bims-meproc Biomed News
on Metabolism in Prostate Cancer
Issue of 2025–11–16
twenty-six papers selected by
Grigor Varuzhanyan, UCLA



  1. BMC Biotechnol. 2025 Nov 10. 25(1): 123
      
    Keywords:  FOXD1; Glycolysis; Hypoxia; Prostate cancer; Tumor microenvironment
    DOI:  https://doi.org/10.1186/s12896-025-01061-6
  2. Int J Mol Sci. 2025 Oct 24. pii: 10347. [Epub ahead of print]26(21):
      Xanthohumol (XN), a naturally occurring flavonoid characterized by the presence of prenyl moieties and obtained from hop plants (Humulus lupulus L.), has garnered growing interest in the scientific community owing to its diverse biological activities, including anti-inflammatory, anticancer, and antioxidant effects. However, its antitumor mechanisms, especially the inhibitory impact and related molecular pathways in prostate cancer, are not yet fully elucidated. This study investigated the effects of XN on prostate cancer and explored its underlying molecular mechanisms. The antiproliferative effect of XN on prostate cancer cells was assessed using the sulforhodamine B assay. Cellular morphological changes were examined by microscopy. Pyroptosis induction following XN treatment was evaluated via flow cytometry and Western blot analysis. Following treatment with XN, prostate cancer cells exhibited characteristic morphological changes consistent with pyroptosis. Protein analysis revealed that XN triggers pyroptosis primarily via the caspase-3/GSDME. The attenuation of XN-induced, GSDME-dependent pyroptosis by the caspase-3-specific inhibitor Z-DEVD-fmk further supported this mechanism. Furthermore, our results indicate that XN promotes the accumulation of reactive oxygen species (ROS) and reduces mitochondrial membrane potential, thereby activating the mitochondrial intrinsic pathway and leading to cytochrome c release, which subsequently triggers caspase-3 activation and the cleavage of GSDME, and ultimately induces pyroptosis. XN induced pyroptosis in prostate cancer cells through the mitochondrial intrinsic pathway, offering novel strategic insights for the treatment of prostate cancer and the development of innovative therapeutic agents.
    Keywords:  GSDME; Xanthohumol; prostate cancer; pyroptotic
    DOI:  https://doi.org/10.3390/ijms262110347
  3. Cancers (Basel). 2025 Nov 05. pii: 3571. [Epub ahead of print]17(21):
      Background: Prostate cancer, an epithelial malignancy occurring in the prostate, is the most common malignant tumor of the male genitourinary system and has a low survival rate in advanced prostate cancer after metastasis. It is urgent to explore novel therapeutic targets and strategies for treating prostate cancer. Circular RNA (circRNA) and ferroptosis both play critical roles in prostate cancer progression. However, the regulatory effect of circRNA on ferroptosis remains unclear. Methods: Here, circRNA expression profiles in prostate cancer were explored by bioinformatics analysis and human prostate cancer tissue microarray. Stable circRNA-knockdown or overexpressed prostate cancer cell lines were constructed by lentivirus. AGO2-RNA immunoprecipitation (AGO2-RIP) was utilized to identify circRNA-microRNA (miRNA) interaction. Results: Results of this study indicate that circATP2C1 is highly expressed in prostate cancer. In addition, circATP2C1 promotes prostate cancer cell proliferation, migration, and invasion by suppressing ferroptosis in vitro. Moreover, circATP2C1 facilitates the tumorigenicity of prostate cancer by inhibiting ferroptosis in vivo. Conclusions: Mechanistically, circATP2C1 hinders ferroptosis by increasing solute carrier family 7 member 11 (SLC7A11) expression via sponging miR-654-3p. In summary, our findings highlight the oncogenic role of circATP2C1 in prostate cancer and provide novel targets and strategies for treating prostate cancer.
    Keywords:  CircATP2C1; SLC7A11; ferroptosis; miR-654-3p; prostate cancer
    DOI:  https://doi.org/10.3390/cancers17213571
  4. Transl Androl Urol. 2025 Oct 31. 14(10): 2885-2901
       Background: The progression of prostate cancer (PCa) is closely associated with metabolic reprogramming and immune microenvironment dysregulation, while the mechanisms by which lactate-associated genes (LAGs) play a role remain unclear. This study aimed to elucidate the prognostic value and functional role of myeloperoxidase (MPO) in PCa and to explore its potential as a therapeutic target through comprehensive bioinformatics and experimental analyses.
