Androgen receptor agon 
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  • ||||||||||  Journal:  Toxicological investigation of lilial. (Pubmed Central) -  Oct 29, 2023   
    Neither lilial nor its metabolites showed mutagenic activity in the HPRT gene mutation test in CHO-K1 cells, nor were they able to cause double-strand breaks in DNA (?H2AX biomarker) in CHO-K1 and HeLa cells. In our study, no negative effects of lilial or its in vitro metabolites were observed up to 100
  • ||||||||||  enzalutamide capsule / Generic mfg.
    Journal:  Androgen receptor agonist and antagonist reduce response of cytokine-induced killer cells on prostate cancer cells. (Pubmed Central) -  Aug 28, 2023   
    Interestingly, pretreating LNCaP and C4-2 cells with either androgen or the androgen receptor (AR) antagonist enzalutamide mediates resistance to this immunogenic attack...The obtained data suggest that the conditioned media from PCa treated cells does not influence a measurable lymphocyte-mediated apoptosis. However, analysing clonal expansion of activated lymphocytes, the androgen-derived conditioned media suppresses lymphocyte proliferation/expansion suggesting inhibition of onco-immunological activity by pretreatment of PCa cells with AR ligands.
  • ||||||||||  vosilasarm (EP0062) / Ellipses Pharma
    Harm From SARMs: RAD-140, A Selective Androgen Receptor Modulator Leading to Acute Liver Injury (Exhibit Hall) -  Jul 29, 2023 - Abstract #ACG2023ACG_1597;    
    Despite the FDA warning against SARM use in body-building products, SARM abuse is a rising problem among athletes. Clinicians should strongly recommend against recreational SARM use and educate patients about the negative effects of these unregulated substances.
  • ||||||||||  Journal:  In Silico Evaluation of the Binding Energies of Androgen Receptor Agonists in Wild-Type and Mutational Models. (Pubmed Central) -  Jun 9, 2023   
    Our results also show the differences and equivalences between the different agonists, in addition to evaluating the difference between the DHT ligand in complex with the wild-type and mutant receptor, presenting the main amino acid residues that involve the interaction with the ligands. The computational methodology used proves to be an operative and sophisticated choice to help in the search for pharmacological agents for various therapies that have androgen as a target.
  • ||||||||||  Contribution of 11-Ketotestosterone and 11-Ketodihydrotestosterone to Castration-Resistant Prostate Cancer (ENDOExpo) -  May 11, 2023 - Abstract #ENDO2023ENDO_1521;    
    Two potent and highly efficacious androgen-receptor agonists of adrenal origin, 11-ketotestosterone and 11-ketodihydrotestosterone, are predominant androgens after castration and play an important role in the development and progression of castration-resistant prostate cancer. Their measurement in blood can be of clinical value during androgen-deprivation therapy.
  • ||||||||||  abiraterone acetate / Generic mfg.
    Mineralocorticoid Excess Syndrome with Abiraterone (ENDOExpo) -  May 11, 2023 - Abstract #ENDO2023ENDO_850;    
    There is minimal literature on abiraterone induced endocrine side effects. This case will increase awareness of these and help endocrinologists individualize management of adverse effects experienced by prostate cancer patients on abiraterone.
  • ||||||||||  Journal:  High-throughput AR dimerization assay identifies androgen disrupting chemicals and metabolites. (Pubmed Central) -  Apr 21, 2023   
    The subsequent reevaluation of the 128 chemicals tested in the presence of individual human CYP enzymes changed the activity calls for five compounds and shifted the estimated potencies for several others. This study shows the AR2 assay is well suited to replace the previous AR dimerization assays in a revised computational model to predict AR bioactivity for parent chemicals and their metabolites.
  • ||||||||||  Review, Journal:  Selective Androgen Receptor Modulators: An Emerging Liver Toxin. (Pubmed Central) -  Dec 9, 2022   
    No clear treatment exists, although patients typically show improvement with cessation of the offending SARM. Given the novelty of these drugs, further study is necessary to understand diagnosis, management, and complications of SARM-related DILI.
