1z95 Citations

Structural basis for antagonism and resistance of bicalutamide in prostate cancer.

Proc Natl Acad Sci U S A 102 6201-6 (2005)
Cited: 211 times
EuropePMC logo PMID: 15833816

Abstract

Carcinoma of the prostate is the most commonly diagnosed cancer in men. The current pharmacological treatment of choice for progressive androgen-dependent prostate cancer is the nonsteroidal antiandrogen, bicalutamide, either as monotherapy or with adjuvant castration or luteinizing hormone-releasing hormone superagonists to block the synthesis of endogenous testosterone. To date, no nonsteroidal or antagonist-bound androgen receptor (AR) structure is available. We solved the x-ray crystal structure of the mutant W741L AR ligand-binding domain bound to R-bicalutamide at 1.8-A resolution. This mutation confers agonist activity to bicalutamide and is likely involved in bicalutamide withdrawal syndrome. The three-dimensional structure demonstrates that the B ring of R-bicalutamide in the W741L mutant is accommodated at the location of the indole ring of Trp-741 in the WT AR bound to dihydrotestosterone. Knowledge of the binding mechanism for R-bicalutamide will provide molecular rationale for the development of new antiandrogens and selective AR modulators.

Reviews - 1z95 mentioned but not cited (7)

  1. Androgen receptor: structure, role in prostate cancer and drug discovery. Tan MH, Li J, Xu HE, Melcher K, Yong EL. Acta Pharmacol Sin 36 3-23 (2015)
  2. Chemistry and structural biology of androgen receptor. Gao W, Bohl CE, Dalton JT. Chem Rev 105 3352-3370 (2005)
  3. Bioinformatics and variability in drug response: a protein structural perspective. Lahti JL, Tang GW, Capriotti E, Liu T, Altman RB. J R Soc Interface 9 1409-1437 (2012)
  4. Targeting alternative sites on the androgen receptor to treat castration-resistant prostate cancer. Lallous N, Dalal K, Cherkasov A, Rennie PS. Int J Mol Sci 14 12496-12519 (2013)
  5. Progress in antiandrogen design targeting hormone binding pocket to circumvent mutation based resistance. Tian X, He Y, Zhou J. Front Pharmacol 6 57 (2015)
  6. A unifying biology of sex steroid-induced apoptosis in prostate and breast cancers. Maximov PY, Abderrahman B, Curpan RF, Hawsawi YM, Fan P, Jordan VC. Endocr Relat Cancer 25 R83-R113 (2018)
  7. Chemical modulation of transcription factors. Wiedemann B, Weisner J, Rauh D. Medchemcomm 9 1249-1272 (2018)

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  1. Overcoming mutation-based resistance to antiandrogens with rational drug design. Balbas MD, Evans MJ, Hosfield DJ, Wongvipat J, Arora VK, Watson PA, Chen Y, Greene GL, Shen Y, Sawyers CL. Elife 2 e00499 (2013)
  2. Structural basis for antagonism and resistance of bicalutamide in prostate cancer. Bohl CE, Gao W, Miller DD, Bell CE, Dalton JT. Proc Natl Acad Sci U S A 102 6201-6206 (2005)
  3. Variability in docking success rates due to dataset preparation. Corbeil CR, Williams CI, Labute P. J Comput Aided Mol Des 26 775-786 (2012)
  4. Modulation of androgen receptor activation function 2 by testosterone and dihydrotestosterone. Askew EB, Gampe RT, Stanley TB, Faggart JL, Wilson EM. J Biol Chem 282 25801-25816 (2007)
  5. Structural basis for accommodation of nonsteroidal ligands in the androgen receptor. Bohl CE, Miller DD, Chen J, Bell CE, Dalton JT. J Biol Chem 280 37747-37754 (2005)
  6. Evaluation of DOCK 6 as a pose generation and database enrichment tool. Brozell SR, Mukherjee S, Balius TE, Roe DR, Case DA, Rizzo RC. J Comput Aided Mol Des 26 749-773 (2012)
  7. Structure of the homodimeric androgen receptor ligand-binding domain. Nadal M, Prekovic S, Gallastegui N, Helsen C, Abella M, Zielinska K, Gay M, Vilaseca M, Taulès M, Houtsmuller AB, van Royen ME, Claessens F, Fuentes-Prior P, Estébanez-Perpiñá E. Nat Commun 8 14388 (2017)
  8. Pharmacophore-based virtual screening versus docking-based virtual screening: a benchmark comparison against eight targets. Chen Z, Li HL, Zhang QJ, Bao XG, Yu KQ, Luo XM, Zhu WL, Jiang HL. Acta Pharmacol Sin 30 1694-1708 (2009)
  9. BSP-SLIM: a blind low-resolution ligand-protein docking approach using predicted protein structures. Lee HS, Zhang Y. Proteins 80 93-110 (2012)
  10. Improving accuracy and efficiency of blind protein-ligand docking by focusing on predicted binding sites. Ghersi D, Sanchez R. Proteins 74 417-424 (2009)
  11. Binding of a cyano- and fluoro-containing drug bicalutamide to cytochrome P450 46A1: unusual features and spectral response. Mast N, Zheng W, Stout CD, Pikuleva IA. J Biol Chem 288 4613-4624 (2013)
  12. Galbanic acid decreases androgen receptor abundance and signaling and induces G1 arrest in prostate cancer cells. Zhang Y, Kim KH, Zhang W, Guo Y, Kim SH, Lü J. Int J Cancer 130 200-212 (2012)
  13. Fragment-based Shape Signatures: a new tool for virtual screening and drug discovery. Zauhar RJ, Gianti E, Welsh WJ. J Comput Aided Mol Des 27 1009-1036 (2013)
  14. Survey of phosphorylation near drug binding sites in the Protein Data Bank (PDB) and their effects. Smith KP, Gifford KM, Waitzman JS, Rice SE. Proteins 83 25-36 (2015)
  15. Using a Consensus Docking Approach to Predict Adverse Drug Reactions in Combination Drug Therapies for Gulf War Illness. Jaundoo R, Bohmann J, Gutierrez GE, Klimas N, Broderick G, Craddock TJA. Int J Mol Sci 19 E3355 (2018)
  16. Structural Dynamics of Agonist and Antagonist Binding to the Androgen Receptor. Azhagiya Singam ER, Tachachartvanich P, La Merrill MA, Smith MT, Durkin KA. J Phys Chem B 123 7657-7666 (2019)
