Continued exploration of the androgen receptor (AR) is crucial, as it plays pivotal roles in diverse diseases such as prostate cancer (PCa), serving as a significant therapeutic focus. Therefore, the Department of Urology Dresden hosted an international meeting for scientists and clinical oncologists to discuss the newest advances in AR research. The 2nd International Androgen Receptor Symposium was held in Dresden, Saxony, Germany, from 26-27.04.2024, organised by Dr. Holger H.H. Erb. Following the format of the first meeting, more than 35 scientists from 8 countries attended the event to discuss recent developments, research challenges, and identification of venues in AR research. An important new feature was the involvement of PhD students and young investigators, acknowledging the high scientific quality of their work. The symposium included three covers: new advances from clinical research, basic and translational research, and novel strategies to target AR. Moreover, based on its increasing clinical relevance, a PSMA theranostic mini-symposium was added at the end of the AR symposium to allow the audience to discuss the newest advances in PSMA theranostic. This report focuses on the highlights and discussions of the meeting.

Department of Biochemistry and Developmental Biology Faculty of Medicine University of Helsinki Helsinki Finland

Department of Clinical and Molecular Pathology Institute of Molecular and Translational Medicine Faculty of Medicine and Dentistry Palacký University and University Hospital Olomouc 779 00 Czech Republic

Department of Translational Imaging in Oncology National Center for Tumor Diseases Dresden Germany

Department of Urology Faculty of Medicine University Hospital Carl Gustav Carus Technische Universität Dresden Dresden Germany

Department of Urology Medical University of Innsbruck Innsbruck Austria

Department of Urology Saarland University Homburg Saar Germany

Division of Oncogenomics Oncode Institute The Netherlands Cancer Institute Amsterdam The Netherlands

German Cancer Consortium Heidelberg Germany

Institut für Radiopharmazie Helmholtz Zentrum Dresden Rossendorf Bautzner Landstraße 400 D 01328 Dresden Germany

Institute of Cancer Research Sutton Surrey UK

Institute of Human Genetics Jena University Hospital Friedrich Schiller University Jena Germany

MRC Oxford Institute for Radiation Oncology Department of Oncology University of Oxford Oxford UK

Universitätsklinikum Carl Gustav Carus an der Technischen Universität Dresden Fetscherstraße 74 01307 Dresden Germany

Zobrazit více v PubMed

Mehralivand S, Thomas C, Puhr M, Claessens F, van de Merbel AF, Dubrovska A et al. New advances of the androgen receptor in prostate cancer: report from the 1st International Androgen Receptor Symposium. J Transl Med. 2024;22(1):71. PubMed PMC

Sung H, Ferlay J, Siegel RL, Laversanne M, Soerjomataram I, Jemal A et al. Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. Cancer J Clin. 2021. PubMed

Ferlay J, Colombet M, Soerjomataram I, Parkin DM, Pineros M, Znaor A et al. Cancer statistics for the year 2020: an overview. Int J Cancer. 2021. PubMed

Isaacs JT. Resolving the Coffey Paradox: what does the androgen receptor do in normal vs. malignant prostate epithelial cells? Am J Clin Experimental Urol. 2018;6(2):55–61. PubMed PMC

Pisano C, Tucci M, Di Stefano RF, Turco F, Scagliotti GV, Di Maio M, et al. Interactions between androgen receptor signaling and other molecular pathways in prostate cancer progression: current and future clinical implications. Crit Rev Oncol Hematol. 2021;157:103185. doi: 10.1016/j.critrevonc.2020.103185. PubMed DOI

Beier AK, Puhr M, Stope MB, Thomas C, Erb HHH. Metabolic changes during prostate cancer development and progression. J Cancer Res Clin Oncol. 2023;149(5):2259–70. doi: 10.1007/s00432-022-04371-w. PubMed DOI PMC

Uo T, Sprenger CC, Plymate SR. Androgen receptor signaling and metabolic and Cellular Plasticity during Progression to Castration resistant prostate Cancer. Front Oncol. 2020;10:580617. doi: 10.3389/fonc.2020.580617. PubMed DOI PMC

Polkinghorn WR, Parker JS, Lee MX, Kass EM, Spratt DE, Iaquinta PJ, et al. Androgen receptor signaling regulates DNA repair in prostate cancers. Cancer Discov. 2013;3(11):1245–53. doi: 10.1158/2159-8290.CD-13-0172. PubMed DOI PMC