  • ||||||||||  Journal:  Structure-Based Study to Overcome Cross-Reactivity of Novel Androgen Receptor Inhibitors. (Pubmed Central) -  Oct 1, 2022   
    Computational modelling revealed that helix 12 of AR undergoes a characteristic shift upon VPC14368 binding causing the agonistic behaviour. Based on the obtained structural data we then designed derivatives of VPC14368 to successfully eliminate the cross-reactivity towards the AR ABS, while maintaining significant anti-AR DBD potency.
  • ||||||||||  The Androgen Receptor as a Therapeutic Target in Breast Cancer () -  Jan 7, 2022 - Abstract #LCC2022LCC_6;    
    The next challenge is to resolve the role of androgen receptors in different sub-groups of estrogen receptor negative breast cancer (e.g. HER2+, TNBC) to advance a rational basis for use of androgen receptor agonists or antagonists. Preliminary data suggests that in some contexts, the androgen receptor sustains a tumour suppressive role in estrogen receptor negative breast cancer.
  • ||||||||||  Clinical, Journal:  Sex hormones regulate lipid metabolism in adult Sertoli cells: a genome-wide study of estrogen and androgen receptor binding sites. (Pubmed Central) -  Sep 1, 2021   
    Moreover, transcript levels of enzymes involved in the lipid metabolic pathways were significantly altered in cultured Sertoli cells treated with estrogen and androgen receptor agonists, demonstrating functional significance of these binding sites. This study elucidates a mechanism by which sex hormones regulate lipid metabolism in Sertoli cells by transcriptionally controlling the expression of these genes, thereby shedding light on the roles of these hormones in male fertility.
  • ||||||||||  Xtandi (enzalutamide) / Pfizer, Astellas, Bausch Health
    Journal:  Predicting the activation of the androgen receptor by mixtures of ligands using Generalized Concentration Addition. (Pubmed Central) -  Jul 22, 2021   
    We generated individual dose-response data for full (dihydroxytestosterone, BMS564929) and partial (TFM-4AS-1) agonists and a competitive antagonist (MDV3100) using reporter data generated in the MDA-kb2 cell line...The generalized concentration addition model fit the empirical mixtures data-full/full agonist, full/partial agonist and full agonist/antagonist-as well or better than relative potency factors or effect summation. The ability of generalized concentration addition to predict the activity of mixtures of different types of androgen receptor ligands is important as a number of environmental compounds act as partial androgen receptor agonists or antagonists.
  • ||||||||||  Journal:  Proposal of novel potent inhibitors against androgen receptor based on ab initio molecular orbital calculations. (Pubmed Central) -  Jun 22, 2021   
    We here propose novel ligands as potent inhibitors against AR and investigate their binding properties to AR, using the same molecular simulations. The results indicate that the most promising ligand binds stronger to AR than the existing non-steroidal ligands, and that our proposed ligand binds strongly to a mutant-type AR, which has drug resistance to the existing non-steroidal ligands.
  • ||||||||||  Journal:  Androgen receptor agonists as breast cancer therapeutics. (Pubmed Central) -  Feb 20, 2021   
    The results indicate that the most promising ligand binds stronger to AR than the existing non-steroidal ligands, and that our proposed ligand binds strongly to a mutant-type AR, which has drug resistance to the existing non-steroidal ligands. No abstract available
  • ||||||||||  flutamide / Generic mfg.
    Journal:  Identification of (anti-)androgenic activities and risks of sludges from industrial and domestic wastewater treatment plants. (Pubmed Central) -  Dec 20, 2020   
    Twelve of the 18 samples exhibited androgen receptor (AR) antagonistic activities, with AR antagonistic equivalents ranging from 1.2 × 10 μg flutamide/g sludge to 1.8 × 10 μg flutamide/g sludge; however, no AR agonistic activity was detected in any of the tested samples...The HI values of all the 12 sludges exceeded 1.0, and the highest HI value was above 3.0 × 10 for children; this indicates that these sludges might cause adverse effects to human health and that children are at a greater risk than adults. The anti-androgenic potencies and risks of the subdivided fractions were also determined, and medium-polar and polar fractions were found to have relatively high detection rates and contribution rates to the AR antagonistic potencies and risks of the raw sample extracts.
