androgen receptor antagonists


Summary: Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.

Top Publications

  1. Masoodi K, Eisermann K, Yang Z, Dar J, Pascal L, Nguyen M, et al. Inhibition of Androgen Receptor Function and Level in Castration-Resistant Prostate Cancer Cells by 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone. Endocrinology. 2017;158:3152-3161 pubmed publisher
    ..These findings suggest that IMTPPE is a potential lead compound for developing clinical candidates for the treatment of CRPC, including those resistant to enzalutamide. ..
  2. Aragon Ching J. Is there an optimal treatment sequencing strategy for metastatic castration-resistant prostate cancer?. Future Oncol. 2013;9:619-22 pubmed publisher
  3. Lundqvist J, Tringali C, Oskarsson A. Resveratrol, piceatannol and analogs inhibit activation of both wild-type and T877A mutant androgen receptor. J Steroid Biochem Mol Biol. 2017;174:161-168 pubmed publisher
    ..We conclude that the resveratrol, piceatannol and analogs are highly interesting for chemoprevention of prostate cancer, since they have a high potency both as inhibitors of androgen synthesis and androgen receptor activation. ..
  4. Lao K, Sun J, Wang C, Wang Y, You Q, Xiao H, et al. Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5?-androst-17?-amide derivatives as dual 5?-reductase inhibitors and androgen receptor antagonists. Bioorg Med Chem Lett. 2017;27:4212-4217 pubmed publisher
    ..Overall, based on biological activities data, compound 11d and 11k can be identified as potential dual 5?-reductase inhibitors and AR antagonists which might be of therapeutic importance for prostate cancer treatment. ..
  5. Argiles J, López Soriano F, Stemmler B, Busquets S. Novel targeted therapies for cancer cachexia. Biochem J. 2017;474:2663-2678 pubmed publisher
    ..Indeed, timing is crucial and has to be taken very seriously when applying the therapeutic approach. ..
  6. Wang Y, Han R, Zhang H, Liu H, Li J, Liu H, et al. Combined Ligand/Structure-Based Virtual Screening and Molecular Dynamics Simulations of Steroidal Androgen Receptor Antagonists. Biomed Res Int. 2017;2017:3572394 pubmed publisher
  7. Gunther J, Parent A, Katzenellenbogen J. Alternative inhibition of androgen receptor signaling: peptidomimetic pyrimidines as direct androgen receptor/coactivator disruptors. ACS Chem Biol. 2009;4:435-40 pubmed publisher
    ..Unlike the activity of traditional androgen receptor antagonists, such as flutamide and bicalutamide, inhibition by these coactivator binding inhibitors is ..
  8. Barton V, Christenson J, Gordon M, Greene L, Rogers T, Butterfield K, et al. Androgen Receptor Supports an Anchorage-Independent, Cancer Stem Cell-like Population in Triple-Negative Breast Cancer. Cancer Res. 2017;77:3455-3466 pubmed publisher
    ..i>Cancer Res; 77(13); 3455-66. ©2017 AACR. ..
  9. Laird M, Thomson K, Fenwick M, Mora J, Franks S, Hardy K. Androgen Stimulates Growth of Mouse Preantral Follicles In Vitro: Interaction With Follicle-Stimulating Hormone and With Growth Factors of the TGFβ Superfamily. Endocrinology. 2017;158:920-935 pubmed publisher
    ..These findings provide insight into abnormal early follicle development in PCOS. ..