  17. A 3-(4-nitronaphthen-1-yl) amino-benzoate analog as a bifunctional AKR1C3 inhibitor and AR antagonist: Head to head comparison with other advanced AKR1C3 targeted therapeutics. Wangtrakuldee P, Adeniji AO, Zang T, Duan L, Khatri B, Twenter BM, Estrada MA, Higgins TF, Winkler JD, Penning TM. J Steroid Biochem Mol Biol 192 105283 (2019)
  18. Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog-Thalidomide PROTACs. Kim GY, Song CW, Yang YS, Lee NR, Yoo HS, Son SH, Lee SJ, Park JS, Lee JK, Inn KS, Kim NJ. Molecules 26 2525 (2021)
  19. Identification & Characterization of lactobacillus salavarius bacteriocins and its relevance in cancer therapeutics. Shaikh F, Abhinand P, Ragunath P. Bioinformation 8 589-594 (2012)
  20. Rational design of novel antiandrogens for neutralizing androgen receptor function in hormone refractory prostate cancer. Singh P, Hallur G, Anchoori RK, Bakare O, Kageyama Y, Khan SR, Isaacs JT. Prostate 68 1570-1581 (2008)
  21. Conformational dynamics of androgen receptors bound to agonists and antagonists. Gim HJ, Park J, Jung ME, Houk KN. Sci Rep 11 15887 (2021)
  22. Structural Changes Due to Antagonist Binding in Ligand Binding Pocket of Androgen Receptor Elucidated Through Molecular Dynamics Simulations. Sakkiah S, Kusko R, Pan B, Guo W, Ge W, Tong W, Hong H. Front Pharmacol 9 492 (2018)
  23. Discovery of a novel AR/HDAC6 dual inhibitor for prostate cancer treatment. Zhou M, Zheng H, Li Y, Huang H, Min X, Dai S, Zhou W, Chen Z, Xu G, Chen Y. Aging (Albany NY) 13 6982-6998 (2021)
  24. High-throughput quantum-mechanics/molecular-mechanics (ONIOM) macromolecular crystallographic refinement with PHENIX/DivCon: the impact of mixed Hamiltonian methods on ligand and protein structure. Borbulevych O, Martin RI, Westerhoff LM. Acta Crystallogr D Struct Biol 74 1063-1077 (2018)
  25. Charge density view on bicalutamide molecular interactions in the monoclinic polymorph and androgen receptor binding pocket. Korlyukov AA, Malinska M, Vologzhanina AV, Goizman MS, Trzybinski D, Wozniak K. IUCrJ 7 71-82 (2020)
  26. Diversity-guided Lamarckian random drift particle swarm optimization for flexible ligand docking. Li C, Sun J, Palade V. BMC Bioinformatics 21 286 (2020)
  27. Divide-and-conquer strategy for large-scale Eulerian solvent excluded surface. Zhao R, Wang M, Tong Y, Wei GW. Commun Inf Syst 18 299-329 (2018)
  28. Structure-Based Study to Overcome Cross-Reactivity of Novel Androgen Receptor Inhibitors. Radaeva M, Li H, LeBlanc E, Dalal K, Ban F, Ciesielski F, Chow B, Morin H, Awrey S, Singh K, Rennie PS, Lallous N, Cherkasov A. Cells 11 2785 (2022)
  29. In silico prediction of nuclear receptor binding to polychlorinated dibenzofurans and its implication on endocrine disruption in humans and wildlife. Akinola LK, Uzairu A, Shallangwa GA, Abechi SE. Curr Res Toxicol 2 357-365 (2021)
  30. A Rationalized Approach to Design and Discover Novel Non-steroidal Derivatives through Computational Aid for the Treatment of Prostate Cancer. Kumar S, Arora P, Wadhwa P, Kaur P. Curr Comput Aided Drug Des (2023)
  31. A multilayer dynamic perturbation analysis method for predicting ligand-protein interactions. Gu L, Li B, Ming D. BMC Bioinformatics 23 456 (2022)
  32. An Assay on the Possible Effect of Essential Oil Constituents on Receptors Involved in Women's Hormonal Health and Reproductive System Diseases. Sakhteman A, Pasdaran A, Afifi M, Hamedi A. J Evid Based Integr Med 25 2515690X20932527 (2020)
  33. Computational Study of Bis-(1-(Benzoyl)-3-Methyl Thiourea) Platinum (II) Complex Derivatives as Anticancer Candidates. Ruswanto R, Mardianingrum R, Nofianti T, Fizriani R, Siswandono S. Adv Appl Bioinform Chem 16 15-36 (2023)
  34. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. Bassetto M, Ferla S, Giancotti G, Pertusati F, Westwell AD, Brancale A, McGuigan C. Medchemcomm 8 1414-1420 (2017)


Reviews citing this publication (54)

  1. Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis. Scher HI, Sawyers CL. J Clin Oncol 23 8253-8261 (2005)
  2. Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore. Fleming FF, Yao L, Ravikumar PC, Funk L, Shook BC. J Med Chem 53 7902-7917 (2010)
  3. Androgen receptor functions in castration-resistant prostate cancer and mechanisms of resistance to new agents targeting the androgen axis. Yuan X, Cai C, Chen S, Chen S, Yu Z, Balk SP. Oncogene 33 2815-2825 (2014)
  4. Androgen receptors in hormone-dependent and castration-resistant prostate cancer. Shafi AA, Yen AE, Weigel NL. Pharmacol Ther 140 223-238 (2013)
  5. Drug insight: Testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging. Bhasin S, Calof OM, Storer TW, Lee ML, Mazer NA, Jasuja R, Montori VM, Gao W, Dalton JT. Nat Clin Pract Endocrinol Metab 2 146-159 (2006)
  6. Drug insight: role of the androgen receptor in the development and progression of prostate cancer. Taplin ME. Nat Clin Pract Oncol 4 236-244 (2007)
  7. Targeting the androgen receptor pathway in castration-resistant prostate cancer: progresses and prospects. Ferraldeschi R, Welti J, Luo J, Attard G, de Bono JS. Oncogene 34 1745-1757 (2015)
  8. Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs). Gao W, Dalton JT. Drug Discov Today 12 241-248 (2007)
  9. Selective androgen receptor modulators as function promoting therapies. Bhasin S, Jasuja R. Curr Opin Clin Nutr Metab Care 12 232-240 (2009)
  10. Towards precision oncology in advanced prostate cancer. Ku SY, Gleave ME, Beltran H. Nat Rev Urol 16 645-654 (2019)
  11. Discovery and therapeutic promise of selective androgen receptor modulators. Chen J, Kim J, Dalton JT. Mol Interv 5 173-188 (2005)
  12. Selective androgen receptor modulators in preclinical and clinical development. Narayanan R, Mohler ML, Bohl CE, Miller DD, Dalton JT. Nucl Recept Signal 6 e010 (2008)