    Methods: We integrated The Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO) databases to identify differentially expressed LAGs. Experimental validation using PCa tissues, PCa cell lines, and xenograft models assessed the functional role of MPO. Immune microenvironment analysis evaluated immune cell infiltration and checkpoint gene expression. Drug sensitivity predictions and Tumor Immune Dysfunction and Exclusion (TIDE) scoring were performed. Pan-cancer analysis examined MPO expression and prognostic significance across multiple cancer types.
    Results: We identified 17 differentially expressed LAGs, finding MPO to be an independent prognostic marker for PCa. MPO was significantly downregulated in PCa tissues and PCa cell lines. Overexpression of MPO inhibited tumor proliferation in vitro and in vivo by suppressing PI3K/AKT pathway phosphorylation (p-PI3K/p-AKT) and reduced tumor volume in xenografts. The MPO high-expression group showed increased infiltration of natural killer (NK) cells and elevated expression of immune checkpoint genes. Drug sensitivity predictions indicated patients with high MPO expression were more sensitive to PI3K/AKT inhibitors (e.g., temsirolimus), but their TIDE score suggested a potentially lower response to immunotherapy. Pan-cancer analysis confirmed low MPO expression in 20 cancer types and significant associations with prognosis in cancers including colorectal cancer and glioblastoma.
    Conclusions: This study revealed that MPO suppresses PCa progression through dual regulation of metabolism and immunity. MPO serves as an independent prognostic marker and its downregulation contributes to tumor growth via PI3K/AKT signaling while influencing the immune microenvironment. These findings suggest MPO as a new target for combined therapeutic strategies based on metabolic intervention.
    Keywords:  Lactate; PI3K/AKT signaling pathway; immunotherapy; myeloperoxidase (MPO); prostate cancer (PCa)
    DOI:  https://doi.org/10.21037/tau-2025-390
  5. Bioorg Chem. 2025 Nov 09. pii: S0045-2068(25)01091-0. [Epub ahead of print]167 109211
      Aberrant activation of the PI3K/Akt signaling pathway and frequent silencing of the tumor suppressor PTEN are central drivers of prostate cancer progression and therapeutic resistance. Addressing this dual dysregulation, we identified compound 25, a novel thiourea derivative, as a potent and selective anticancer agent. Among structurally related analogs, 25 exhibited the strongest antiproliferative activity in prostate cancer cells, while showing minimal cytotoxicity toward normal colon and kidney cells, indicating high selectivity for cancer cells. In vivo, 25 significantly suppressed tumor growth in a prostate cancer xenograft model in a dose-dependent manner, with greater efficacy than docetaxel. Target identification using AI-based target prediction platforms and kinase profiling revealed ROCK2 as the primary molecular target of 25. Mechanistically, 25 inhibited ROCK2 activity and nuclear expression, disrupting its interaction with transcriptional coactivators p300 and PGC-1α, thereby repressing oncogenic gene transcription, while restoring PTEN expression through the activation of FOXO1. This activation of PTEN led to suppression of PI3K/Akt signaling, cell cycle arrest, and apoptosis. Collectively, these findings uncover a nuclear transcriptional role of ROCK2 in sustaining oncogenic signaling and demonstrate that its inhibition by 25 restores tumor-suppressive PTEN/FOXO1 pathways. Compound 25 thus emerges as a promising therapeutic candidate for advanced prostate cancer.
    Keywords:  FOXO1; PI3K/Akt; PTEN; Prostate cancer; ROCK2; Thiourea derivatives
    DOI:  https://doi.org/10.1016/j.bioorg.2025.109211
  6. Discov Oncol. 2025 Nov 14. 16(1): 2102
       OBJECTIVE: To investigate the impact of neoadjuvant hormonal therapy (NHT) on interleukin‑17 A (IL‑17 A) signaling and inflammation in prostate cancer (PCa), and to explore the role of the IL‑17 A/signal transducer and activator of transcription 3 (STAT3) axis in tumor progression after androgen deprivation.
