recurrent prostate cancer: Safety, tolerability, and dose determination.

Paller CJ, Rudek MA, Zhou XC, Wagner WD, Hudson TS, Anders N, Hammers HJ, Dowling D, King S, Antonarakis ES, Drake CG, Eisenberger MA, Denmeade SR, Rosner GL, Carducci MA.

Prostate. 2015 Oct;75(14):1518-25. doi: 10.1002/pros.23024. Epub 2015 May 27.


CCAAT/Enhancer binding protein β controls androgen-deprivation-induced senescence in prostate cancer cells.

Barakat DJ, Zhang J, Barberi T, Denmeade SR, Friedman AD, Paz-Priel I.

Oncogene. 2015 Nov 26;34(48):5912-22. doi: 10.1038/onc.2015.41. Epub 2015 Mar 16.


Effect of bipolar androgen therapy for asymptomatic men with castration-resistant prostate cancer: results from a pilot clinical study.

Schweizer MT, Antonarakis ES, Wang H, Ajiboye AS, Spitz A, Cao H, Luo J, Haffner MC, Yegnasubramanian S, Carducci MA, Eisenberger MA, Isaacs JT, Denmeade SR.

Sci Transl Med. 2015 Jan 7;7(269):269ra2. doi: 10.1126/scitranslmed.3010563.


Protease-activated pore-forming peptides for the treatment and imaging of prostate cancer.

LeBeau AM, Denmeade SR.

Mol Cancer Ther. 2015 Mar;14(3):659-68. doi: 10.1158/1535-7163.MCT-14-0744. Epub 2014 Dec 23.


AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer.

Antonarakis ES, Lu C, Wang H, Luber B, Nakazawa M, Roeser JC, Chen Y, Mohammad TA, Chen Y, Fedor HL, Lotan TL, Zheng Q, De Marzo AM, Isaacs JT, Isaacs WB, Nadal R, Paller CJ, Denmeade SR, Carducci MA, Eisenberger MA, Luo J.

N Engl J Med. 2014 Sep 11;371(11):1028-38. doi: 10.1056/NEJMoa1315815. Epub 2014 Sep 3.


Clinical activity of enzalutamide in Docetaxel-naïve and Docetaxel-pretreated patients with metastatic castration-resistant prostate cancer.

Nadal R, Zhang Z, Rahman H, Schweizer MT, Denmeade SR, Paller CJ, Carducci MA, Eisenberger MA, Antonarakis ES.

Prostate. 2014 Nov;74(15):1560-8. doi: 10.1002/pros.22874. Epub 2014 Aug 31.


Targeting thapsigargin towards tumors.

Doan NT, Paulsen ES, Sehgal P, Møller JV, Nissen P, Denmeade SR, Isaacs JT, Dionne CA, Christensen SB.

Steroids. 2015 May;97:2-7. doi: 10.1016/j.steroids.2014.07.009. Epub 2014 Jul 24. Review.


Pharmacokinetics and toxicology of a fibroblast activation protein (FAP)-activated prodrug in murine xenograft models of human cancer.

Brennen WN, Rosen DM, Chaux A, Netto GJ, Isaacs JT, Denmeade SR.

Prostate. 2014 Sep;74(13):1308-19. doi: 10.1002/pros.22847. Epub 2014 Jul 22.


The effect of the frequency and duration of PSA measurement on PSA doubling time calculations in men with biochemically recurrent prostate cancer.

Paller CJ, Olatoye D, Xie S, Zhou X, Denmeade SR, Eisenberger MA, Antonarakis ES, Carducci MA, Rosner GL.

Prostate Cancer Prostatic Dis. 2014 Mar;17(1):28-33. doi: 10.1038/pcan.2013.40. Epub 2013 Oct 8.


Mesenchymal stem cells as a vector for the inflammatory prostate microenvironment.

Brennen WN, Denmeade SR, Isaacs JT.

Endocr Relat Cancer. 2013 Aug 23;20(5):R269-90. doi: 10.1530/ERC-13-0151. Print 2013 Oct. Review.


Structural optimization, biological evaluation, and application of peptidomimetic prostate specific antigen inhibitors.

Kostova MB, Rosen DM, Chen Y, Mease RC, Denmeade SR.

J Med Chem. 2013 Jun 13;56(11):4224-35. doi: 10.1021/jm301718c. Epub 2013 Jun 4.


Single copies of mutant KRAS and mutant PIK3CA cooperate in immortalized human epithelial cells to induce tumor formation.

Wang GM, Wong HY, Konishi H, Blair BG, Abukhdeir AM, Gustin JP, Rosen DM, Denmeade SR, Rasheed Z, Matsui W, Garay JP, Mohseni M, Higgins MJ, Cidado J, Jelovac D, Croessmann S, Cochran RL, Karnan S, Konishi Y, Ota A, Hosokawa Y, Argani P, Lauring J, Park BH.

Cancer Res. 2013 Jun 1;73(11):3248-61. doi: 10.1158/0008-5472.CAN-12-1578. Epub 2013 Apr 11.


Proteolysis of complement factors iC3b and C5 by the serine protease prostate-specific antigen in prostatic fluid and seminal plasma.

Manning ML, Williams SA, Jelinek CA, Kostova MB, Denmeade SR.

J Immunol. 2013 Mar 15;190(6):2567-74. doi: 10.4049/jimmunol.1200856. Epub 2013 Feb 11.


Quantification of Mesenchymal Stem Cells (MSCs) at sites of human prostate cancer.