  13. Mechanisms of Therapeutic Resistance in Prostate Cancer. Nakazawa M, Paller C, Kyprianou N. Curr Oncol Rep 19 13 (2017)
  14. Androgen receptor antagonists for prostate cancer therapy. Helsen C, Van den Broeck T, Voet A, Prekovic S, Van Poppel H, Joniau S, Claessens F. Endocr Relat Cancer 21 T105-18 (2014)
  15. Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands. Gao W, Kim J, Dalton JT. Pharm Res 23 1641-1658 (2006)
  16. Androgen receptor and prostate cancer. Richter E, Srivastava S, Dobi A. Prostate Cancer Prostatic Dis 10 114-118 (2007)
  17. Moving Beyond the Androgen Receptor (AR): Targeting AR-Interacting Proteins to Treat Prostate Cancer. Foley C, Mitsiades N. Horm Cancer 7 84-103 (2016)
  18. Constitutive activity of the androgen receptor. Chan SC, Dehm SM. Adv Pharmacol 70 327-366 (2014)
  19. Androgen receptor: role and novel therapeutic prospects in prostate cancer. Taplin ME. Expert Rev Anticancer Ther 8 1495-1508 (2008)
  20. Recent developments in antiandrogens and selective androgen receptor modulators. Haendler B, Cleve A. Mol Cell Endocrinol 352 79-91 (2012)
  21. Maximal androgen blockade for advanced prostate cancer. Klotz L. Best Pract Res Clin Endocrinol Metab 22 331-340 (2008)
  22. Novel therapeutic approaches for the treatment of castration-resistant prostate cancer. Heidegger I, Massoner P, Eder IE, Pircher A, Pichler R, Aigner F, Bektic J, Horninger W, Klocker H. J Steroid Biochem Mol Biol 138 248-256 (2013)
  23. Androgen receptor variation affects prostate cancer progression and drug resistance. McCrea E, Sissung TM, Price DK, Chau CH, Figg WD. Pharmacol Res 114 152-162 (2016)
  24. Enzalutamide and blocking androgen receptor in advanced prostate cancer: lessons learnt from the history of drug development of antiandrogens. Ito Y, Sadar MD. Res Rep Urol 10 23-32 (2018)
  25. Androgen deprivation therapy in castrate-resistant prostate cancer: how important is GnRH agonist backbone therapy? Merseburger AS, Hammerer P, Rozet F, Roumeguère T, Caffo O, da Silva FC, Alcaraz A. World J Urol 33 1079-1085 (2015)
  26. Androgen receptor as a therapeutic target. Gao W. Adv Drug Deliv Rev 62 1277-1284 (2010)
  27. Risks and benefits of hormonal manipulation as monotherapy or adjuvant treatment in localised prostate cancer. Abrahamsson PA, Anderson J, Boccon-Gibod L, Schulman C, Studer UE, Wirth M. Eur Urol 48 900-905 (2005)
  28. Endocrine disrupting compounds and prostate cancer. Hess-Wilson JK, Knudsen KE. Cancer Lett 241 1-12 (2006)
  29. Secondary hormonal therapy for prostate cancer: what lies on the horizon? Sharifi N, Dahut WL, Figg WD. BJU Int 101 271-274 (2008)
  30. Mechanisms of prostate cancer progression to androgen independence. McPhaul MJ. Best Pract Res Clin Endocrinol Metab 22 373-388 (2008)
  31. Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021. Wu Q, Qian W, Sun X, Jiang S. J Hematol Oncol 15 143 (2022)
  32. Combined androgen blockade revisited: emerging options for the treatment of castration-resistant prostate cancer. Simmons MN, Klein EA. Urology 73 697-705 (2009)
  33. Structures of androgen receptor bound with ligands: advancing understanding of biological functions and drug discovery. Sakkiah S, Ng HW, Tong W, Hong H. Expert Opin Ther Targets 20 1267-1282 (2016)
  34. Using biochemistry and biophysics to extinguish androgen receptor signaling in prostate cancer. Asangani I, Blair IA, Van Duyne G, Hilser VJ, Moiseenkova-Bell V, Plymate S, Sprenger C, Wand AJ, Penning TM. J Biol Chem 296 100240 (2021)
  35. WOMEN IN CANCER THEMATIC REVIEW: New roles for nuclear receptors in prostate cancer. Leach DA, Powell SM, Bevan CL. Endocr Relat Cancer 23 T85-T108 (2016)
  36. Precision medicine applications in prostate cancer. McCrea EM, Lee DK, Sissung TM, Figg WD. Ther Adv Med Oncol 10 1758835918776920 (2018)
  37. Therapeutic targeting of the androgen receptor (AR) and AR variants in prostate cancer. Narayanan R. Asian J Urol 7 271-283 (2020)
  38. Antiandrogen withdrawal syndrome (AAWS) in the treatment of patients with prostate cancer. Leone G, Tucci M, Buttigliero C, Zichi C, Pignataro D, Bironzo P, Vignani F, Scagliotti GV, Di Maio M. Endocr Relat Cancer 25 R1-R9 (2018)
  39. Endocrine Disrupting Chemicals Mediated through Binding Androgen Receptor Are Associated with Diabetes Mellitus. Sakkiah S, Wang T, Zou W, Wang Y, Pan B, Tong W, Hong H. Int J Environ Res Public Health 15 E25 (2017)
  40. Androgen and estrogen receptors: potential of crystallography in the fight against cancer. Nahoum V, Bourguet W. Int J Biochem Cell Biol 39 1280-1287 (2007)
  41. Androgen receptor modulators: a marriage of chemistry and biology. McEwan IJ. Future Med Chem 5 1109-1120 (2013)
  42. Developments in nonsteroidal antiandrogens targeting the androgen receptor. Liu B, Su L, Geng J, Liu J, Zhao G. ChemMedChem 5 1651-1661 (2010)
  43. Non-Coding RNAs Set a New Phenotypic Frontier in Prostate Cancer Metastasis and Resistance. Altschuler J, Stockert JA, Kyprianou N. Int J Mol Sci 22 2100 (2021)
  44. The hurdle of antiandrogen drug resistance: drug design strategies. Trendel JA. Expert Opin Drug Discov 8 1491-1501 (2013)
  45. Cheminformatics Driven Development of Novel Therapies for Drug Resistant Prostate Cancer. Ban F, Dalal K, LeBlanc E, Morin H, Rennie PS, Cherkasov A. Mol Inform 37 e1800043 (2018)
  46. Pharmacotherapy for prostate cancer, with emphasis on hormonal treatments. Barmoshe S, Zlotta AR. Expert Opin Pharmacother 7 1685-1699 (2006)
  47. Recent advances in allosteric androgen receptor inhibitors for the potential treatment of castration-resistant prostate cancer. Martinez-Ariza G, Hulme C. Pharm Pat Anal 4 387-402 (2015)