    METHODS: Paired prostate tissue samples from 27 patients receiving ≥ 3 months of NHT were analyzed. Histological inflammation was assessed by hematoxylin-eosin staining. Immunohistochemistry was used to evaluate IL-17 A, interleukin‑17 receptor A (IL‑17RA), interleukin‑17 receptor C (IL‑17RC), STAT3, and androgen receptor (AR). Statistical analyses were performed to examine differences in expression and correlations between markers.
    RESULTS: Chronic inflammation significantly increased in tumor tissues after NHT (P < 0.05). IL-17 A and IL-17RC expression were higher in tumor tissues than adjacent benign tissues (P < 0.001), with further upregulation after NHT (P < 0.05). Longer NHT duration (≥ 6 months) was associated with elevated IL-17 A and IL-17RC levels. IL-17 A expression positively correlated with STAT3 (r = 0.388, P = 0.045), but not with androgen receptor (AR).
    CONCLUSIONS: Prolonged NHT enhances IL-17 A/IL-17RC-mediated inflammation in prostate cancer, potentially promoting tumor progression through STAT3 activation. Targeting the IL-17 A/STAT3 axis may offer therapeutic potential for advanced prostate cancer, although further validation is required before NHT can be incorporated into clinical guidelines.
    Keywords:  IL-17A; Inflammation; Neoadjuvant hormonal therapy; Prostate cancer; STAT3
    DOI:  https://doi.org/10.1007/s12672-025-03945-7
  7. Epigenomics. 2025 Nov 10. 1-14
       AIMS: Matrix metalloproteinases (MMPs) promote prostate cancer (PCa) progression by degrading the extracellular matrix and enhancing metastasis. PCa is considered an "epigenetic catastrophe" due to disrupted histone modifications caused by chromatin-modifying enzyme dysregulation. We previously showed that lysine demethylase 6A (KDM6A) and 6B (KDM6B) are higher in metastatic PCa (LNCaP) versus benign prostatic hyperplasia (BPH-1). We investigated whether their elevation contributes to MMP upregulation.
    METHODS AND RESULTS: LNCaP cells were treated with the KDM6 inhibitor GSK-J4, and mRNA levels of 23 MMPs were quantified by RT-qPCR. GSK-J4 reduced mRNA levels of 6 MMPs (MMP-7, -8, -11, -15, -16, and -19) out of 23. Decline in pre-spliced mRNA levels of MMP-7, -11, and -16 by GSK-J4 suggested transcriptional changes; only MMP-11 and -16 exhibited corresponding protein decreases. Among downregulated MMPs, MMP-7, -11, -15 and -16 mRNA were higher in LNCaP versus BPH-1, confirmed at protein level for MMP-11 and -16. KDM6A - but not KDM6B - siRNA reduced MMP-11 and -16 expression. GSK-J4 increased histone3 lysine27 trimethylation (H3K27me3) enrichment at MMP-11 and -16 promoters, as shown by Chromatin Immunoprecipitation (ChIP).
    CONCLUSION: KDM6A demethylates H3K27me3 at MMP-11 and -16 promoters, sustaining their enhanced expression in PCa and revealing a novel epigenetic mechanism driving metastasis-associated protease expression.
    Keywords:  Epigenetic; GSK-J4; KDM6A; KDM6B; MMP; prostate cancer
    DOI:  https://doi.org/10.1080/17501911.2025.2586858
  8. Cancer Res. 2025 Nov 12.
      Advanced prostate cancer (PrCa) remains a leading cause of cancer-related death among men due to disease progression in nearly all patients on standard of care therapy targeting the androgen receptor. An important mechanism driving therapeutic resistance is lineage plasticity, which enables PrCa cells to reprogram into lineage variants no longer dependent on androgen receptor signaling. As inhibitors of the histone methyltransferase EZH2 are being evaluated clinically for the treatment of advanced PrCa, we investigated here how EZH2 affects PrCa lineage plasticity. Data from genetically engineered mice and human clinical samples demonstrated that genetic or pharmacological suppression of EZH2 altered chromatin to expand active transcription factor programs. These changes in gene expression during PrCa progression increased the diversity of PrCa lineage variants that arose. EZH2 suppression did not inhibit disease progression or therapeutic resistance in this context. These findings advance the current understanding of PrCa lineage plasticity and suggest EZH2 inhibitors may be less effective in treating PrCa prone to lineage plasticity.