More Information


  1. Beer T, Tombal B. Enzalutamide in metastatic prostate cancer before chemotherapy. N Engl J Med. 2014;371:1755-6 pubmed publisher
  2. Norris J, Ellison S, Baker J, Stagg D, Wardell S, Park S, et al. Androgen receptor antagonism drives cytochrome P450 17A1 inhibitor efficacy in prostate cancer. J Clin Invest. 2017;127:2326-2338 pubmed publisher
    ..The results of this study suggest that the ability of CYP17 inhibitors to directly antagonize the AR may contribute to their clinical efficacy in CRPC. ..
  3. Lebbe M, Taylor A, Visser J, Kirkman Brown J, Woodruff T, Arlt W. The Steroid Metabolome in the Isolated Ovarian Follicle and Its Response to Androgen Exposure and Antagonism. Endocrinology. 2017;158:1474-1485 pubmed publisher
  4. Graff J, Beer T. Reducing Skeletal-Related Events in Metastatic Castration-Resistant Prostate Cancer. Oncology (Williston Park). 2015;29:416-23 pubmed
    ..Finally, we review the available data regarding the cost of denosumab compared with that of zoledronic acid. ..
  5. Divakar S, Saravanan K, Karthikeyan P, Elancheran R, Kabilan S, Balasubramanian K, et al. Iminoenamine based novel androgen receptor antagonist exhibited anti-prostate cancer activity in androgen independent prostate cancer cells through inhibition of AKT pathway. Chem Biol Interact. 2017;275:22-34 pubmed publisher
    ..The ARA3 induces the apoptosis in AIPC cells by preventing the AR mediated activation of AKT pathway. The bicalutamide did not induce the apoptosis because it failed to prevent the AR mediated activation of AKT. ..
  6. Abedinpour P, BARON V, Chrastina A, Rondeau G, Pelayo J, Welsh J, et al. Plumbagin improves the efficacy of androgen deprivation therapy in prostate cancer: A pre-clinical study. Prostate. 2017;77:1550-1562 pubmed publisher
    ..This study evaluates the effectiveness of treatment with combinations of plumbagin and alternative strategies for ADT in mouse models of prostate cancer to support its clinical use...
  7. Mohler M, Bohl C, Jones A, Coss C, Narayanan R, He Y, et al. Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem. 2009;52:3597-617 pubmed publisher
  8. Wang Z, Wang C, Wu Z, Xue J, Shen B, Zuo W, et al. Artesunate Suppresses the Growth of Prostatic Cancer Cells through Inhibiting Androgen Receptor. Biol Pharm Bull. 2017;40:479-485 pubmed publisher
    ..The results indicated that ART suppressed tumor growth of prostatic cancer cells through AR-DNMT3b pathway, underlying ART will allow for the utilization of this Chinese therapeutic agent for the potential treatment of prostate cancer. ..
  9. Shore N. Darolutamide (ODM-201) for the treatment of prostate cancer. Expert Opin Pharmacother. 2017;18:945-952 pubmed publisher
    ..These features may offer potential advantages over the second-generation antiandrogens. In the phase I/II ARADES trial, darolutamide demonstrated promising antitumor activity and a favorable safety profile in men with metastatic CRPC. ..
  10. Harmon S, Perk T, Lin C, Eickhoff J, Choyke P, Dahut W, et al. Quantitative Assessment of Early [18F]Sodium Fluoride Positron Emission Tomography/Computed Tomography Response to Treatment in Men With Metastatic Prostate Cancer to Bone. J Clin Oncol. 2017;35:2829-2837 pubmed publisher
    ..Total functional burden assessed after three cycles of hormonal therapy or chemotherapy was predictive of PFS for men with mCRPC. This supports ongoing development of NaF PET/CT-based imaging biomarkers in mCRPC to bone. ..
  11. Sharifi N. Steroid receptors aplenty in prostate cancer. N Engl J Med. 2014;370:970-1 pubmed publisher
  12. Ozgür E, Celik A, Darendeliler E, Gezer U. PCA3 Silencing Sensitizes Prostate Cancer Cells to Enzalutamide-mediated Androgen Receptor Blockade. Anticancer Res. 2017;37:3631-3637 pubmed
    ..Furthermore, PCA3 silencing sensitized PCa cells to enzalutamide-induced loss of cell growth. PCA3, as a therapeutic target in PCa, might be used to potentiate AR antagonists. ..