  48. Resistance to second generation antiandrogens in prostate cancer: pathways and mechanisms. Verma S, Prajapati KS, Kushwaha PP, Shuaib M, Kumar Singh A, Kumar S, Gupta S. Cancer Drug Resist 3 742-761 (2020)
  49. Current treatment options for newly diagnosed metastatic hormone-sensitive prostate cancer-a narrative review. Ong S, O'Brien J, Medhurst E, Lawrentschuk N, Murphy D, Azad A. Transl Androl Urol 10 3918-3930 (2021)
  50. Molecular and Functional Diagnostic Tools in Precision Oncology for Urological Malignancies. Sekar V, Mehrotra DG, Majumder B. Indian J Surg Oncol 8 24-32 (2017)
  51. [Myoanabolic steroids and selective androgen receptor modulators: mechanism of action and perspectives]. Tóth M. Orv Hetil 150 2051-2059 (2009)
  52. Assessment of Prostate and Bladder Cancer Genomic Biomarkers Using Artificial Intelligence: a Systematic Review. Bazarkin A, Morozov A, Androsov A, Fajkovic H, Rivas JG, Singla N, Koroleva S, Teoh JY, Zvyagin AV, Shariat SF, Somani B, Enikeev D. Curr Urol Rep 25 19-35 (2024)
  53. Liver Microenvironment Response to Prostate Cancer Metastasis and Hormonal Therapy. Buxton AK, Abbasova S, Bevan CL, Leach DA. Cancers (Basel) 14 6189 (2022)
  54. [Development of novel nuclear receptor ligands based on receptor-folding inhibition hypothesis]. Tanatani A. Yakugaku Zasshi 127 341-351 (2007)

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  1. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A, Wasielewska T, Welsbie D, Chen CD, Higano CS, Beer TM, Hung DT, Scher HI, Jung ME, Sawyers CL. Science 324 787-790 (2009)
  2. Anti-androgens and androgen-depleting therapies in prostate cancer: new agents for an established target. Chen Y, Clegg NJ, Scher HI. Lancet Oncol 10 981-991 (2009)
  3. Suppression of androgen receptor-mediated gene expression by a sequence-specific DNA-binding polyamide. Nickols NG, Dervan PB. Proc Natl Acad Sci U S A 104 10418-10423 (2007)
  4. Comparison of crystal structures of human androgen receptor ligand-binding domain complexed with various agonists reveals molecular determinants responsible for binding affinity. Pereira de Jésus-Tran K, Côté PL, Cantin L, Blanchet J, Labrie F, Breton R. Protein Sci 15 987-999 (2006)
  5. Functional analysis of androgen receptor mutations that confer anti-androgen resistance identified in circulating cell-free DNA from prostate cancer patients. Lallous N, Volik SV, Awrey S, Leblanc E, Tse R, Murillo J, Singh K, Azad AA, Wyatt AW, LeBihan S, Chi KN, Gleave ME, Rennie PS, Collins CC, Cherkasov A. Genome Biol 17 10 (2016)
  6. Androgen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancer. Vasaitis T, Belosay A, Schayowitz A, Khandelwal A, Chopra P, Gediya LK, Guo Z, Fang HB, Njar VC, Brodie AM. Mol Cancer Ther 7 2348-2357 (2008)
  7. A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. Fagart J, Hillisch A, Huyet J, Bärfacker L, Fay M, Pleiss U, Pook E, Schäfer S, Rafestin-Oblin ME, Kolkhof P. J Biol Chem 285 29932-29940 (2010)
  8. Antitumor agents. 250. Design and synthesis of new curcumin analogues as potential anti-prostate cancer agents. Lin L, Shi Q, Nyarko AK, Bastow KF, Wu CC, Su CY, Shih CC, Lee KH. J Med Chem 49 3963-3972 (2006)
  9. Ligand-specific dynamics of the androgen receptor at its response element in living cells. Klokk TI, Kurys P, Elbi C, Nagaich AK, Hendarwanto A, Slagsvold T, Chang CY, Hager GL, Saatcioglu F. Mol Cell Biol 27 1823-1843 (2007)
  10. Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. Dalal K, Roshan-Moniri M, Sharma A, Li H, Ban F, Hessein M, Hsing M, Singh K, LeBlanc E, Dehm S, Tomlinson Guns ES, Cherkasov A, Rennie PS. J Biol Chem 289 26417-26429 (2014)
  11. Androgen receptor serine 81 phosphorylation mediates chromatin binding and transcriptional activation. Chen S, Gulla S, Cai C, Balk SP. J Biol Chem 287 8571-8583 (2012)
  12. Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer. Yang YC, Banuelos CA, Mawji NR, Wang J, Kato M, Haile S, McEwan IJ, Plymate S, Sadar MD. Clin Cancer Res 22 4466-4477 (2016)
  13. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Guerrero J, Alfaro IE, Gómez F, Protter AA, Bernales S. Prostate 73 1291-1305 (2013)
  14. Recent advances in the investigation of curcuminoids. Itokawa H, Shi Q, Akiyama T, Morris-Natschke SL, Lee KH. Chin Med 3 11 (2008)
  15. Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor. Yu Z, Cai C, Gao S, Simon NI, Shen HC, Balk SP. Clin Cancer Res 20 4075-4085 (2014)
  16. Crystal structure of the T877A human androgen receptor ligand-binding domain complexed to cyproterone acetate provides insight for ligand-induced conformational changes and structure-based drug design. Bohl CE, Wu Z, Miller DD, Bell CE, Dalton JT. J Biol Chem 282 13648-13655 (2007)
  17. Interleukin-6 increases prostate cancer cells resistance to bicalutamide via TIF2. Feng S, Tang Q, Sun M, Chun JY, Evans CP, Gao AC. Mol Cancer Ther 8 665-671 (2009)
  18. Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Bisson WH, Cheltsov AV, Bruey-Sedano N, Lin B, Chen J, Goldberger N, May LT, Christopoulos A, Dalton JT, Sexton PM, Zhang XK, Abagyan R. Proc Natl Acad Sci U S A 104 11927-11932 (2007)
  19. Renin-angiotensin system is an important factor in hormone refractory prostate cancer. Uemura H, Hasumi H, Ishiguro H, Teranishi J, Miyoshi Y, Kubota Y. Prostate 66 822-830 (2006)
  20. Mechanism of androgen receptor antagonism by bicalutamide in the treatment of prostate cancer. Osguthorpe DJ, Hagler AT. Biochemistry 50 4105-4113 (2011)
  21. Detecting predictive androgen receptor modifications in circulating prostate cancer cells. Steinestel J, Luedeke M, Arndt A, Schnoeller TJ, Lennerz JK, Wurm C, Maier C, Cronauer MV, Steinestel K, Schrader AJ. Oncotarget 10 4213-4223 (2019)