    DOI:  https://doi.org/10.1158/0008-5472.CAN-25-2747
  9. Proc Natl Acad Sci U S A. 2025 Nov 18. 122(46): e2513468122
      Epigenetic and transcriptional dysregulation plays a fundamental role in tumor lineage plasticity (LP). However, the underlying mechanisms, especially for the initial events of LP development, are still poorly understood. Here, we report that in progression of prostate cancer from adenocarcinoma to treatment-induced neuroendocrine prostate cancer (t-NEPC), anti-androgen receptor (AR) signaling inhibitors (ARSIs) reprogram the function of circadian regulator/nuclear receptor REV-ERBα by switching its target gene programs from kinase signaling and metabolic programs to programs of LP, which includes neurogenesis, stem cell, and epithelial-mesenchymal transition as well as over fifteen LP drivers including POU3F2/BRN2, ASCL1, FOXA2, ONECUT2, and MYCN. Unexpectedly, REV-ERBα facilitates the chromatin occupancy of BRN2, ASCL1, and FOXA1 in their activation of LP programs, thus functioning as a master regulator of ARSI-induced LP driver network. Mechanistically, REV-ERBα induces chromatin accessibility and H3K27ac modification at promoters of LP genes through its recruitment of BRD4 and p300. Overexpression of REV-ERBα alone is sufficient to induce LP and neuroendocrine phenotype and confers resistance to ARSI in adenocarcinoma cells. Loss of REV-ERBα potently inhibits NEPC cell growth and abolishes the expression of LP drivers and gene programs. Pharmacological inhibition of REV-ERBα exhibits high potency in blocking the growth of NEPC tumors including patient-derived xenografts. Our findings reveal that therapy-induced LP development entails a coordinated induction of a network of LP drivers and that REV-ERBα is an unexpected master regulator of the network and a promising therapeutic target for treatment of advanced prostate cancer such as NEPC.
    Keywords:  NEPC; REV-ERBα; drug resistance; lineage plasticity; therapeutic targeting
    DOI:  https://doi.org/10.1073/pnas.2513468122
  10. Endocr Relat Cancer. 2025 Nov 12. pii: ERC-25-0272. [Epub ahead of print]
      The CUT/Hox transcription factor ONECUT2 (OC2) promotes lineage plasticity and is a confirmed therapeutic target in prostate cancer and several other malignancies where cell phenotype plays a substantial role in treatment resistance. OC2 governs a broad growth and lineage identity process in prostate cancer that promotes neuroendocrine (NE) differentiation, androgen receptor (AR) suppression, and the emergence of a wide range of treatment-resistant pathways. The mode of action of OC2 includes incorporation of the protein into transcription complexes at gene promoters as an activator and repressor, alteration of chromatin accessibility and epigenetic marks, and extensive alteration of large-scale chromatin modifications, such as super-enhancers and chromatin loops. Notably, OC2 may be unique among NE drivers in that it can promote AR-indifference in adenocarcinoma as a direct upstream activator of the glucocorticoid receptor, thus assuming indirect control of a portion of the AR cistrome. OC2 expression and activity increase substantially following hormone therapy in association with aggressive disease in prostate and breast cancer. Experiments in model systems have shown that OC2 has a survival function in both human castration-sensitive and castration-resistant prostate cancer cells. OC2 can be targeted directly with a family of novel small molecule inhibitors that show therapeutic efficacy in vivo in prostate, breast and gastric cancer models, including regression of established distant metastases in mice. These findings suggest that inhibition of OC2 clinically may confer substantial therapeutic benefit in some aggressive malignancies, including in localized, hormone-sensitive disease.
    DOI:  https://doi.org/10.1530/ERC-25-0272
  11. Cytojournal. 2025 ;22 80
       Objective: The objectives of the study are to investigate the differential metabolic paradigms and distribution of regulatory T (Tregs) cells between primary prostate cancer (PCa) and lymph node (LN) metastases.
    Material and Methods: Single-cell RNA sequencing analysis of primary PCa and LN metastases was employed to reveal the immune infiltration, identify Treg cell clusters, and analyze their metabolic regulation. Immunohistochemical (IHC) for FOXP3 and cluster of differentiation antigen 45 was used to verify different distribution and infiltration of Treg cells.