  • ||||||||||  relacorilant (CORT125134) / Corcept Therap
    [VIRTUAL] Discovery of potent and selective non-steroidal glucocorticoid receptor antagonists (On Demand Poster) -  Aug 20, 2020 - Abstract #ACSFall2020ACS-Fall_5406;    
    Optimization of a series from the starting point of a non-steroid antagonist, Relacorilant, led to the discovery of OP-4954, a potent, orally bioavailable, and selective non-steroidal GR antagonist with minimal progesterone receptor antagonism and androgen receptor agonism. In addition, the compound has demonstrated substantial inhibition of GR transcriptional activity in GR-positive TNBC xenograft models.
  • ||||||||||  Journal:  Senolytic compounds control a distinct fate of androgen receptor agonist- and antagonist-induced cellular senescent LNCaP prostate cancer cells. (Pubmed Central) -  May 1, 2020   
    Subsequently, cells were incubated with the HSP90 inhibitor Ganetespib (GT), the Bcl-2 family inhibitor ABT263, or the Akt inhibitor MK2206 to analyze senolysis...These data indicate a difference in the agonist- or antagonist-induced cellular senescence and suggest a novel role of MK2206 as a senolytic agent preferentially for AR antagonist-treated cells. Taken together, our data suggest that both AR agonist and antagonist induce cellular senescence but differentially upregulate a pro-survival signaling which preferentially sensitize androgen-sensitive PCa LNCaP cells to a specific senolytic compound.
  • ||||||||||  Ostarine (enobosarm) / Oncternal Therapeutics
    Journal:  Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs. (Pubmed Central) -  Apr 15, 2020   
    Ostarine is the selective androgen receptor modulators (SARMs) containing a CF group in clinical trial III...Some SF-derivatives showed androgen receptor (AR) agonistic activities in vitro. The results pointed to the potential of using this scaffold to develop new AR agonists.
  • ||||||||||  Zytiga (abiraterone acetate) / J&J, spironolactone / Generic mfg.
    Journal:  Abiraterone and spironolactone in prostate cancer: a combination to avoid. (Pubmed Central) -  Mar 29, 2020   
    This is supported by the observations described in this case report. Therefore, spironolactone should be avoided in prostate cancer patients suffering from treatment-associated side effects of abiraterone.
  • ||||||||||  Clinical, Journal:  Cancer cachexia, a clinical challenge. (Pubmed Central) -  Mar 20, 2020   
    Therefore, spironolactone should be avoided in prostate cancer patients suffering from treatment-associated side effects of abiraterone. Cancer cachexia has two main components: anorexia and metabolic alterations and both have to be taken into consideration for the treatment of the syndrome.
  • ||||||||||  Discovery of potent and selective non-steroidal glucocorticoid receptor antagonists (Exhibit Hall D, Pennsylvania Convention Center) -  Feb 13, 2020 - Abstract #ACSSp2020ACS_Sp_4016;    
    Optimization of a series from the starting point of a pyrazolodecalin led to the discovery of OP-4954, a potent, orally bioavailable, and selective non-steroidal GR antagonist with minimal progesterone receptor antagonism and androgen receptor agonism. In addition, the compound has demonstrated substantial inhibition of GR transcriptional activity in GR-positive TNBC xenograft models.
  • ||||||||||  Zytiga (abiraterone acetate) / J&J
    Abiraterone Acetate: Enough of the S.A.M.E. Old Steroids (Exhibit Hall, Walter E. Washington Convention Center) -  Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_1512;    
    Case Description A 82-year-old male, with a past medical history of metastatic prostate cancer on treatment with leuprolide, abiraterone, and prednisone, presented with progressive weakness and falls. Abiraterone is an effective steroidal inhibitor for castrate-resistant prostate cancer, but can lead to the SAME, which clinicians should be able to recognize and treat.
  • ||||||||||  Biomarker, Journal:  Ca-activated K channels as cancer therapeutic targets (Pubmed Central) -  Sep 23, 2019   
    We determined K3.1 activators are a possible therapeutic option to suppress the tumor-promoting activities of IL-10. These results may provide new insights into cancer treatment focused on Ca-activated K channels.