SC912 inhibits AR-V7 activity in castration-resistant prostate cancer by targeting the androgen receptor N-terminal domain

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;79:263–82.

Article  CAS  PubMed  Google Scholar 

Potter GA, Barrie SE, Jarman M, Rowlands MG. Novel steroidal inhibitors of human cytochrome P45017. alpha.-Hydroxylase-C17, 20-lyase): potential agents for the treatment of prostatic cancer. J. Med. Chem. 1995;38:2463–71.

Article  CAS  PubMed  Google Scholar 

Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009;324:787–90.

Article  CAS  PubMed  PubMed Central  Google Scholar 

de Bono JS, Logothetis CJ, Molina A, Fizazi K, North S, Chu L, et al. Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med. 2011;364:1995–2005.

Article  PubMed  PubMed Central  Google Scholar 

Scher HI, Fizazi K, Saad F, Taplin ME, Sternberg CN, Miller K, et al. Increased survival with enzalutamide in prostate cancer after chemotherapy. N Engl J Med. 2012;367:1187–97.

Article  CAS  PubMed  Google Scholar 

Moilanen AM, Riikonen R, Oksala R, Ravanti L, Aho E, Wohlfahrt G, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Sci Rep. 2015;5:12007.

Article  PubMed  PubMed Central  Google Scholar 

Kanayama M, Lu C, Luo J, Antonarakis ES. AR splicing variants and resistance to AR targeting agents. Cancers. 2021;13:2563.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Uo T, Plymate SR, Sprenger CC. The potential of AR-V7 as a therapeutic target. Expert Opin Ther Targets. 2018;22:201–16.

Article  CAS  PubMed  Google Scholar 

Chan SC, Li Y, Dehm SM. Androgen receptor splice variants activate androgen receptor target genes and support aberrant prostate cancer cell growth independent of canonical androgen receptor nuclear localization signal. J Biol Chem. 2012;287:19736–49.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Kim S, Au CC, Jamalruddin MAB, Abou-Ghali NE, Mukhtar E, Portella L, et al. AR-V7 exhibits non-canonical mechanisms of nuclear import and chromatin engagement in castrate-resistant prostate cancer. Elife. 2022;11:e73396.

Article  PubMed  PubMed Central  Google Scholar 

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;129:192–208.

Article  PubMed  Google Scholar 

Welti J, Rodrigues DN, Sharp A, Sun S, Lorente D, Riisnaes R, et al. Analytical validation and clinical qualification of a new immunohistochemical assay for androgen receptor splice variant-7 protein expression in metastatic castration-resistant prostate cancer. Eur Urol. 2016;70:599–608.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Antonarakis ES, Lu C, Wang H, Luber B, Nakazawa M, Roeser JC, et al. AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer. N Engl J Med. 2014;371:1028–38.

Article  PubMed  PubMed Central  Google Scholar 

Antonarakis ES, Lu C, Luber B, Wang H, Chen Y, Nakazawa M, et al. Androgen receptor splice variant 7 and efficacy of taxane chemotherapy in patients with metastatic castration-resistant prostate cancer. JAMA Oncol. 2015;1:582–91.

Article  PubMed  PubMed Central  Google Scholar 

Li Y, Yang R, Henzler CM, Ho Y, Passow C, Auch B, et al. Diverse AR gene rearrangements mediate resistance to androgen receptor inhibitors in metastatic prostate cancerar gene rearrangements in prostate cancer. Clin Cancer Res. 2020;26:1965–76.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Annala M, Taavitsainen S, Khalaf DJ, Vandekerkhove G, Beja K, Sipola J, et al. Evolution of castration-resistant prostate cancer in ctDNA during sequential androgen receptor pathway inhibitionprostate cancer evolution during sequential ar inhibition. Clin Cancer Res. 2021;27:4610–23.