    Results: Immune cell infiltration was prominent around PCa cells, with Tregs significantly enriched in node-positive samples, suggesting an immunosuppressive microenvironment. Three Treg subsets were identified: Inhibitory Tregs, effector Tregs, and double-positive Tregs, each exhibiting distinct metabolic profiles. IHC confirmed higher Treg infiltration in LN metastases compared to primary tumors, particularly within tumor stroma.
    Conclusion: Tregs promote lymphatic metastasis in PCa through metabolic reprogramming, with their infiltration levels serving as a potential biomarker for metastatic risk.
    Keywords:  Foxp3; Metabolic feature; Prostate cancer; Regulatory T cell; Single-cell RNA sequencing
    DOI:  https://doi.org/10.25259/Cytojournal_44_2025
  12. Urol Oncol. 2025 Nov 13. pii: S1078-1439(25)00416-8. [Epub ahead of print]
       OBJECTIVES: This study used urine NMR spectroscopy to define a potential metabolic profile indicating presence of prostate cancer, which could be a useful noninvasive method for diagnosis of this neoplasia.
    METHODS: Urine samples were obtained from patients undergoing transrectal prostate biopsy after prostate massage. Patients were classified as diseased if cancerous tissue was obtained from biopsy histology, and all spectra were acquired using a Bruker Avance III DRX 600 spectrometer. Univariate and multivariate analyses were performed with metabolites and clinical variables with the objective of predicting tumor presence.
    RESULTS: A total of 201 patients were included in the study, with a mean age of 67.20 ± 7.90 years. Prostate cancer was diagnosed in 107 (53.2%) cases, with a negative result for malignancy in the other 94 (46.8%).Metabolic analysis revealed metabolic pathways such as glycolysis, Krebs cycle, and the metabolism of different amino acids as involved in the presence of prostate cancer. The 28 metabolites detected in urine, together with prostate volume and ultrasound suspicion for tumor, formed a predictive model of prostate cancer in tissue, with an area under the curve (AUC) of 0.89, a sensitivity of 89%, a positive predictive value (PPV) of 82% and a negative predictive value (NPV) of 83%.
    CONCLUSIONS: Metabolomics can be used to build a useful predictive model for diagnosing prostate cancer from the metabolic profile in urine, using a total of 28 metabolites. Combining metabolites, particularly molecules of glycerophospholipid metabolism, glycolysis, and amino acid metabolism, with clinical variables provides an effective strategy.
    DOI:  https://doi.org/10.1016/j.urolonc.2025.10.015
  13. Int J Mol Sci. 2025 Oct 31. pii: 10621. [Epub ahead of print]26(21):
      Fatty acid-binding protein 4 (FABP4) is an important adipokine associated with inflammatory responses and metabolic regulation. Although a high-fat diet (HF) and/or HF-mediated obesity have been clearly linked to the progression of prostate cancer, with FABP4 potentially playing a critical role in this relationship, the mechanisms by which FABP4 facilitates this interaction remain unclear. After generating FABP4 knockout (FABP4-/-) transgenic adenocarcinoma of the mouse prostate (TRAMP) mice, it was found that FABP4-/- TRAMP mice presented significantly ameliorated prostate tumorigenesis and tumor progression along with decreased body weight, protumorigenic cytokine secretion, and pan-amino acid synthesis when compared to TRAMP mice under the HF condition. Additionally, treatment with BMS309403-a chemical inhibitor of FABP4-was observed to abrogate the HF-mediated TRAMP tumor progression, along with reductions in body weight and cytokine production. Thus, FABP4 plays an essential role in the progression of HF-mediated prostate cancer through the modulation of metabolic and inflammatory pathways, providing a potential therapeutic target for prostate cancer.
    Keywords:  FABP4; TRAMP mice; high-fat diet; prostate cancer
    DOI:  https://doi.org/10.3390/ijms262110621
  14. Cell Oncol (Dordr). 2025 Nov 11.
      PURPOSE RETINOBLASTOMA L: (RB1) mutations frequently emerge as late subclonal events in advanced prostate cancer (PCa), driving inevitable recurrence and therapy resistance. Therapy-induced senescence (TIS) could promote metastasis at a late stage. However, the underlying mechanisms and therapeutic approaches for decetaxel-induced senescence (DIS) in RB1-deficient castration-resistant prostate cancer (CRPC) remain poorly understood.