  22. Niclosamide and Bicalutamide Combination Treatment Overcomes Enzalutamide- and Bicalutamide-Resistant Prostate Cancer. Liu C, Armstrong CM, Lou W, Lombard AP, Cucchiara V, Gu X, Yang JC, Nadiminty N, Pan CX, Evans CP, Gao AC. Mol Cancer Ther 16 1521-1530 (2017)
  23. Noncanonical Wnt signaling mediates androgen-dependent tumor growth in a mouse model of prostate cancer. Takahashi S, Watanabe T, Okada M, Inoue K, Ueda T, Takada I, Watabe T, Yamamoto Y, Fukuda T, Nakamura T, Akimoto C, Fujimura T, Hoshino M, Imai Y, Metzger D, Miyazono K, Minami Y, Chambon P, Kitamura T, Matsumoto T, Kato S. Proc Natl Acad Sci U S A 108 4938-4943 (2011)
  24. Antiandrogen gold nanoparticles dual-target and overcome treatment resistance in hormone-insensitive prostate cancer cells. Dreaden EC, Gryder BE, Austin LA, Tene Defo BA, Hayden SC, Pi M, Quarles LD, Oyelere AK, El-Sayed MA. Bioconjug Chem 23 1507-1512 (2012)
  25. Improved docking, screening and selectivity prediction for small molecule nuclear receptor modulators using conformational ensembles. Park SJ, Kufareva I, Abagyan R. J Comput Aided Mol Des 24 459-471 (2010)
  26. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. Ponnusamy S, Coss CC, Thiyagarajan T, Watts K, Hwang DJ, He Y, Selth LA, McEwan IJ, Duke CB, Pagadala J, Singh G, Wake RW, Ledbetter C, Tilley WD, Moldoveanu T, Dalton JT, Miller DD, Narayanan R. Cancer Res 77 6282-6298 (2017)
  27. Allosteric conversation in the androgen receptor ligand-binding domain surfaces. Grosdidier S, Carbó LR, Buzón V, Brooke G, Nguyen P, Baxter JD, Bevan C, Webb P, Estébanez-Perpiñá E, Fernández-Recio J. Mol Endocrinol 26 1078-1090 (2012)
  28. Marketed Drugs Can Inhibit Cytochrome P450 27A1, a Potential New Target for Breast Cancer Adjuvant Therapy. Mast N, Lin JB, Pikuleva IA. Mol Pharmacol 88 428-436 (2015)
  29. Systematic structure-function analysis of androgen receptor Leu701 mutants explains the properties of the prostate cancer mutant L701H. van de Wijngaart DJ, Molier M, Lusher SJ, Hersmus R, Jenster G, Trapman J, Dubbink HJ. J Biol Chem 285 5097-5105 (2010)
  30. Bicalutamide failure in prostate cancer treatment: involvement of Multi Drug Resistance proteins. Colabufo NA, Pagliarulo V, Berardi F, Contino M, Inglese C, Niso M, Ancona P, Albo G, Pagliarulo A, Perrone R. Eur J Pharmacol 601 38-42 (2008)
  31. Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models. Sugawara T, Baumgart SJ, Nevedomskaya E, Reichert K, Steuber H, Lejeune P, Mumberg D, Haendler B. Int J Cancer 145 1382-1394 (2019)
  32. Antiandrogen withdrawal syndrome and alternative antiandrogen therapy associated with the W741C mutant androgen receptor in a novel prostate cancer xenograft. Terada N, Shimizu Y, Yoshida T, Maeno A, Kamba T, Inoue T, Nakamura E, Kamoto T, Ogawa O. Prostate 70 252-261 (2010)
  33. Determining direct binders of the Androgen Receptor using a high-throughput Cellular Thermal Shift Assay. Shaw J, Leveridge M, Norling C, Karén J, Molina DM, O'Neill D, Dowling JE, Davey P, Cowan S, Dabrowski M, Main M, Gianni D. Sci Rep 8 163 (2018)
  34. Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators. Bohl CE, Wu Z, Chen J, Mohler ML, Yang J, Hwang DJ, Mustafa S, Miller DD, Bell CE, Dalton JT. Bioorg Med Chem Lett 18 5567-5570 (2008)
  35. Clinical efficacy of alternative antiandrogen therapy in Japanese men with relapsed prostate cancer after first-line hormonal therapy. Okihara K, Ukimura O, Kanemitsu N, Mizutani Y, Kawauchi A, Miki T, Kyoto Prefectural University of Medicine Prostate Cancer Research Group. Int J Urol 14 128-132 (2007)
  36. In silico discovery of androgen receptor antagonists with activity in castration resistant prostate cancer. Shen HC, Shanmugasundaram K, Simon NI, Cai C, Wang H, Chen S, Balk SP, Rigby AC. Mol Endocrinol 26 1836-1846 (2012)
  37. Characterization of the in vitro metabolism of selective androgen receptor modulator using human, rat, and dog liver enzyme preparations. Gao W, Wu Z, Bohl CE, Yang J, Miller DD, Dalton JT. Drug Metab Dispos 34 243-253 (2006)
  38. Circumventing anti-androgen resistance by molecular design. McGinley PL, Koh JT. J Am Chem Soc 129 3822-3823 (2007)
  39. Growth and migration of LNCaP prostate cancer cells are promoted by triclosan and benzophenone-1 via an androgen receptor signaling pathway. Kim SH, Hwang KA, Shim SM, Choi KC. Environ Toxicol Pharmacol 39 568-576 (2015)
  40. Visible-light-induced multicomponent cascade cycloaddition involving N-propargyl aromatic amines, diaryliodonium salts and sulfur dioxide: rapid access to 3-arylsulfonylquinolines. Sun D, Yin K, Zhang R. Chem Commun (Camb) 54 1335-1338 (2018)
  41. X-ray structures of progesterone receptor ligand binding domain in its agonist state reveal differing mechanisms for mixed profiles of 11β-substituted steroids. Lusher SJ, Raaijmakers HC, Vu-Pham D, Kazemier B, Bosch R, McGuire R, Azevedo R, Hamersma H, Dechering K, Oubrie A, van Duin M, de Vlieg J. J Biol Chem 287 20333-20343 (2012)
  42. Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring. Ohta K, Goto T, Fijii S, Suzuki T, Ohta S, Endo Y. Bioorg Med Chem 16 8022-8028 (2008)
  43. Molecular basis of agonicity and antagonicity in the androgen receptor studied by molecular dynamics simulations. Bisson WH, Abagyan R, Cavasotto CN. J Mol Graph Model 27 452-458 (2008)
  44. Molecular determinants of the recognition of ulipristal acetate by oxo-steroid receptors. Petit-Topin I, Fay M, Resche-Rigon M, Ulmann A, Gainer E, Rafestin-Oblin ME, Fagart J. J Steroid Biochem Mol Biol 144 Pt B 427-435 (2014)
  45. Structure-based virtual screening and identification of a novel androgen receptor antagonist. Song CH, Yang SH, Park E, Cho SH, Gong EY, Khadka DB, Cho WJ, Lee K. J Biol Chem 287 30769-30780 (2012)