Shiota M, Yokomizo A, Naito S. Pro-survival and anti-apoptotic properties of androgen receptor signaling by oxidative stress promote treatment resistance in prostate cancer. Endocrine-related Cancer. 2012;19. PubMed

Schiewer MJ, Augello MA, Knudsen KE. The AR dependent cell cycle: mechanisms and cancer relevance. Mol Cell Endocrinol. 2012;352(1–2):34–45. doi: 10.1016/j.mce.2011.06.033. PubMed DOI PMC

Cornford P, van den Bergh RCN, Briers E, Van den Broeck T, Brunckhorst O, Darraugh J et al. EAU-EANM-ESTRO-ESUR-ISUP-SIOG guidelines on prostate Cancer-2024 update. Part I: screening, diagnosis, and local treatment with curative intent. Eur Urol. 2024. PubMed

Cornford P, van den Bergh RCN, Briers E, Van den Broeck T, Cumberbatch MG, De Santis M, et al. EAU-EANM-ESTRO-ESUR-SIOG guidelines on prostate Cancer. Part II-2020 update: treatment of relapsing and metastatic prostate Cancer. Eur Urol. 2021;79(2):263–82. doi: 10.1016/j.eururo.2020.09.046. PubMed DOI

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. PubMed

Santer FR, Erb HH, McNeill RV. Therapy escape mechanisms in the malignant prostate. Sem Cancer Biol. 2015;35:133–44. doi: 10.1016/j.semcancer.2015.08.005. PubMed DOI

Claessens F, Helsen C, Prekovic S, Van den Broeck T, Spans L, Van Poppel H, et al. Emerging mechanisms of enzalutamide resistance in prostate cancer. Nat Rev Urol. 2014;11(12):712–6. doi: 10.1038/nrurol.2014.243. PubMed DOI

Gravis G, Fizazi K, Joly F, Oudard S, Priou F, Esterni B, et al. Androgen-deprivation therapy alone or with docetaxel in non-castrate metastatic prostate cancer (GETUG-AFU 15): a randomised, open-label, phase 3 trial. Lancet Oncol. 2013;14(2):149–58. doi: 10.1016/S1470-2045(12)70560-0. PubMed DOI

Thomas C, Baunacke M, Erb HHH, Füssel S, Erdmann K, Putz J et al. Systemic triple therapy in metastatic hormone-sensitive prostate Cancer (mHSPC): ready for Prime Time or still to be. Explored? Cancers. 2021;14(1). PubMed PMC

Wang L, Paller CJ, Hong H, De Felice A, Alexander GC, Brawley O. Comparison of systemic treatments for metastatic castration-sensitive prostate Cancer: a systematic review and network Meta-analysis. JAMA Oncol. 2021;7(3):412–20. doi: 10.1001/jamaoncol.2020.6973. PubMed DOI PMC

Mandel P, Hoeh B, Wenzel M, Preisser F, Tian Z, Tilki D, et al. Triplet or Doublet Therapy in metastatic hormone-sensitive prostate Cancer patients: a systematic review and network Meta-analysis. Eur Urol Focus. 2023;9(1):96–105. doi: 10.1016/j.euf.2022.08.007. PubMed DOI

Hussain M, Kocherginsky M, Agarwal N, Adra N, Zhang J, Paller C, et al. BRCAAway: a randomized phase 2 trial of abiraterone, olaparib, or abiraterone + olaparib in patients with metastatic castration-resistant prostate cancer (mCRPC) bearing homologous recombination-repair mutations (HRRm) J Clin Oncol. 2024;42:19. doi: 10.1200/JCO.2024.42.4_suppl.19. PubMed DOI

Hofman MS, Emmett L, Sandhu S, Iravani A, Joshua AM, Goh JC, et al. [< sup > 177 Lu]Lu-PSMA-617 versus cabazitaxel in patients with metastatic castration-resistant prostate cancer (TheraP): a randomised, open-label, phase 2 trial. Lancet. 2021;397(10276):797–804. doi: 10.1016/S0140-6736(21)00237-3. PubMed DOI