    METHODS: We systematically evaluated the association between RB1 expression and tumor malignancy using TCGA-PRAD data and clinical prostate cancer samples. Multiple CRPC models were established, including RM-1 C57BL/6 and PC-3 BALB/c-nu mouse models, as well as human PC-3 and 22RV1 cells to uncover the double-edged nature of DIS. Subsequently, RNA sequencing of shRB1-DIS identified tumorigenic SASP factors. Furthermore, we investigated the molecular mechanisms of the combined treatment using techniques such as immunofluorescence, flow cytometry, chromatin immunoprecipitation (ChIP), dual luciferase reporter assay, and molecular docking.
    RESULTS: The clinical significance and negative correlation between RB1 expression and malignancy were verified in human PCa samples. Using murine and human CRPC models, we demonstrated that DIS response was retained in both RB1-knockdown and control groups. Strikingly, DIS promoted metastasis and accelerated the transition to neuroendocrine prostate cancer (NEPC) in RB1-deficient models. shRB1-DIS was marked by elevated senescence-associated β-galactosidase (SA-β-gal) activity and upregulation of p27Kip. RNA-seq analysis revealed a senescence-associated secretory phenotype (SASP) profile of shRB1-DIS, with upregulated IL-1α, CCL5, CCL20, MMP3, and IL-20. Mechanistically, we identified a novel FOXA1-IL20-IL20Rβ signaling axis which promoted macrophage polarization to M2-like phenotype. Notably, our data revealed that administration of ABT-263, eliminated shRB1 DIS-associated markers and SASPs, particularly, IL-20, both in vitro and in vivo experiments. Furthermore, molecular docking confirmed ABT-263 could directly bond to the IL-20 pocket with high affinity, and oeIL-20 advanced CRPC cells exhibited increased sensitivity to ABT-263 treatment. Therefore, the suppression of M2-like macrophages by ABT-263 was associated with reduced aggressiveness and decreased resistance to docetaxel in RB1-deficient CRPC.
    CONCLUSION: DIS accelerates the malignant progression of shRB1 CRPC, mediated by tumorigenic SASP, especially IL-20 enrichment. Notably, we identifies a novel FOXA1-IL-20-IL20Rβ axis that drives M2-like macrophage polarization and contributes to tumor aggressiveness and docetaxel resistance. Importantly, senolytic agent ABT-263 not only selectively eliminated shRB1-DIS cells but also restricted expression of tumorigenic SASPs, thereby restoring sensitivity to docetaxel. Wherein, IL-20 is inhibited through its interaction with ABT-263. These results provide a novel mechanistic rationale for using senolytic therapies to mitigate SASP-driven malignancy and improve treatment response in RB1-deficient CRPC.
    CLINICAL TRIAL NUMBER: Not applicable.
    DOI:  https://doi.org/10.1007/s13402-025-01126-w
  15. Neoplasia. 2025 Nov 13. pii: S1476-5586(25)00133-2. [Epub ahead of print]71 101253
      Androgen receptor (AR) signaling remains a key driver of castration-resistant prostate cancer (CRPC), with AR splice variants like AR-V7 contributing to resistance against second-generation antiandrogens. Targeting the AR N-terminal domain (NTD) provides a strategy to bypass ligand-binding domain (LBD)-mediated resistance. We developed ITRI-148, a CRBN-based AR-NTD degrader incorporating a rigid piperidine-alkyne linker optimized for oral pharmacokinetics. ITRI-148 efficiently degrades full-length AR, AR-V7, and clinically relevant mutants (L702H, H875Y). It facilitates the recruitment of active AR species to CRBN in the nucleus, promoting their polyubiquitination and proteasomal degradation. In CRPC and enzalutamide-resistant models, ITRI-148 robustly suppresses AR signaling and inhibits cell viability, outperforming enzalutamide. With long-term treatment, it achieves sustained AR suppression without inducing compensatory AR-V7 upregulation or PSA re-expression. In vivo, ITRI-148 demonstrates potent antitumor efficacy in both castrated and hormone-intact CRPC models, supported by favorable pharmacokinetic properties, stability and safety profiles. These findings position ITRI-148 as a promising next-generation AR-targeting agent capable of degrading resistant AR variants and providing durable inhibition of AR signaling in advanced prostate cancer.