Article  CAS  PubMed  Google Scholar 

Liang J, Wang L, Poluben L, Nouri M, Arai S, Xie L, et al. Androgen receptor splice variant 7 functions independently of the full length receptor in prostate cancer cells. Cancer Lett. 2021;519:172–84.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Roggero CM, Jin L, Cao S, Sonavane R, Kopplin NG, Ta HQ, et al. A detailed characterization of stepwise activation of the androgen receptor variant 7 in prostate cancer cells. Oncogene. 2021;40:1106–17.

Article  CAS  PubMed  Google Scholar 

Andersen RJ, Mawji NR, Wang J, Wang G, Haile S, Myung JK, et al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010;17:535–46.

Article  CAS  PubMed  Google Scholar 

Dalal K, Che M, Que NS, Sharma A, Yang R, Lallous N, et al. Bypassing drug resistance mechanisms of prostate cancer with small molecules that target androgen receptor–chromatin interactionstargeting androgen receptor interactions with chromatin. Mol Cancer Ther. 2017;16:2281–91.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Dalal K, Ban F, Li H, Morin H, Roshan-Moniri M, Tam KJ, et al. Selectively targeting the dimerization interface of human androgen receptor with small-molecules to treat castration-resistant prostate cancer. Cancer Lett. 2018;437:35–43.

Article  CAS  PubMed  Google Scholar 

Ponnusamy S, He Y, Hwang D-J, Thiyagarajan T, Houtman R, Bocharova V, et al. Orally bioavailable androgen receptor degrader, potential next-generation therapeutic for enzalutamide-resistant prostate cancera novel ar degrader for the treatment of prostate cancer. Clin Cancer Res. 2019;25:6764–80.

Article  CAS  PubMed  Google Scholar 

Liu C, Armstrong CM, Ning S, Yang JC, Lou W, Lombard AP, et al. ARVib suppresses growth of advanced prostate cancer via inhibition of androgen receptor signaling. Oncogene. 2021;40:5379–92.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Lee GT, Nagaya N, Desantis J, Madura K, Sabaawy HE, Kim W-J. et al.Effects of MTX-23, a novel PROTAC of androgen receptor splice variant-7 and androgen receptor, on CRPC resistant to second-line antiandrogen therapy.Mol Cancer Ther. 2021;20:490–9.

Article  CAS  PubMed  Google Scholar 

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;41:1536–49.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Luna Velez MV, Verhaegh GW, Smit F, Sedelaar JPM, Schalken JA. Suppression of prostate tumor cell survival by antisense oligonucleotide-mediated inhibition of AR-V7 mRNA synthesis. Oncogene. 2019;38:3696–709.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Asangani IA, Dommeti VL, Wang X, Malik R, Cieslik M, Yang R, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014;510:278–82.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Welti J, Sharp A, Brooks N, Yuan W, McNair C, Chand SN, et al. Targeting the p300/CBP axis in lethal prostate cancertargeting the p300/CBP axis in lethal prostate cancer. Cancer Discov. 2021;11:1118–37.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Shaffer PL, Jivan A, Dollins DE, Claessens F, Gewirth DT. Structural basis of androgen receptor binding to selective androgen response elements. Proc Natl Acad Sci USA. 2004;101:4758–63.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Lavery DN, McEwan IJ. Structural characterization of the native NH2-terminal transactivation domain of the human androgen receptor: a collapsed disordered conformation underlies structural plasticity and protein-induced folding. Biochem. 2008;47:3360–9.

Article  CAS  Google Scholar 

Tsafou K, Tiwari PB, Forman-Kay JD, Metallo SJ, Toretsky JA. Targeting intrinsically disordered transcription factors: changing the paradigm. J Mol Biol. 2018;430:2321–41.

Article  CAS  PubMed  Google Scholar 

Monaghan AE, McEwan IJ. A sting in the tail: the N-terminal domain of the androgen receptor as a drug target. Asian J Androl. 2016;18:687.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Sadar MD. Discovery of drugs that directly target the intrinsically disordered region of the androgen receptor. Expert Opin Drug Discov. 2020;15:551–60.

Article  CAS  PubMed  PubMed Central  Google Scholar 

留言 (0)

沒有登入
gif