Brennen WN, Chen S, Denmeade SR, Isaacs JT.

Oncotarget. 2013 Jan;4(1):106-17.


Prospective, randomized, double-blind, vehicle controlled, multicenter phase IIb clinical trial of the pore forming protein PRX302 for targeted treatment of symptomatic benign prostatic hyperplasia.

Elhilali MM, Pommerville P, Yocum RC, Merchant R, Roehrborn CG, Denmeade SR.

J Urol. 2013 Apr;189(4):1421-6. doi: 10.1016/j.juro.2012.11.003. Epub 2012 Nov 7.


The unfolding treatment landscape for men with castration-resistant prostate cancer.

Kim JJ, Keizman D, Denmeade SR, Antonarakis ES.

Clin Investig (Lond). 2011 Nov;1(11):1533-1544.


Targeting carcinoma-associated fibroblasts within the tumor stroma with a fibroblast activation protein-activated prodrug.

Brennen WN, Rosen DM, Wang H, Isaacs JT, Denmeade SR.

J Natl Cancer Inst. 2012 Sep 5;104(17):1320-34. doi: 10.1093/jnci/djs336. Epub 2012 Aug 21.


Design, synthesis, and evaluation of pH-dependent hydrolyzable emetine analogues as treatment for prostate cancer.

Akinboye ES, Rosen MD, Denmeade SR, Kwabi-Addo B, Bakare O.

J Med Chem. 2012 Sep 13;55(17):7450-9. doi: 10.1021/jm300426q. Epub 2012 Aug 16.


Engineering enzymatically activated "molecular grenades" for cancer.

Denmeade SR, Isaacs JT.

Oncotarget. 2012 Jul;3(7):666-7.


Engineering a prostate-specific membrane antigen-activated tumor endothelial cell prodrug for cancer therapy.

Denmeade SR, Mhaka AM, Rosen DM, Brennen WN, Dalrymple S, Dach I, Olesen C, Gurel B, Demarzo AM, Wilding G, Carducci MA, Dionne CA, Møller JV, Nissen P, Christensen SB, Isaacs JT.

Sci Transl Med. 2012 Jun 27;4(140):140ra86. doi: 10.1126/scitranslmed.3003886. Erratum in: Sci Transl Med. 2012 Jul 18;4(143):143er4.


A phase I/IIA study of AGS-PSCA for castration-resistant prostate cancer.

Morris MJ, Eisenberger MA, Pili R, Denmeade SR, Rathkopf D, Slovin SF, Farrelly J, Chudow JJ, Vincent M, Scher HI, Carducci MA.

Ann Oncol. 2012 Oct;23(10):2714-9. Epub 2012 May 2.


Adaptive auto-regulation of androgen receptor provides a paradigm shifting rationale for bipolar androgen therapy (BAT) for castrate resistant human prostate cancer.

Isaacs JT, D'Antonio JM, Chen S, Antony L, Dalrymple SP, Ndikuyeze GH, Luo J, Denmeade SR.

Prostate. 2012 Oct 1;72(14):1491-505. doi: 10.1002/pros.22504. Epub 2012 Mar 6.


Rationale behind targeting fibroblast activation protein-expressing carcinoma-associated fibroblasts as a novel chemotherapeutic strategy.

Brennen WN, Isaacs JT, Denmeade SR.

Mol Cancer Ther. 2012 Feb;11(2):257-66. doi: 10.1158/1535-7163.MCT-11-0340. Review.


Trypsin-like proteolytic contamination of commercially available psa purified from human seminal fluid.

Manning ML, Kostova M, Williams SA, Denmeade SR.

Prostate. 2012 Aug 1;72(11):1233-8. doi: 10.1002/pros.22474. Epub 2011 Dec 28.


Phase I rapid dose-escalation study of AGS-1C4D4, a human anti-PSCA (prostate stem cell antigen) monoclonal antibody, in patients with castration-resistant prostate cancer: a PCCTC trial.

Antonarakis ES, Carducci MA, Eisenberger MA, Denmeade SR, Slovin SF, Jelaca-Maxwell K, Vincent ME, Scher HI, Morris MJ.

Cancer Chemother Pharmacol. 2012 Mar;69(3):763-71. doi: 10.1007/s00280-011-1759-9. Epub 2011 Oct 22.


Enzymatically active prostate-specific antigen promotes growth of human prostate cancers.

Williams SA, Jelinek CA, Litvinov I, Cotter RJ, Isaacs JT, Denmeade SR.

Prostate. 2011 Nov;71(15):1595-607. doi: 10.1002/pros.21375. Epub 2011 Mar 10.


Synthesis and cytotoxic activities of some 2-arylnaphtho[2,3-d]oxazole-4,9-dione derivatives on androgen-dependent (LNCaP) and androgen-independent (PC3) human prostate cancer cell lines.

Brandy Y, Ononiwu I, Adedeji D, Williams V, Mouamba C, Kanaan Y, Copeland RL Jr, Wright DA, Butcher RJ, Denmeade SR, Bakare O.

Invest New Drugs. 2012 Aug;30(4):1709-14. doi: 10.1007/s10637-011-9635-3. Epub 2011 Jan 18.


Phase 1 and 2 studies demonstrate the safety and efficacy of intraprostatic injection of PRX302 for the targeted treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia.

Denmeade SR, Egerdie B, Steinhoff G, Merchant R, Abi-Habib R, Pommerville P.

Eur Urol. 2011 May;59(5):747-54. doi: 10.1016/j.eururo.2010.11.024. Epub 2010 Nov 24.

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