Sartor O, de Bono J, Chi KN, Fizazi K, Herrmann K, Rahbar K, et al. Lutetium-177–PSMA-617 for metastatic castration-resistant prostate Cancer. N Engl J Med. 2021;385(12):1091–103. doi: 10.1056/NEJMoa2107322. PubMed DOI PMC

Hofman MS, Emmett L, Sandhu S, Iravani A, Buteau JP, Joshua AM, et al. Overall survival with [(177)Lu]Lu-PSMA-617 versus cabazitaxel in metastatic castration-resistant prostate cancer (TheraP): secondary outcomes of a randomised, open-label, phase 2 trial. Lancet Oncol. 2024;25(1):99–107. doi: 10.1016/S1470-2045(23)00529-6. PubMed DOI

Buteau J, Martin A, Emmett L, Iravani A, Sandhu S, Joshua A, et al. PSMA PET and FDG PET as predictors of response and prognosis in a randomized phase 2 trial of 177 Lu-PSMA-617 (LuPSMA) versus cabazitaxel in metastatic, castration-resistant prostate cancer (mCRPC) progressing after docetaxel (TheraP ANZUP 1603) J Clin Oncol. 2022;40:10. doi: 10.1200/JCO.2022.40.6_suppl.010. DOI

Chen Q-H, Munoz E, Ashong D. Insight into recent advances in degrading androgen receptor for castration-resistant prostate Cancer. Cancers [Internet]. 2024; 16(3). PubMed PMC

Gao X, Iii H, Vuky J, Dreicer R, Sartor A, Sternberg C, et al. Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC) J Clin Oncol. 2022;40:17. doi: 10.1200/JCO.2022.40.6_suppl.017. DOI

Petrylak D, Garmezy B, Shen J, Kalebasty A, Sartor O, Dreicer R, et al. 1803P phase I/II study of bavdegalutamide, a PROTAC androgen receptor (AR) degrader in metastatic castration-resistant prostate cancer (mCRPC): Radiographic progression-free survival (rPFS) in patients (pts) with AR ligand-binding domain (LBD) mutations. Ann Oncol. 2023;34:S973–4. doi: 10.1016/j.annonc.2023.09.2751. DOI

Petrylak D, Stewart T, Gao X, Berghorn E, Lu H, Chan E, et al. A phase 2 expansion study of ARV-766, a PROTACandrogen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC) J Clin Oncol. 2023;41:TPS290–TPS. doi: 10.1200/JCO.2023.41.6_suppl.TPS290. DOI

Bernard-Tessier A, Mulier G, Nay P, Baldini C, Albiges L, Colomba E, et al. Androgen receptor (AR) mutations in men with metastatic castration-resistant prostate cancer (mCRPC): incidence and natural history. J Clin Oncol. 2023;41:221. doi: 10.1200/JCO.2023.41.6_suppl.221. DOI

Antonarakis E, Zhang N, Saha J, Nevalaita L, Shell S, Garratt C et al. REAL-WORLD ASSESSMENT OF AR-LBD MUTATIONS IN METASTATIC CASTRATION-RESISTANT PROSTATE CANCER2023.

Crippa A, De Laere B, Discacciati A, Larsson B, Connor JT, Gabriel EE, et al. The ProBio trial: molecular biomarkers for advancing personalized treatment decision in patients with metastatic castration-resistant prostate cancer. Trials. 2020;21(1):579. doi: 10.1186/s13063-020-04515-8. PubMed DOI PMC

Kreuz M, Otto DJ, Fuessel S, Blumert C, Bertram C, Bartsch S, et al. ProstaTrend-A Multivariable Prognostic RNA expression score for aggressive prostate Cancer. Eur Urol. 2020;78(3):452–9. doi: 10.1016/j.eururo.2020.06.001. PubMed DOI

Ebersbach C, Beier A-MK, Hönscheid P, Sperling C, Jöhrens K, Baretton GB et al. Influence of systemic therapy on the expression and activity of selected STAT proteins in prostate Cancer tissue. Life. 2022;12(2). PubMed PMC

Ebersbach C, Beier A-MK, Thomas C, Erb HHH. Impact of STAT proteins in Tumor Progress and Therapy Resistance in Advanced and metastasized prostate Cancer. Cancers. 2021;13(19):4854. doi: 10.3390/cancers13194854. PubMed DOI PMC

