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    BIOMARKER:

    AR overexpression

    i
    Other names: AR, AIS, DHTR, HUMARA, NR3C4, SBMA, SMAX1, Androgen receptor
    Entrez ID:
    367
    Related biomarkers:
    Expression
    Mutation
    CNA
    Others
    11d
    The Decreased Proliferation Capacity of Cardiomyocytes Induced By Androsterone Is Mediated By the Interactions Between Androgen Receptor and Retinoblastoma Protein. (PubMed, J Biochem Mol Toxicol)
    The repression of cell proliferation in response to androsterone was alleviated partly through the downregulation of Rb by siRNA transfection. In conclusion, AR repression to cell cycle and DNA replication-related gene expression, mediated by recruitment of Rb, may be one of the potential mechanisms of cell cycle arrest in cardiomyocytes induced by androsterone.
    Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression
    21d
    MYO6 contributes to tumor progression and enzalutamide resistance in castration-resistant prostate cancer by activating the focal adhesion signaling pathway. (PubMed, Cell Commun Signal)
    MYO6 has pro-tumor and Enz-resistant effects in CRPC, suggesting that targeting MYO6 may be beneficial for ENZ-resistant CRPC therapy through the AR/MYO6/FAK signaling pathway.
    Journal
    |
    AR (Androgen receptor) • MYO6 (Myosin VI)
    |
    AR overexpression • AR expression
    |
    Xtandi (enzalutamide capsule)
    1m
    Social isolation promotes tumor immune evasion via β2-adrenergic receptor. (PubMed, Brain Behav Immun)
    Pharmacological inhibition of β2-AR signaling effectively enhanced CD8+ T cell anti-tumor immune responses and improved the efficacy of anti-PD-1 immunotherapy in the context of social isolation. Thus, our study uncovers a mechanism through which social isolation induces tumor immune evasion and offers potential directions for cancer immunotherapy in socially isolated patients.
    Journal
    |
    CD8 (cluster of differentiation 8)
    |
    AR overexpression
    1m
    Systemic treatments in recurrent or metastatic salivary gland cancer: a systematic review. (PubMed, ESMO Open)
    Systemic treatments contribute to the survival of patients with salivary gland cancer at relapsed or newly advanced stages. The response to treatment is heavily influenced by histological subtype and treatment specificity.
    Review • Journal • Metastases
    |
    AR (Androgen receptor)
    |
    HER-2 overexpression • AR overexpression • AR expression • KIT expression
    |
    Herceptin (trastuzumab) • bicalutamide
    1m
    Retrospective study assessing the role of the androgen receptor in clear cell renal cell cancer patients treated with VEGFR inhibitors in monotherapy. (PubMed, Clin Transl Oncol)
    AR-overexpression and its association with other genes could favor a transcriptomic signature set to aid in identifying patients suitable for TKI in monotherapy, rather than aggressive combinations, enhancing thus, precision and personalized therapeutic decisions.
    Retrospective data • Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression • AR expression
    2ms
    FOXM1 Transcriptionally Co-Upregulates Centrosome Amplification and Clustering Genes and Is a Biomarker for Poor Prognosis in Androgen Receptor-Low Triple-Negative Breast Cancer. (PubMed, Cancers (Basel))
    Targeting FOXM1 in AR-low TNBC may render cancer cells incapable of clustering their centrosomes and impair their ability to generate excess centrosomes. Hence, our review illuminates FOXM1 as a potential actionable target for AR-low TNBC.
    Review • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • PGR (Progesterone receptor) • AR (Androgen receptor) • BIRC5 (Baculoviral IAP repeat containing 5) • AURKB (Aurora Kinase B) • FOXM1 (Forkhead Box M1) • KIFC1 (Kinesin Family Member C1) • ATAD2 (ATPase Family AAA Domain Containing 2) • CDCA8 (Cell Division Cycle Associated 8) • E2F1 (E2F transcription factor 1)
    |
    AR overexpression
    2ms
    The prognostic significance of androgen receptor expression in gliomas. (PubMed, Sci Rep)
    Higher AR expression levels are associated with higher grade disease and histopathologic features predicting poorer prognosis in lower grade gliomas. Higher gene expression in LGG patients is correlated with poor prognosis but not in the glioblastoma cohort suggesting saturated expression/functions of AR in glioblastoma.
    Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression • AR expression • AR underexpression
    2ms
    Azolato-Bridged Dinuclear Platinum(II) Complexes Exhibit Androgen Receptor-Mediated Anti-Prostate Cancer Activity. (PubMed, Inorg Chem)
    Several of the complexes, particularly 5-H-Y ([{cis-Pt(NH3)2}2(μ-OH)(μ-tetrazolato-N2,N3)](ClO4)2), effectively inhibited LNCaP cell growth, even at low concentrations, by direct modulation of AR signaling, and by binding to DNA and inducing apoptosis, which is a common mechanism of action of Pt-based drugs such as cisplatin (cis-diamminedichloridoplatinum(II))...Further investigation revealed that 5-H-Y suppressed mRNA expression of genes downstream from AR and induced apoptosis, particularly in cells overexpressing AR, highlighting its potential as an AR antagonist. Thus, we provide here insights into the mechanisms underlying the antiproliferative effects of azolato-bridged complexes in prostate cancer.
    Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression
    |
    cisplatin
    7ms
    Enzalutamide induces cytotoxicity in desmoplastic small round cell tumor independent of the androgen receptor. (PubMed, Commun Biol)
    Here, we demonstrate that AR is highly expressed in DSRCT relative to other fusion-driven sarcomas and that the AR antagonists enzalutamide and flutamide reduce DSRCT growth. Further, we find that AR antagonists reduce DSRCT growth in cells depleted of AR, establishing an AR-independent mechanism of action. These findings suggest that AR dependence is not the reason for male predominance in DSRCT and that AR-targeted therapies may provide therapeutic benefit primarily through an AR-independent mechanism that requires further elucidation.
    Journal
    |
    AR (Androgen receptor) • WT1 (WT1 Transcription Factor) • EWSR1 (EWS RNA Binding Protein 1)
    |
    AR overexpression
    |
    Xtandi (enzalutamide capsule) • flutamide
    8ms
    Caffeic acid phenethyl ester suppresses the expression of androgen receptor variant 7 via inhibition of CDK1 and AKT. (PubMed, Cancer Gene Ther)
    Intraperitoneal injection of 10 mg/kg CAPE retarded the growth of 22Rv1 xenografts in nude mice and suppressed the protein levels of AR-V7, CDK1 and AKT in 22Rv1 xenografts. Our study provided the rationale of applying CAPE for inhibition of AR-V7 in prostate tumors.
    Journal
    |
    AR (Androgen receptor) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CDK1 (Cyclin-dependent kinase 1)
    |
    AR overexpression • AR expression • AR splice variant 7 • AR-V7 expression • AKT1 overexpression • AR-V7 overexpression • AR splice variant 7 expression • CDK1 overexpression
    9ms
    NCI-2018-01054: Apalutamide, Abiraterone Acetate, and Prednisone in Treating Participants With Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=7, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Apr 2024 --> Apr 2025 | Trial primary completion date: Apr 2024 --> Apr 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    PTEN (Phosphatase and tensin homolog)
    |
    AR overexpression • AR expression • AR-V7 expression
    |
    abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
    10ms
    Therapeutic Potential of Bipolar Androgen Therapy for Castration-Resistant Prostate Cancer: In Vitro and In Vivo Studies. (PubMed, Biomedicines)
    Bicalutamide inhibited PCa cell viability but not in the adapted cell lines...In vivo, high AR-expressing LNCaP cells proliferated under castrate conditions, while BAT-treated xenografts exhibited significant growth inhibition with low Ki-67 and mitotic indexes and a high cell death index. This study provides preliminary evidence that BAT is effective for the treatment of CRPC through rapid cycling between supraphysiologic and near-castrate serum testosterone levels, inducing an anti-tumor effect.
    Preclinical • Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression • AR expression • AR splice variant 7 • AR-V7 expression • AR splice variant 7 expression
    |
    bicalutamide
    10ms
    Discovery of the First-in-Class RORγ Covalent Inhibitors for Treatment of Castration-Resistant Prostate Cancer. (PubMed, J Med Chem)
    Importantly, it markedly suppressed the tumor growth in a 22Rv1 mouse tumor xenograft model with good safety. These results clearly demonstrate that 29 is a highly potent and selective RORγ covalent inhibitor.
    Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression • AR expression
    1year
    Androgen receptor promotes cell stemness via interacting with co-factor YAP1 in gastric cancer. (PubMed, Biochem Pharmacol)
    Mechanically, AR upregulated CD44 expression by directly binding to its promoter region and Yes-associated protein 1 (YAP1) served as the co-factor of AR, which was demonstrated by the fact that the promoting effects of AR on GC cells stemness were partially counteracted by YAP1 knockdown. Thus, this study revealed that AR facilitates CSCs properties and chemoresistance of GC cells via forming complex with YAP1and indicates a potential therapeutic approach to GC patients.
    Journal
    |
    AR (Androgen receptor) • YAP1 (Yes associated protein 1) • CD44 (CD44 Molecule)
    |
    AR positive • AR overexpression • AR expression • CD44 expression
    1year
    AR eGFP reporter mouse enables elucidation of AR expression dynamics during anti-tumor immune responses. (PubMed, Nat Commun)
    In response to PD-L1 blockade, the emergence of PD-1AR cells correlates with successful therapeutic responses, whilst IL-18 is identified as a cytokine that potently upregulates AR and synergizes with AR deficiency to improve anti-tumor immunity. These studies provide insight into the biology of AR in the context of anti-tumor immunity and reveals potential combination immunotherapy approaches.
    Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • IL18 (Interleukin 18) • CD86 (CD86 Molecule)
    |
    AR overexpression • AR expression
    1year
    Jiawei Danxuan Koukang Alleviates Arecoline Induced Oral Mucosal Lesions: Network Pharmacology and the Combined Ultra-High Performance Liquid Chromatography (UPLC) and Mass Spectrometry (MS). (PubMed, Drug Des Devel Ther)
    Quercetin targeted AR protein to improve arecoline-induced OSF. JDK and quercetin inhibited arecoline-induced NOTCH1 protein expression in CAL27 and SCC-25 cells to play an anti-oral cancer role.
    Journal
    |
    NOTCH1 (Notch 1) • CDH1 (Cadherin 1) • VIM (Vimentin)
    |
    AR overexpression • AR expression • CDH1 expression • NOTCH1 expression • VIM expression
    1year
    NCI-2018-01054: Apalutamide, Abiraterone Acetate, and Prednisone in Treating Participants With Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=7, Active, not recruiting, M.D. Anderson Cancer Center | Suspended --> Active, not recruiting | N=60 --> 7
    Enrollment closed • Enrollment change • Metastases
    |
    PTEN (Phosphatase and tensin homolog)
    |
    AR overexpression • AR expression • AR-V7 expression
    |
    abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
    1year
    TARGETING ANDROGEN RECEPTOR IN OSTEOSARCOMA CELLS WITH VARYING METASTATIC POTENTIAL (CTOS 2023)
    The presence of LM remains the most important clinical determinant of OS prognosis, nevertheless few treatment options are available for these patients. Recent studies suggest that upregulation of the AR pathway in human LM tissue samples may provide a therapeutic target for patients with LM resistant to conventional chemotherapy. Similar to what has been observed in prostate cancer, AR overexpression may result in aberrant ALDH1A1 expression in OS patients presenting with LM.
    Metastases
    |
    AR (Androgen receptor) • ALDH1A1 (Aldehyde Dehydrogenase 1 Family Member A1)
    |
    AR overexpression
    |
    Xtandi (enzalutamide capsule)
    over1year
    Functional implications and therapeutic targeting of androgen response elements in prostate cancer. (PubMed, Biochimie)
    Importantly, in castration resistant prostate cancer, ARVs lacking the LBD become constitutively active and promote hormone-independent development, underlining the need to concentrate on the other domain or the AR-DNA interface for the identification of novel actionable targets. In this review, we highlight the plasticity of AR-DNA binding and explain how fine-tuning AR's cooperative interactions with DNA translate into developing an alternative strategy to antagonize AR activity.
    Review • Journal
    |
    AR mutation • AR overexpression • AR amplification
    over1year
    Targeted treatment in a case series of AR+, HRAS/PIK3CA co-mutated salivary duct carcinoma. (PubMed, Front Oncol)
    One patient each was treated with immune checkpoint inhibition (Mixed Response) and combination therapies of tipifarnib and ADT (SD) and alpelisib and ADT (PR). Combination therapies, PI3K-inhibitors and immune therapy warrant further investigation, ideally in clinical trials. Future research should consider this rare subgroup of SDC.
    Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • TMB (Tumor Mutational Burden) • AR (Androgen receptor) • HRAS (Harvey rat sarcoma viral oncogene homolog)
    |
    PD-L1 expression • PIK3CA mutation • HRAS mutation • AR overexpression • AR expression • PIK3CA expression • HRAS overexpression • PIK3CA overexpression
    |
    Piqray (alpelisib) • Zarnestra (tipifarnib)
    over1year
    Bipolar Androgen Therapy Followed by Androgen Receptor Inhibition as Sequential Therapy for Prostate Cancer. (PubMed, Oncologist)
    As expected, resistance to BAT is associated with adaptive downregulation of AR expression. Intriguingly, this downregulation is associated with restoration of sensitivity to subsequent AR inhibitor therapies.
    Journal
    |
    AR overexpression • AR expression
    over1year
    Clinical impact of androgen receptor-suppressing miR-146b expression in papillary thyroid cancer aggressiveness. (PubMed, J Clin Endocrinol Metab)
    To sum up, miR-146b is a molecular target of AR transcriptional repression, therefore, AR suppresses miR-146b expression to reduce PTC tumor aggressiveness.
    Journal
    |
    AR (Androgen receptor) • MIR146B (MicroRNA 146b)
    |
    AR overexpression • AR expression
    over1year
    Lead Optimization of Androgen Receptor-HSP27 Disrupting Agents in Glioblastoma. (PubMed, J Med Chem)
    Lead optimization resulted with two new derivatives (compounds 4 and 26) showing potent anti-GBM activity and improved drug distribution in comparison to the lead compound. Compounds 4 and 6 exhibit ICs of 35 and 23 nM, respectively, to inhibit cell proliferation and also show significant activity to decrease the tumor growth in vivo.
    Journal
    |
    AR (Androgen receptor) • HSPB1 (Heat shock 27kDa protein 1)
    |
    AR overexpression
    over1year
    Darolutamide for patients with androgen receptor positive salivary gland cancers (DISCOVARY): The results of phase 2 study of darolutamide monotherapy. (ASCO 2023)
    The study consists of two sequential components: a monotherapy part with darolutamide alone (monotherapy part) and a combination part with darolutamide and goserelin (combination part). This is the first prospective trial of darolutamide for AR-positive SGC. The response rate by ICR and other secondary endpoints confirmed clinically meaningful activity and a well-tolerated safety profile. Patient enrollment to the combination component is now ongoing to evaluate additional benefits.
    Clinical • P2 data
    |
    AR (Androgen receptor)
    |
    AR positive • AR overexpression • AR expression
    |
    Nubeqa (darolutamide) • goserelin acetate
    over1year
    Comprehensive characterization of androgen receptor expression in breast cancer. (ASCO 2023)
    Our data suggest a strong association between AR expression and increased mutations in several cancer related genes, immune checkpoint markers, the IL2-STAT5 pathway, differential immune cell infiltration, and improved overall survival.