    Keywords:  AR, AR-V7; Drug resistance; PROTAC; Prostate cancer
    DOI:  https://doi.org/10.1016/j.neo.2025.101253
  16. Toxicol Appl Pharmacol. 2025 Nov 11. pii: S0041-008X(25)00414-4. [Epub ahead of print] 117638
      Metastatic, castration-resistant prostate cancer (mPC) is driven by epithelial-to-mesenchymal transition (EMT), acquisition of stem-like traits, and resistance to apoptosis, processes orchestrated by TGF-β and reinforced by Wnt/β-catenin signaling. Effective agents that can simultaneously intercept these pathways remain scarce. Here, we investigated the dietary lignan Matairesinol (MAT) as a multitarget EMT antagonist in PC3 cells. RNA-seq followed by rigorous quality control (Phred >30; > 90 % unique mapping) identified 152 MAT-responsive transcripts (74 up-, 78 down-regulated). GeneCodis and Hallmark enrichment revealed MAT-mediated suppression of hypoxia response, NF-κB/TNF signaling, focal adhesion, and ECM-receptor interaction, alongside activation of p53 and senescence programs. Overlap with 24 cancer Hallmark gene sets yielded 56 prostate-relevant DEGs, highlighting down-regulation of EMT-supportive pathways and up-regulation of tumor-suppressive networks. Functional validation in a TGF-β-induced EMT model showed that MAT (50, 100, and 150 μM) partially restored epithelial morphology, curtailed clonogenicity, and inhibited migration. JC-1 and ROS assays demonstrated reversal of EMT-associated apoptosis resistance via mitochondrial depolarization and oxidative-stress elevation. MAT also reduced mitochondrial biomass and dismantled actin stress fibers. Analysis by qRT-PCR and flow cytometry confirmed re-expression of E-cadherin, suppression of Vimentin/N-cadherin, and down-regulation of Snail, Twist, and Zeb1. Importantly, MAT lowered β-catenin while restoring GSK3β, inhibited downstream targets MYC and CCND1, shrank tumorspheres, and reduced CD44 expression. Collectively, MAT counters TGF-β/Wnt-driven EMT, stemness, and survival signaling at both transcriptomic and phenotypic levels. These findings nominate MAT as a promising scaffold for anti-metastatic therapy in advanced prostate cancer and warrant further in-vivo evaluation.
    Keywords:  Matairesinol; Metastatic Prostate cancer (mPCa); PC3 Cells; TGF-β-Induced EMT
    DOI:  https://doi.org/10.1016/j.taap.2025.117638
  17. Front Sports Act Living. 2025 ;7 1602123
       Introduction: The incidence of metastatic prostate cancer (mPCa) is increasing despite a decrease in the prevalence of prostate cancer (PCa). Androgen deprivation therapy (ADT), the mainstay of systemic treatment for mPCa, is associated with numerous side effects, including a decline in muscle mass and physical function, which lead to the exacerbation of age-related frailty and sarcopenia. Exercise plays a key role in ameliorating or preventing the progression of ADT-related side effects and in improving muscle mass, fitness, and strength. However, exercise interventions in patients with mPCa have been understudied, with a lack of studies focusing on frailty and sarcopenia and the mechanisms by which exercise could address these issues.
    Purpose: Thus, we have designed the FIERCE trial to assess the effects of a 16-week multicomponent exercise intervention, encompassing resistance and aerobic training, on frailty and sarcopenic status and their potential mechanistic biomarkers, as well as on cancer cell proliferation (NCT06040125).
    Methods: The FIERCE trial is a prospective study aiming to recruit 80 pre-frail/frail men with mPCa receiving ADT who will be randomized to either an exercise or an attention control group. The 16-week exercise intervention will include thrice-weekly, clinic-supervised, resistance exercise circuit training and self-directed home-based aerobic exercise. The attention control group will receive a stretching program and will be offered the exercise program following the study period. The primary outcome is frailty, measured by the Fried frailty phenotype (i.e., muscle loss, exhaustion, physical activity, gait speed, and strength) and frailty-associated biomarkers [IL-6, TNF-α, C-reactive protein (CRP)]. Secondary outcomes include sarcopenia, measured using dual-energy x-ray absorptiometry scans and sarcopenia-associated muscle biopsy-driven biomarkers (myokines and insulin pathway markers). An exploratory outcome will assess how exercising patient-derived plasma will affect the proliferation of prostate cancer cells (LNCaP cells).