Puhr M, Hoefer J, Eigentler A, Ploner C, Handle F, Schaefer G, et al. The glucocorticoid receptor is a key player for prostate Cancer cell survival and a target for Improved Antiandrogen Therapy. Clin cancer Research: Official J Am Association Cancer Res. 2018;24(4):927–38. doi: 10.1158/1078-0432.CCR-17-0989. PubMed DOI

Erb HH, Bodenbender J, Handle F, Diehl T, Donix L, Tsaur I, et al. Assessment of STAT5 as a potential therapy target in enzalutamide-resistant prostate cancer. PLoS ONE. 2020;15(8):e0237248. doi: 10.1371/journal.pone.0237248. PubMed DOI PMC

Arora VK, Schenkein E, Murali R, Subudhi SK, Wongvipat J, Balbas MD, et al. Glucocorticoid receptor confers resistance to antiandrogens by bypassing androgen receptor blockade. Cell. 2013;155(6):1309–22. doi: 10.1016/j.cell.2013.11.012. PubMed DOI PMC

Desai K, Serritella AV, Stadler WM, O’Donnell PH, Sweis RF, Szmulewitz RZ. Phase I trial of enzalutamide (Enz) plus the glucocorticoid receptor antagonist relacorilant (rela) for patients with metastatic castration resistant prostate cancer. J Clin Oncol. 2023;41(16suppl):5062. doi: 10.1200/JCO.2023.41.16_suppl.5062. DOI

Serritella AV, Shevrin D, Heath EI, Wade JL, Martinez E, Anderson A, et al. Phase I/II trial of Enzalutamide and Mifepristone, a glucocorticoid receptor antagonist, for metastatic castration-resistant prostate Cancer. Clin cancer Research: Official J Am Association Cancer Res. 2022;28(8):1549–59. doi: 10.1158/1078-0432.CCR-21-4049. PubMed DOI PMC

Abida W, Hahn AW, Shore N, Agarwal N, Sieber P, Smith MR, et al. Phase I study of ORIC-101, a glucocorticoid receptor antagonist, in combination with Enzalutamide in patients with metastatic castration-resistant prostate Cancer progressing on Enzalutamide. Clin cancer Research: Official J Am Association Cancer Res. 2024;30(6):1111–20. doi: 10.1158/1078-0432.CCR-23-3508. PubMed DOI PMC

Morris MJ, Linch MD, Crabb SJ, Beer TM, Heath EI, Gordon MS, et al. Phase 1 efficacy and pharmacodynamic results of exicorilant + enzalutamide in patients with metastatic castration-resistant prostate cancer. J Clin Oncol. 2023;41(6suppl):145. doi: 10.1200/JCO.2023.41.6_suppl.145. PubMed DOI

Eigentler A, Handle F, Schanung S, Degen A, Hackl H, Erb HHH, et al. Glucocorticoid treatment influences prostate cancer cell growth and the tumor microenvironment via altered glucocorticoid receptor signaling in prostate fibroblasts. Oncogene. 2024;43(4):235–47. doi: 10.1038/s41388-023-02901-5. PubMed DOI PMC

Linxweiler J, Hajili T, Körbel C, Berchem C, Zeuschner P, Müller A, et al. Cancer-associated fibroblasts stimulate primary tumor growth and metastatic spread in an orthotopic prostate cancer xenograft model. Sci Rep. 2020;10(1):12575. doi: 10.1038/s41598-020-69424-x. PubMed DOI PMC

Taurozzi AJ, Beekharry R, Wantoch M, Labarthe M-C, Walker HF, Seed RI, et al. Spontaneous development of Epstein-Barr virus associated human lymphomas in a prostate cancer xenograft program. PLoS ONE. 2017;12(11):e0188228. doi: 10.1371/journal.pone.0188228. PubMed DOI PMC

Saar M, Körbel C, Linxweiler J, Jung V, Hasenfus A, Stöckle M et al. Orthotopic tumorgrafts in nude mice: a new method to study human prostate cancer. Prostate. 2015;13. PubMed

Sailer V, von Amsberg G, Duensing S, Kirfel J, Lieb V, Metzger E, et al. Experimental in vitro, ex vivo and in vivo models in prostate cancer research. Nat Rev Urol. 2023;20(3):158–78. doi: 10.1038/s41585-022-00677-z. PubMed DOI