  46. Agonist-mediated docking of androgen receptor onto the mitotic chromatin platform discriminates intrinsic mode of action of prostate cancer drugs. Kumar S, Chaturvedi NK, Kumar S, Tyagi RK. Biochim Biophys Acta 1783 59-73 (2008)
  47. Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens. Shi Q, Wada K, Ohkoshi E, Lin L, Huang R, Morris-Natschke SL, Goto M, Lee KH. Bioorg Med Chem 20 4020-4031 (2012)
  48. Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. Bassetto M, Ferla S, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C. Eur J Med Chem 118 230-243 (2016)
  49. Interaction mechanism exploration of R-bicalutamide/S-1 with WT/W741L AR using molecular dynamics simulations. Liu H, An X, Li S, Wang Y, Li J, Liu H. Mol Biosyst 11 3347-3354 (2015)
  50. Small molecule screening reveals a transcription-independent pro-survival function of androgen receptor in castration-resistant prostate cancer. Narizhneva NV, Tararova ND, Ryabokon P, Shyshynova I, Prokvolit A, Komarov PG, Purmal AA, Gudkov AV, Gurova KV. Cell Cycle 8 4155-4167 (2009)
  51. Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. Hwang DJ, Yang J, Xu H, Rakov IM, Mohler ML, Dalton JT, Miller DD. Bioorg Med Chem 14 6525-6538 (2006)
  52. Targeting androgen receptor phase separation to overcome antiandrogen resistance. Xie J, He H, Kong W, Li Z, Gao Z, Xie D, Sun L, Fan X, Jiang X, Zheng Q, Li G, Zhu J, Zhu G. Nat Chem Biol 18 1341-1350 (2022)
  53. The discovery of novel human androgen receptor antagonist chemotypes using a combined pharmacophore screening procedure. Voet A, Helsen C, Zhang KY, Claessens F. ChemMedChem 8 644-651 (2013)
  54. Acidic heterocycles as novel hydrophilic pharmacophore of androgen receptor ligands with a carborane core structure. Fujii S, Ohta K, Goto T, Kagechika H, Endo Y. Bioorg Med Chem 17 344-350 (2009)
  55. CYP3A5 regulates prostate cancer cell growth by facilitating nuclear translocation of AR. Mitra R, Goodman OB. Prostate 75 527-538 (2015)
  56. Gartanin, an isoprenylated xanthone from the mangosteen fruit (Garcinia mangostana), is an androgen receptor degradation enhancer. Li G, Petiwala SM, Yan M, Won JH, Petukhov PA, Johnson JJ. Mol Nutr Food Res 60 1458-1469 (2016)
  57. In vitro and in vivo structure-activity relationships of novel androgen receptor ligands with multiple substituents in the B-ring. Chen J, Hwang DJ, Chung K, Bohl CE, Fisher SJ, Miller DD, Dalton JT. Endocrinology 146 5444-5454 (2005)
  58. Proteomic-coupled-network analysis of T877A-androgen receptor interactomes can predict clinical prostate cancer outcomes between White (non-Hispanic) and African-American groups. Zaman N, Giannopoulos PN, Chowdhury S, Bonneil E, Thibault P, Wang E, Trifiro M, Paliouras M. PLoS One 9 e113190 (2014)
  59. Sulforaphane increases the efficacy of anti-androgens by rapidly decreasing androgen receptor levels in prostate cancer cells. Khurana N, Talwar S, Chandra PK, Sharma P, Abdel-Mageed AB, Mondal D, Sikka SC. Int J Oncol 49 1609-1619 (2016)
  60. Evaluation of Darolutamide (ODM201) Efficiency on Androgen Receptor Mutants Reported to Date in Prostate Cancer Patients. Lallous N, Snow O, Sanchez C, Parra Nuñez AK, Sun B, Hussain A, Lee J, Morin H, Leblanc E, Gleave ME, Cherkasov A. Cancers (Basel) 13 2939 (2021)
  61. Rhodium-catalyzed addition of sulfonyl hydrazides to allenes: regioselective synthesis of branched allylic sulfones. Khakyzadeh V, Wang YH, Breit B. Chem Commun (Camb) 53 4966-4968 (2017)
  62. 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment. Ferroni C, Pepe A, Kim YS, Lee S, Guerrini A, Parenti MD, Tesei A, Zamagni A, Cortesi M, Zaffaroni N, De Cesare M, Beretta GL, Trepel JB, Malhotra SV, Varchi G. J Med Chem 60 3082-3093 (2017)
  63. Changes to the dihydropyrimidine dehydrogenase gene copy number influence the susceptibility of cancers to 5-FU-based drugs: Data mining of the NCI-DTP data sets and validation with human tumour xenografts. Kobunai T, Ooyama A, Sasaki S, Wierzba K, Takechi T, Fukushima M, Watanabe T, Nagawa H. Eur J Cancer 43 791-798 (2007)
  64. Development of a benzopyran-containing androgen receptor antagonist to treat antiandrogen-resistant prostate cancer. Oh S, Nam HJ, Park J, Beak SH, Park SB. ChemMedChem 5 529-533 (2010)
  65. Impaired helix 12 dynamics due to proline 892 substitutions in the androgen receptor are associated with complete androgen insensitivity. Elhaji YA, Stoica I, Dennis S, Purisima EO, Lumbroso R, Beitel LK, Trifiro MA. Hum Mol Genet 15 921-931 (2006)
  66. Nonsteroidal selective androgen receptor modulators enhance female sexual motivation. Jones A, Hwang DJ, Duke CB, He Y, Siddam A, Miller DD, Dalton JT. J Pharmacol Exp Ther 334 439-448 (2010)
  67. Protocadherin B9 promotes resistance to bicalutamide and is associated with the survival of prostate cancer patients. Sekino Y, Oue N, Mukai S, Shigematsu Y, Goto K, Sakamoto N, Sentani K, Hayashi T, Teishima J, Matsubara A, Yasui W. Prostate 79 234-242 (2019)
  68. 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. Wakabayashi K, Imai K, Miyachi H, Hashimoto Y, Tanatani A. Bioorg Med Chem 16 6799-6812 (2008)
  69. One-Pot Synthesis of Allylic Sulfones, Ketosulfones, and Triflyl Allylic Alcohols from Domino Reactions of Allylic Alcohols with Sulfinic Acid under Metal-Free Conditions. Chu XQ, Meng H, Xu XP, Ji SJ. Chemistry 21 11359-11368 (2015)
  70. Prosaposin is a novel androgen-regulated gene in prostate cancer cell line LNCaP. Koochekpour S, Lee TJ, Wang R, Sun Y, Delorme N, Hiraiwa M, Grabowski GA, Culig Z, Minokadeh A. J Cell Biochem 101 631-641 (2007)