    Tumor mutational burden • PD(L)-1 Biomarker • MSi-H Biomarker • IO biomarker
    |
    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • PTEN (Phosphatase and tensin homolog) • AR (Androgen receptor) • ARID1A (AT-rich interaction domain 1A) • NF1 (Neurofibromin 1) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • LAG3 (Lymphocyte Activating 3) • CDH1 (Cadherin 1) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • PD-L2 (Programmed Cell Death 1 Ligand 2) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • CXCL9 (Chemokine (C-X-C motif) ligand 9) • IL2 (Interleukin 2) • IL10 (Interleukin 10) • CCL2 (Chemokine (C-C motif) ligand 2) • MAP3K1 (Mitogen-Activated Protein Kinase Kinase Kinase 1) • FOXP3 (Forkhead Box P3) • ARG1 (Arginase 1) • CXCR1 (Chemokine (C-X-C motif) receptor 1) • GATA3 (GATA binding protein 3)
    |
    MSI-H/dMMR • HER-2 negative • PTEN mutation • AR overexpression • LAG3 expression • AR expression • FOXP3 expression
    |
    MI Tumor Seek™
    |
    Herceptin (trastuzumab) • paclitaxel • doxorubicin hydrochloride
    over1year
    Androgen receptor transcriptionally inhibits programmed death ligand-1 (PD-L1) expression and influences immune escape in bladder cancer. (PubMed, Lab Invest)
    Injection of anti-PD-L1 monoclonal antibodies into C3H/HeN mice significantly suppressed tumor growth, and stable expression of AR dramatically enhanced the antitumor activity in vivo. In conclusion, this study describes a novel role of AR in regulating the immune response to BCa by targeting PD-L1, thus providing potential therapeutic strategies for immunotherapy in BCa.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    AR (Androgen receptor) • CD8 (cluster of differentiation 8)
    |
    PD-L1 expression • PD-L1 negative • AR overexpression • AR expression • AR negative
    over1year
    SMAD3 promotes expression and activity of the androgen receptor in prostate cancer. (PubMed, Nucleic Acids Res)
    A SMAD3 PROTAC inhibitor reduced levels of AR, AR-V7 and AR targets in prostate cancer cells. This study suggests that SMAD3 could be targeted to inhibit AR in prostate cancer.
    Journal
    |
    AR (Androgen receptor) • SMAD4 (SMAD family member 4) • SMAD2 (SMAD Family Member 2) • SMAD3 (SMAD Family Member 3)
    |
    AR overexpression • AR expression • AR splice variant 7
    over1year
    A molecular guide to systemic therapy in salivary gland carcinoma. (PubMed, Head Neck)
    In the last decade, a number of targetable molecular alterations have been identified in SGCs including HER2 upregulation, androgen receptor overexpression, Notch receptor activation, NTRK gene fusions, and RET alterations which have dramatically improved treatment outcomes in this disease. Here, we review the landscape of precision therapy in SGC including current options for systemic management, ongoing clinical trials, and promising future directions.
    Review • Journal • IO biomarker
    |
    HER-2 (Human epidermal growth factor receptor 2) • AR (Androgen receptor) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    HER-2 overexpression • AR overexpression • AR expression • NTRK fusion
    over1year
    Artesunate increases enzalutamide efficacy in advanced prostate cancer (AACR 2023)
    Taking these together suggests that ART may target HSF1 directly. Our results suggest ART induced AR degradation could be a promising clinical strategy for advanced prostate cancer.
    Clinical • Metastases
    |
    HSF1 (Heat Shock Transcription Factor 1) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
    |
    AR mutation • AR overexpression
    |
    Xtandi (enzalutamide capsule)
    over1year
    EZH2 mediated kinome reprogramming drives AR phosphorylation and activation in receptor tyrosine kinase inhibitors resistant renal carcinoma models (AACR 2023)
    Our previous studies of acquired resistance to the RTKI sunitinib identified two major regulators, EZH2 and androgen receptor (AR)...Finally, our lab has generated 786-0 strains resistant to other RTKI including pazopanib and lenvatinib, and found that AR is expressed in these resistant models, solidifying AR activation as a conserved feature of RTKI resistance. Overall, our results suggest that AR activation is driven by phosphorylation induced by EZH2 dependent kinome reprogramming. Untangling the cross talk between AR and EZH2 in RTKI resistant RCC will provide the rationale for novel therapeutic strategies to improve the clinical outcome in patients with this disease.
    IO biomarker
    |
    EGFR (Epidermal growth factor receptor)
    |
    EZH2 mutation • AR overexpression
    |
    sunitinib • Lenvima (lenvatinib) • pazopanib
    over1year
    Inhibition of HSF1 demonstrates therapeutic efficacy in preclinical models of cholangiocarcinoma (AACR 2023)
    NXP800, a HSF1 inhibitor, demonstrated significant therapeutic activity in a cholangiocarcinoma PDX. Further studies are needed and being performed to determine the role of HSF1 inhibition in human cholangiocarcinoma.