ERB HHH, OSTER MA, GELBRICH N, CAMMANN C, THOMAS C, MUSTEA A, et al. Enzalutamide-induced proteolytic degradation of the androgen receptor in prostate Cancer cells is mediated only to a limited extent by the Proteasome System. Anticancer Res. 2021;41(7):3271–9. doi: 10.21873/anticanres.15113. PubMed DOI

Siciliano T, Simons IH, Beier A-MK, Ebersbach C, Aksoy C, Seed RI, et al. A systematic comparison of Antiandrogens identifies androgen receptor protein Stability as an Indicator for Treatment Response. Life. 2021;11(9):874. doi: 10.3390/life11090874. PubMed DOI PMC

Siciliano T, Sommer U, Beier AK, Stope MB, Borkowetz A, Thomas C, et al. The androgen hormone-Induced increase in Androgen receptor protein expression is caused by the autoinduction of the androgen receptor translational activity. Curr Issues Mol Biol. 2022;44(2):597–608. doi: 10.3390/cimb44020041. PubMed DOI PMC

Zaalberg A, Pottendorfer E, Zwart W, Bergman AM. It takes two to Tango: the interplay between prostate Cancer and its Microenvironment from an epigenetic perspective. Cancers [Internet]. 2024; 16(2). PubMed PMC

Linder S, Hoogstraat M, Stelloo S, Eickhoff N, Schuurman K, de Barros H, et al. Drug-Induced Epigenomic Plasticity reprograms Circadian Rhythm Regulation to drive prostate Cancer toward androgen independence. Cancer Discov. 2022;12(9):2074–97. doi: 10.1158/2159-8290.CD-21-0576. PubMed DOI PMC

Niu Y, Altuwaijri S, Lai K-P, Wu C-T, Ricke WA, Messing EM et al. Androgen receptor is a tumor suppressor and proliferator in prostate cancer. Proceedings of the National Academy of Sciences. 2008;105(34):12182-7. PubMed PMC

Calabrese EJ. Androgens: biphasic dose responses. Crit Rev Toxicol. 2001;31(4–5):517–22. doi: 10.1080/20014091111794. PubMed DOI

Atri Roozbahani G, Kokal-Ribaudo M, Heidari Horestani M, Pungsrinont T, Baniahmad A. The protein composition of exosomes released by prostate cancer cells is distinctly regulated by androgen receptor-antagonists and -agonist to stimulate growth of target cells. Cell Communication Signal. 2024;22(1):219. doi: 10.1186/s12964-024-01584-z. PubMed DOI PMC

Mirzakhani K, Kallenbach J, Rasa SMM, Ribaudo F, Ungelenk M, Ehsani M, et al. The androgen receptor-lncRNASAT1-AKT-p15 axis mediates androgen-induced cellular senescence in prostate cancer cells. Oncogene. 2022;41(7):943–59. doi: 10.1038/s41388-021-02060-5. PubMed DOI PMC

Melnyk JE, Steri V, Nguyen HG, Hwang YC, Gordan JD, Hann B, et al. Targeting a splicing-mediated drug resistance mechanism in prostate cancer by inhibiting transcriptional regulation by PKCβ1. Oncogene. 2022;41(11):1536–49. doi: 10.1038/s41388-022-02179-z. PubMed DOI PMC

Van Goubergen J, Handle F, Cronauer MV, Santer FR. Abstract 2692: identification of functional single nucleotide polymorphisms in cryptic exon 3 of the androgen receptor gene. Cancer Res. 2022;82(12Supplement):2692. doi: 10.1158/1538-7445.AM2022-2692. PubMed DOI

Goubergen J, Handle F, Cronauer MV, Santer F. Identification of functional single nucleotide polymorphisms in cryptic exon 3 of the androgen receptor gene. Eur Urol Open Sci. 2022;44:S183. doi: 10.1016/S2666-1683(22)01947-4. DOI

Van Goubergen J, Perina M, Handle F, Morales E, Kremer A, Schmidt O et al. Die Spleißapparat-Komponente SRSF9 reguliert in einer rs5918762-abhängigen Weise die Expression von ARV7 [Abstractbook]. 2024 [cited 2024 02/06/2024]. https://www.egms.de/static/en/meetings/urobay2024/24urobay29.shtml