  71. Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production. Hu LY, Lei HJ, Du D, Johnson TR, Fedij V, Kostlan C, Yue WS, Lovdahl M, Li JJ, Carroll M, Dettling D, Asbill J, Fan C, Wade K, Pocalyko D, Lapham K, Yalamanchili R, Samas B, Vrieze D, Ciotti S, Krieger-Burke T, Sliskovic D, Welgus H. Bioorg Med Chem Lett 17 5693-5697 (2007)
  72. Aldol derivatives of Thioxoimidazolidinones as potential anti-prostate cancer agents. Khatik GL, Kaur J, Kumar V, Tikoo K, Venugopalan P, Nair VA. Eur J Med Chem 46 3291-3301 (2011)
  73. Apples and oranges. Re: 7.4-year update of the ongoing bicalutamide Early Prostate Cancer (EPC) trial programme. Sternberg CN. BJU Int 97 435-438 (2006)
  74. BAY 1024767 blocks androgen receptor mutants found in castration-resistant prostate cancer patients. Sugawara T, Lejeune P, Köhr S, Neuhaus R, Faus H, Gelato KA, Busemann M, Cleve A, Lücking U, von Nussbaum F, Brands M, Mumberg D, Jung K, Stephan C, Haendler B. Oncotarget 7 6015-6028 (2016)
  75. Crystal structure, docking study and structure-activity relationship of carborane-containing androgen receptor antagonist 3-(12-hydroxymethyl-1,12-dicarba-closo-dodecaboran-1-yl)benzonitrile. Ohta K, Goto T, Fujii S, Kawahata M, Oda A, Ohta S, Yamaguchi K, Hirono S, Endo Y. Bioorg Med Chem 19 3540-3548 (2011)
  76. Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists. Yamada A, Fujii S, Mori S, Kagechika H. ACS Med Chem Lett 4 937-941 (2013)
  77. (1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production. Hu LY, Du D, Hoffman J, Smith Y, Fedij V, Kostlan C, Johnson TR, Huang Y, Kesten S, Harter W, Yue WS, Li JJ, Barvian N, Mitchell L, Lei HJ, Lefker B, Carroll M, Dettling D, Krieger-Burke T, Samas B, Yalamanchili R, Lapham K, Pocalyko D, Sliskovic D, Ciotti S, Stoller B, Hena MA, Ding Q, Maiti SN, Stier M, Welgus H. Bioorg Med Chem Lett 17 5983-5988 (2007)
  78. Carnosic acid promotes degradation of the androgen receptor and is regulated by the unfolded protein response pathway in vitro and in vivo. Petiwala SM, Li G, Bosland MC, Lantvit DD, Petukhov PA, Johnson JJ. Carcinogenesis 37 827-838 (2016)
  79. Deep Learning Modeling of Androgen Receptor Responses to Prostate Cancer Therapies. Snow O, Lallous N, Ester M, Cherkasov A. Int J Mol Sci 21 E5847 (2020)
  80. Discovery of an orally-active nonsteroidal androgen receptor pure antagonist and the structure-activity relationships of its derivatives. Tachibana K, Imaoka I, Shiraishi T, Yoshino H, Nakamura M, Ohta M, Kawata H, Taniguchi K, Ishikura N, Tsunenari T, Saito H, Nagamuta M, Nakagawa T, Takanashi K, Onuma E, Sato H. Chem Pharm Bull (Tokyo) 56 1555-1561 (2008)
  81. Iminoenamine based novel androgen receptor antagonist exhibited anti-prostate cancer activity in androgen independent prostate cancer cells through inhibition of AKT pathway. Divakar S, Saravanan K, Karthikeyan P, Elancheran R, Kabilan S, Balasubramanian KK, Devi R, Kotoky J, Ramanathan M. Chem Biol Interact 275 22-34 (2017)
  82. PARP7 mono-ADP-ribosylates the agonist conformation of the androgen receptor in the nucleus. Kamata T, Yang CS, Paschal BM. Biochem J 478 2999-3014 (2021)
  83. Predicting anti-androgenic activity of bisphenols using molecular docking and quantitative structure-activity relationships. Yang X, Liu H, Yang Q, Liu J, Chen J, Shi L. Chemosphere 163 373-381 (2016)
  84. A multi-parameter imaging assay identifies different stages of ligand-induced androgen receptor activation. van Royen ME, van de Wijngaart DJ, Cunha SM, Trapman J, Houtsmuller AB. Cytometry A 83 806-817 (2013)
  85. Design and evaluation of novel oxadiazole derivatives as potential prostate cancer agents. Mochona B, Qi X, Euynni S, Sikazwi D, Mateeva N, Soliman KF. Bioorg Med Chem Lett 26 2847-2851 (2016)
  86. Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists. Ivachtchenko AV, Ivanenkov YA, Mitkin OD, Vorobiev AA, Kuznetsova IV, Shevkun NA, Koryakova AG, Karapetian RN, Trifelenkov AS, Kravchenko DV, Veselov MS, Chufarova NV. Eur J Med Chem 99 51-66 (2015)
  87. Discovery of Novel Androgen Receptor Ligands by Structure-based Virtual Screening and Bioassays. Zhou W, Duan M, Fu W, Pang J, Tang Q, Sun H, Xu L, Chang S, Li D, Hou T. Genomics Proteomics Bioinformatics 16 416-427 (2018)
  88. Perspectives on designs of antiandrogens for prostate cancer. Estébanez-Perpiñá E, Jouravel N, Fletterick RJ. Expert Opin Drug Discov 2 1341-1355 (2007)
  89. Prior switching to a second-line nonsteroidal antiandrogen does not impact the therapeutic efficacy of abiraterone acetate in patients with metastatic castration-resistant prostate cancer: a real-world retrospective study. Zhao JG, Liu JD, Shen PF, Tang X, Sun GX, Zhang XM, Chen JR, Shu KP, Shi M, Zeng H. Asian J Androl 20 545-550 (2018)
  90. Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. Saravanan K, Elancheran R, Divakar S, Anand SA, Ramanathan M, Kotoky J, Lokanath NK, Kabilan S. Bioorg Med Chem Lett 27 1199-1204 (2017)
  91. Discovery of novel androgen receptor antagonists: a hybrid approach of pharmacophore-based and docking-based virtual screening. Liu J, Liu B, Guo G, Jing Y, Zhao G. Anticancer Drugs 26 747-753 (2015)
  92. Discovery of novel antagonists targeting the DNA binding domain of androgen receptor by integrated docking-based virtual screening and bioassays. Pang JP, Shen C, Zhou WF, Wang YX, Shan LH, Chai X, Shao Y, Hu XP, Zhu F, Zhu DY, Xiao L, Xu L, Xu XH, Li D, Hou TJ. Acta Pharmacol Sin 43 229-239 (2022)
  93. Preclinical pharmacology of a nonsteroidal ligand for androgen receptor-mediated imaging of prostate cancer. Yang J, Bohl CE, Nair VA, Mustafa SM, Hong SS, Miller DD, Dalton JT. J Pharmacol Exp Ther 317 402-408 (2006)