    Preclinical • Tumor mutational burden
    |
    TMB (Tumor Mutational Burden) • NRAS (Neuroblastoma RAS viral oncogene homolog) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1) • AR (Androgen receptor) • ARID1A (AT-rich interaction domain 1A) • HSF1 (Heat Shock Transcription Factor 1)
    |
    NRAS mutation • ARID1A mutation • FGFR2 mutation • FGFR1 mutation • NRAS Q61 • AR overexpression • FGFR2 overexpression • AR expression • FGFR2 expression
    |
    NXP800
    over1year
    Vaccination against androgen receptor splice variant induces anti-tumor adaptive immune responses (AACR 2023)
    These data demonstrate the potential of AR and AR splice variants as immunologic targets of prostate cancer vaccines, which elicit AR specific T cell immunity and produce anti-tumor responses in prostate cancers.
    PD(L)-1 Biomarker • IO biomarker
    |
    AR (Androgen receptor)
    |
    AR overexpression • AR expression • AR splice variant 7 • AR-V7 expression • AR splice variant 7 expression
    over1year
    Predicting progression in metastatic castrate-sensitive prostate cancer by coupling PSA and testosterone dynamics to a mechanistic mathematical model (AACR 2023)
    By fitting to both PSA and testosterone dynamics, we can distinguish between tumors that maintain testosterone-dependent cells from those with increasing resistant cell types. This allows for better quantification of the underlying tumor composition to help optimize therapies that target those cell types and better maintain tumor control.
    Metastases
    |
    AR (Androgen receptor)
    |
    AR overexpression
    over1year
    NCI-2018-01054: Apalutamide, Abiraterone Acetate, and Prednisone in Treating Participants With Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=60, Suspended, M.D. Anderson Cancer Center | Trial completion date: Oct 2022 --> Apr 2024 | Trial primary completion date: Oct 2022 --> Apr 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    PTEN (Phosphatase and tensin homolog)
    |
    AR overexpression • AR expression • AR-V7 expression
    |
    abiraterone acetate • Erleada (apalutamide) • Yonsa (abiraterone acetate)
    over1year
    Anti-oncogenic effects of dutasteride, a dual 5-alpha reductase inhibitor and a drug for benign prostate hyperplasia, in bladder cancer. (PubMed, J Transl Med)
    Dutasteride inhibited testosterone-induced BCa progression dependent on SLC39A9 in AR-negative BCa and repressed oncogenic signaling pathways, including those of metalloproteases, p21, BCL-2, NF-KB, and WNT. Our results also suggest that SRD5A1 plays a pro-oncogenic role in BCa. This work provides potential therapeutic targets for the treatment of BCa.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • AR (Androgen receptor) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • SRD5A1 (Steroid 5 Alpha-Reductase 1)
    |
    AR overexpression • AR expression • AR negative
    almost2years
    HER2 status in recurrent/metastatic androgen receptor overexpressing salivary gland carcinoma patients. (PubMed, Front Oncol)
    In our patient population, HER2 amplification was a negative prognostic factor, and it was associated with a non-statistically significant higher risk of developing CNS metastasis. Further studies are needed to explore the potential clinical benefit of tackling the two biological pathways (AR and HER2) in patients affected by this rare and aggressive malignancy.
    Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • AR (Androgen receptor)
    |
    HER-2 overexpression • HER-2 amplification • HER-2 negative • AR positive • AR overexpression • AR expression
    almost2years
    An Exemestane Derivative, Oxymestane-D1, as a New Multi-Target Steroidal Aromatase Inhibitor for Estrogen Receptor-Positive (ER) Breast Cancer: Effects on Sensitive and Resistant Cell Lines. (PubMed, Molecules)
    Thus, the multi-target action of Oxy may be a therapeutic advantage over the three AIs applied in clinic. Furthermore, this new multi-target compound has the ability to sensitize the AI-resistant BC cells, which represents another advantage over the endocrine therapy used in the clinic, since resistance is a major drawback in the clinic.
    Preclinical • Journal
    |
    ER (Estrogen receptor)
    |
    ER positive • AR overexpression
    |
    exemestane
    almost2years
    Increased AR expression in castration-resistant prostate cancer rapidly induces AR signaling reprogramming with the collaboration of EZH2. (PubMed, Front Oncol)
    Mechanistically, we found that AR-EZH2 interaction is impaired by the pre-castration level of androgens but can be recovered by the post-castration level of androgens. Overall, our study provides new molecular insights into AR signaling reprogramming with the engagement of specific epigenetic factors.
    Journal
    |
    CAST (Calpastatin)
    |
    AR overexpression • AR expression