Chou J, Quigley DA, Robinson TM, Feng FY, Ashworth A. Transcription-Associated cyclin-dependent kinases as targets and biomarkers for Cancer Therapy. Cancer Discov. 2020;10(3):351–70. doi: 10.1158/2159-8290.CD-19-0528. PubMed DOI

Rescigno P, Gurel B, Pereira R, Crespo M, Rekowski J, Rediti M, et al. Characterizing CDK12-Mutated prostate cancers. Clin Cancer Res. 2021;27(2):566–74. doi: 10.1158/1078-0432.CCR-20-2371. PubMed DOI PMC

Gondane A, Itkonen HM. Revealing the history and mystery of RNA-Seq. Curr Issues Mol Biol. 2023;45(3):1860–74. doi: 10.3390/cimb45030120. PubMed DOI PMC

Sun R, Wei T, Ding D, Zhang J, Chen S, He HH, et al. CYCLIN K down-regulation induces androgen receptor gene intronic polyadenylation, variant expression and PARP inhibitor vulnerability in castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2022;119(39):e2205509119. doi: 10.1073/pnas.2205509119. PubMed DOI PMC

Liang J, Gondane A, Itkonen HM. CDK12-inactivation-induced MYC signaling causes dependency on the splicing kinase SRPK1. Mol Oncol. 2024. PubMed PMC

Pallasaho G, Duveau. Thomas, Loda, Itkonen. Compromised CDK12 activity causes dependency on the non-essential spliceosome components. bioRxiv2021.

Chen EX, Hotte S, Hirte H, Siu LL, Lyons J, Squires M, et al. A phase I study of cyclin-dependent kinase inhibitor, AT7519, in patients with advanced cancer: NCIC clinical trials Group IND 177. Br J Cancer. 2014;111(12):2262–7. doi: 10.1038/bjc.2014.565. PubMed DOI PMC

Mahadevan D, Plummer R, Squires MS, Rensvold D, Kurtin S, Pretzinger C, et al. A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Ann Oncol. 2011;22(9):2137–43. doi: 10.1093/annonc/mdq734. PubMed DOI

Hu Q, Poulose N, Girmay S, Heleva A, Doultsinos D, Gondane A, et al. Inhibition of CDK9 activity compromises global splicing in prostate cancer cells. RNA Biol. 2021;18(sup2):722–9. doi: 10.1080/15476286.2021.1983287. PubMed DOI PMC

Gondane A, Poulose N, Walker S, Mills IG, Itkonen HM. O-GlcNAc transferase maintains metabolic homeostasis in response to CDK9 inhibition. Glycobiology. 2022;32(9):751–9. PubMed PMC

Itkonen HM, Poulose N, Steele RE, Martin SES, Levine ZG, Duveau DY, et al. Inhibition of O-GlcNAc transferase renders prostate Cancer cells dependent on CDK9. Mol Cancer Res. 2020;18(10):1512–21. doi: 10.1158/1541-7786.MCR-20-0339. PubMed DOI PMC

Yalala S, Gondane A, Poulose N, Liang J, Mills IG, Itkonen HM. CDK9 inhibition activates innate immune response through viral mimicry. Faseb j. 2024;38(8):e23628. doi: 10.1096/fj.202302375R. PubMed DOI

Barfeld SJ, Urbanucci A, Itkonen HM, Fazli L, Hicks JL, Thiede B, et al. c-Myc antagonises the transcriptional activity of the androgen receptor in prostate Cancer Affecting Key Gene Networks. EBioMedicine. 2017;18:83–93. doi: 10.1016/j.ebiom.2017.04.006. PubMed DOI PMC

Pernigoni N, Zagato E, Calcinotto A, Troiani M, Mestre RP, Calì B, et al. Commensal bacteria promote endocrine resistance in prostate cancer through androgen biosynthesis. Science. 2021;374(6564):216–24. doi: 10.1126/science.abf8403. PubMed DOI

Sharp A, Coleman I, Yuan W, Sprenger C, Dolling D, Rodrigues DN, et al. Androgen receptor splice variant-7 expression emerges with castration resistance in prostate cancer. J Clin Invest. 2019;129(1):192–208. doi: 10.1172/JCI122819. PubMed DOI PMC