  94. The indications of tautomeric conversion in amorphous bicalutamide drug. Rams-Baron M, Wlodarczyk P, Dulski M, Wlodarczyk A, Kruk D, Rachocki A, Jachowicz R, Paluch M. Eur J Pharm Sci 110 117-123 (2017)
  95. CH5137291, an androgen receptor nuclear translocation-inhibiting compound, inhibits the growth of castration-resistant prostate cancer cells. Ishikura N, Kawata H, Nishimoto A, Nakamura R, Tsunenari T, Watanabe M, Tachibana K, Shiraishi T, Yoshino H, Honma A, Emura T, Ohta M, Nakagawa T, Houjo T, Corey E, Vessella RL, Aoki Y, Sato H. Int J Oncol 46 1560-1572 (2015)
  96. Development of Androgen-Antagonistic Coumarinamides with a Unique Aromatic Folded Pharmacophore. Koga H, Negishi M, Kinoshita M, Fujii S, Mori S, Ishigami-Yuasa M, Kawachi E, Kagechika H, Tanatani A. Int J Mol Sci 21 E5584 (2020)
  97. High intratumoral dihydrotestosterone is associated with antiandrogen resistance in VCaP prostate cancer xenografts in castrated mice. Huhtaniemi R, Sipilä P, Junnila A, Oksala R, Knuuttila M, Mehmood A, Aho E, Laajala TD, Aittokallio T, Laiho A, Elo L, Ohlsson C, Thulin MH, Kallio P, Mäkelä S, Mustonen MVJ, Poutanen M. iScience 25 104287 (2022)
  98. Learning from estrogen receptor antagonism: structure-based identification of novel antiandrogens effective against multiple clinically relevant androgen receptor mutants. Liu B, Geng G, Lin R, Ren C, Wu JH. Chem Biol Drug Des 79 300-312 (2012)
  99. Quantitative Evaluation of the Transcriptional Activity of Steroid Hormone Receptor Mutants and Variants Using a Single Vector With Two Reporters and a Receptor Expression Cassette. Ji H, Li Y, Liu Z, Tang M, Zou L, Su F, Zhang Y, Zhang J, Li H, Li L, Ai B, Ma J, Wang L, Liu M, Xiao F. Front Endocrinol (Lausanne) 11 167 (2020)
  100. Structural Based Screening of Antiandrogen Targeting Activation Function-2 Binding Site. Liu Y, Wu M, Wang T, Xie Y, Cui X, He L, He Y, Li X, Liu M, Hu L, Cen S, Zhou J. Front Pharmacol 9 1419 (2018)
  101. Structural basis for computational screening of non-steroidal androgen receptor ligands. Nyrönen TH, Söderholm AA. Expert Opin Drug Discov 5 5-20 (2010)
  102. The T850D Phosphomimetic Mutation in the Androgen Receptor Ligand Binding Domain Enhances Recruitment at Activation Function 2. Helsen C, Nguyen T, Vercruysse T, Wouters S, Daelemans D, Voet A, Claessens F. Int J Mol Sci 23 1557 (2022)
  103. 11C, 12C and 13C-Cyanation of Electron-Rich Arenes via Organic Photoredox Catalysis. Wu X, Chen W, Holmberg-Douglas N, Bida GT, Tu X, Ma X, Wu Z, Nicewicz DA, Li Z. Chem 9 343-362 (2023)
  104. Design, Synthesis, and Biological Evaluation of (E)-N'-((1-Chloro-3,4-Dihydronaphthalen-2-yl)Methylene)Benzohydrazide Derivatives as Anti-prostate Cancer Agents. Arjun HA, Elancheran R, Manikandan N, Lakshmithendral K, Ramanathan M, Bhattacharjee A, Lokanath NK, Kabilan S. Front Chem 7 474 (2019)
  105. Pantolactams as androgen receptor antagonists for the topical suppression of sebum production. Sexton KE, Barrett S, Bridgwood K, Carroll M, Dettling D, Du D, Fakhoury S, Fedij V, Hu LY, Kostlan C, Pocalyko D, Raheja N, Smith Y, Shanmugasundaram V, Wade K. Bioorg Med Chem Lett 21 5230-5233 (2011)
  106. Preclinical pharmacology of FL442, a novel nonsteroidal androgen receptor modulator. Poutiainen PK, Huhtala T, Jääskeläinen T, Petsalo A, Küblbeck J, Kaikkonen S, Palvimo JJ, Raunio H, Närvänen A, Peräkylä M, Juvonen RO, Honkakoski P, Laatikainen R, Pulkkinen JT. Mol Cell Endocrinol 387 8-18 (2014)
  107. Roles of androgen-dependent and -independent activation of signal transduction pathways for cell proliferation of prostate cancer cells. Inoue T, Kobayashi T, Terada N, Shimizu Y, Kamoto T, Ogawa O, Nakamura E. Expert Rev Endocrinol Metab 2 689-704 (2007)
  108. Simulating androgen receptor selection in designer yeast. Zhang H, Zhang L, Xu Y, Chen S, Ma Z, Yao M, Li F, Li B, Yuan Y. Synth Syst Biotechnol 7 1108-1116 (2022)
  109. Synthesis of oxazolidinedione derived bicalutamide analogs. Nair VA, Mustafa SM, Mohler ML, Dalton JT, Miller DD. Tetrahedron Lett 47 3953-3955 (2006)
  110. A hotspot for posttranslational modifications on the androgen receptor dimer interface drives pathology and anti-androgen resistance. Alegre-Martí A, Jiménez-Panizo A, Martínez-Tébar A, Poulard C, Peralta-Moreno MN, Abella M, Antón R, Chiñas M, Eckhard U, Piulats JM, Rojas AM, Fernández-Recio J, Rubio-Martínez J, Le Romancer M, Aytes Á, Fuentes-Prior P, Estébanez-Perpiñá E. Sci Adv 9 eade2175 (2023)
  111. A partially open conformation of an androgen receptor ligand-binding domain with drug-resistance mutations. Doamekpor SK, Peng P, Xu R, Ma L, Tong Y, Tong L. Acta Crystallogr F Struct Biol Commun 79 95-104 (2023)
  112. Discovery and Identification of Pyrazolopyramidine Analogs as Novel Potent Androgen Receptor Antagonists. Wang L, Song T, Wang X, Li J. Front Pharmacol 9 864 (2018)
  113. Discovery of novel 5-methyl-1H-pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation. Zhang D, Asnake S, Zhang J, Olsson PE, Zhao G. Chem Biol Drug Des 91 1113-1124 (2018)
  114. Estrogens drive the endoplasmic reticulum-associated degradation and promote proto-oncogene c-Myc expression in prostate cancer cells by androgen receptor/estrogen receptor signaling. Erzurumlu Y, Dogan HK, Catakli D, Aydogdu E, Muhammed MT. J Cell Commun Signal 17 793-811 (2023)
  115. Identification of bicalutamide resistance-related genes and prognosis prediction in patients with prostate cancer. Li Y, Wang H, Pan Y, Wang S, Zhang Z, Zhou H, Xu M, Liu X. Front Endocrinol (Lausanne) 14 1125299 (2023)
  116. The ERα-NRF2 signalling axis promotes bicalutamide resistance in prostate cancer. Tian L, Peng Y, Yang K, Cao J, Du X, Liang Z, Shi J, Zhang J. Cell Commun Signal 20 178 (2022)