Calcinotto A, Spataro C, Zagato E, Di Mitri D, Gil V, Crespo M, et al. IL-23 secreted by myeloid cells drives castration-resistant prostate cancer. Nature. 2018;559(7714):363–9. doi: 10.1038/s41586-018-0266-0. PubMed DOI PMC

Guo C, Sharp A, Gurel B, Crespo M, Figueiredo I, Jain S, et al. Targeting myeloid chemotaxis to reverse prostate cancer therapy resistance. Nature. 2023;623(7989):1053–61. doi: 10.1038/s41586-023-06696-z. PubMed DOI PMC

Liu C, Lou W, Yang JC, Liu L, Armstrong CM, Lombard AP, et al. Proteostasis by STUB1/HSP70 complex controls sensitivity to androgen receptor targeted therapy in advanced prostate cancer. Nat Commun. 2018;9(1):4700. doi: 10.1038/s41467-018-07178-x. PubMed DOI PMC

Ferraldeschi R, Welti J, Powers MV, Yuan W, Smyth T, Seed G, et al. Second-generation HSP90 inhibitor Onalespib blocks mRNA splicing of androgen receptor variant 7 in prostate Cancer cells. Cancer Res. 2016;76(9):2731–42. doi: 10.1158/0008-5472.CAN-15-2186. PubMed DOI PMC

Nappi L, Aguda AH, Nakouzi NA, Lelj-Garolla B, Beraldi E, Lallous N, et al. Ivermectin inhibits HSP27 and potentiates efficacy of oncogene targeting in tumor models. J Clin Invest. 2020;130(2):699–714. doi: 10.1172/JCI130819. PubMed DOI PMC

Shrestha L, Bolaender A, Patel HJ, Taldone T. Heat shock protein (HSP) Drug Discovery and Development: Targeting Heat Shock proteins in Disease. Curr Top Med Chem. 2016;16(25):2753–64. doi: 10.2174/1568026616666160413141911. PubMed DOI PMC

Sommer U, Siciliano T, Ebersbach C, Beier A-MK, Stope MB, Jöhrens K, et al. Impact of androgen receptor activity on prostate-specific membrane Antigen expression in prostate Cancer cells. Int J Mol Sci. 2022;23(3):1046. doi: 10.3390/ijms23031046. PubMed DOI PMC

Peters SMB, Prive BM, de Bakker M, de Lange F, Jentzen W, Eek A, et al. Intra-therapeutic dosimetry of [(177)Lu]Lu-PSMA-617 in low-volume hormone-sensitive metastatic prostate cancer patients and correlation with treatment outcome. Eur J Nucl Med Mol Imaging. 2022;49(2):460–9. doi: 10.1007/s00259-021-05471-4. PubMed DOI PMC

Violet J, Jackson P, Ferdinandus J, Sandhu S, Akhurst T, Iravani A, et al. Dosimetry of < sup > 177 Lu-PSMA-617 in metastatic castration-resistant prostate Cancer: correlations between Pretherapeutic Imaging and whole-body tumor dosimetry with treatment outcomes. J Nucl Med. 2019;60(4):517–23. doi: 10.2967/jnumed.118.219352. PubMed DOI

Mah LJ, El-Osta A, Karagiannis TC. γH2AX: a sensitive molecular marker of DNA damage and repair. Leukemia. 2010;24(4):679–86. doi: 10.1038/leu.2010.6. PubMed DOI

Cornelissen B, Kersemans V, Darbar S, Thompson J, Shah K, Sleeth K, et al. Imaging DNA damage in vivo using gammaH2AX-targeted immunoconjugates. Cancer Res. 2011;71(13):4539–49. doi: 10.1158/0008-5472.CAN-10-4587. PubMed DOI PMC

Marinescu IM, Rogg M, Spohn S, von Büren M, Kamps M, Jilg CA, et al. Ex vivo γH2AX assay for tumor radiosensitivity in primary prostate cancer patients and correlation with clinical parameters. Radiat Oncol. 2022;17(1):163. doi: 10.1186/s13014-022-02131-1. PubMed DOI PMC

O’Neill E, Mosley M, Cornelissen B. Imaging DNA damage response by γH2AX in vivo predicts treatment response to Lutetium-177 radioligand therapy and suggests senescence as a therapeutically desirable outcome. Theranostics. 2023;13(4):1302–10. doi: 10.7150/thno.82101. PubMed DOI PMC

Reissig F, Bauer D, Zarschler K, Novy Z, Bendova K, Ludik M-C et al. Towards Targeted Alpha Therapy with Actinium-225: Chelators for Mild Condition Radiolabeling and Targeting PSMA—A Proof of Concept Study. Cancers [Internet]. 2021; 13(8). PubMed PMC

Kratochwil C, Bruchertseifer F, Giesel FL, Weis M, Verburg FA, Mottaghy F, et al. 225Ac-PSMA-617 for PSMA-Targeted α-Radiation Therapy of Metastatic Castration-resistant prostate Cancer. J Nucl Med. 2016;57(12):1941–4. doi: 10.2967/jnumed.116.178673. PubMed DOI

Usmani S, Rasheed R, Al Kandari F, Marafi F, Naqvi SAR. 225Ac prostate-specific membrane Antigen Posttherapy α imaging: comparing 2 and 3 photopeaks. Clin Nucl Med. 2019;44(5):401–3. doi: 10.1097/RLU.0000000000002525. PubMed DOI

Michler E, Kästner D, Brogsitter C, Pretze M, Hartmann H, Freudenberg R, et al. First-in-human SPECT/CT imaging of [212Pb]Pb-VMT-α-NET in a patient with metastatic neuroendocrine tumor. Eur J Nucl Med Mol Imaging. 2024;51(5):1490–2. doi: 10.1007/s00259-023-06529-1. PubMed DOI PMC

Emmett L, Buteau J, Papa N, Moon D, Thompson J, Roberts MJ, et al. The Additive Diagnostic Value of prostate-specific membrane Antigen Positron Emission Tomography Computed Tomography to Multiparametric Magnetic Resonance Imaging Triage in the diagnosis of prostate Cancer (PRIMARY): a prospective Multicentre Study. Eur Urol. 2021;80(6):682–9. doi: 10.1016/j.eururo.2021.08.002. PubMed DOI

Hofman MS, Lawrentschuk N, Francis RJ, Tang C, Vela I, Thomas P, et al. Prostate-specific membrane antigen PET-CT in patients with high-risk prostate cancer before curative-intent surgery or radiotherapy (proPSMA): a prospective, randomised, multicentre study. Lancet. 2020;395(10231):1208–16. doi: 10.1016/S0140-6736(20)30314-7. PubMed DOI

Horsley PJ, Koo CM, Eade T, Hsiao E, Emmett L, Brown C, et al. Mapping of local recurrences after Radical Prostatectomy using 68-Gallium-prostate-specific membrane Antigen Positron Emission Tomography/Computed tomography: implications for Postprostatectomy Radiation Therapy Clinical Target volumes. Int J Radiat Oncol Biol Phys. 2023;115(1):106–17. doi: 10.1016/j.ijrobp.2022.05.044. PubMed DOI

Emmett L, Subramaniam S, Crumbaker M, Nguyen A, Joshua AM, Weickhardt A, et al. [(177)Lu]Lu-PSMA-617 plus enzalutamide in patients with metastatic castration-resistant prostate cancer (ENZA-p): an open-label, multicentre, randomised, phase 2 trial. Lancet Oncol. 2024;25(5):563–71. doi: 10.1016/S1470-2045(24)00135-9. PubMed DOI

Suman S, Parghane RV, Joshi A, Prabhash K, Talole S, Basu S, Combined. (177) Lu-PSMA-617 PRLT and abiraterone acetate versus (177) Lu-PSMA-617 PRLT monotherapy in metastatic castration-resistant prostate cancer: An observational study comparing the response and durability. The Prostate. 2021;81(15):1225-34. PubMed

Schuurman T, Witteveen P, Wall E, Passier J, Huitema A, Amant F et al. Tamoxifen and pregnancy: an absolute contraindication? Breast Cancer Res Treat. 2019;175. PubMed

Puhr M, Eigentler A, Handle F, Hackl H, Ploner C, Heidegger I, et al. Targeting the glucocorticoid receptor signature gene Mono Amine Oxidase-A enhances the efficacy of chemo- and anti-androgen therapy in advanced prostate cancer. Oncogene. 2021;40(17):3087–100. doi: 10.1038/s41388-021-01754-0. PubMed DOI PMC