    Conclusion: This first-of-its-kind study targets a vulnerable, understudied population: frail men with mPCa. If successful, our findings will establish the efficacy of a multicomponent exercise intervention on frailty and sarcopenic status, providing the foundation for future larger phase II and III trials to confirm the findings and potentially establish exercise as a safe and necessary part of the standard of care for frail metastatic prostate cancer patients.
    Keywords:  androgen deprivation therapy; exercise; frailty; prostate cancer; sarcopenia
    DOI:  https://doi.org/10.3389/fspor.2025.1602123
  18. In Silico Pharmacol. 2025 ;13(3): 169
      This study investigates the therapeutic potential of bioactive compounds from Lepidium sativum in the treatment of prostate cancer. Through a series of in silico analyses, three key compounds were identified and evaluated for their drug-likeness, pharmacokinetic properties, and safety profiles. These compounds demonstrated favorable drug-likeness according to Lipinski's rule and other drug-likeness criteria, high gastrointestinal tract absorption, and non-inhibition of major cytochrome P450 enzymes. Protein-protein interaction network analysis identified ten hub genes, with AKT1 and PIK3CA emerging as prime targets for therapeutic intervention. Functional annotation and pathway analysis highlighted key biological processes and pathways associated with prostate cancer, emphasizing the significance of these targets. Molecular docking and dynamic simulation studies further confirmed the binding affinities and stability of the identified compounds with both mutated and non-mutated forms of the target genes. These findings suggest that compounds from Lepidium sativum hold promise as potential therapeutics for prostate cancer, warranting further investigation and development.
    Supplementary Information: The online version contains supplementary material available at 10.1007/s40203-025-00482-7.
    Keywords:  Lepidium sativum; Molecular dynamics; Network pharmacology; Prostate cancer
    DOI:  https://doi.org/10.1007/s40203-025-00482-7
  19. Transl Androl Urol. 2025 Oct 31. 14(10): 3256-3267
       Background: Metabolic obesity phenotypes have been identified as predictive factors for various cancers. This study aimed to investigate the association between metabolic obesity phenotypes and prostate cancer (PCa) among the U.S. population aged ≥50 years.
    Methods: This cross-sectional study analyzed data from the National Health and Nutrition Examination Survey 1999-2018. Participants were categorized into four groups: metabolically healthy non-obese (MHNO), metabolically healthy obese (MHO), metabolically unhealthy non-obese (MUNO), and metabolically unhealthy obese (MUO). Weighted multivariable logistic regression was used to identify groups with a higher prevalence of PCa, and subgroup analyses were conducted based on age.
    Results: The median age of the participants was 64 years. No significant differences in PCa prevalence were found between the obese and non-obese groups (P=0.33). In the younger population (50 to 64 years old), metabolic abnormalities such as hyperglycemia (P=0.004) and hypertension (P<0.001) was strongly correlated with an increased PCa prevalence. Individuals with MUNO [odds ratio (OR) =3.179; 95% confidence interval (CI): 1.449-6.974] and those with MUO (OR =4.345; 95% CI: 2.076-9.093) were significantly associated with higher PCa prevalence. No significant differences in PCa prevalence were found between the MHNO and MHO groups, or between the MUNO and MUO groups. In the older population (age ≥65 years), no association was found between metabolic obesity phenotypes and PCa prevalence.
    Conclusions: Metabolic abnormalities play a more critical role than obesity alone in determining PCa prevalence, particularly among individuals aged 50 to 64 years old.
    Keywords:  Obesity; metabolic abnormalities; metabolic obesity phenotypes; prostate cancer (PCa)
    DOI:  https://doi.org/10.21037/tau-2025-538
  20. Diagnostics (Basel). 2025 Oct 31. pii: 2767. [Epub ahead of print]15(21):
      Background/Objective: Biochemical recurrence (BCR) after radical prostatectomy (RP) for prostate cancer indicates disease progression. Although type 2 diabetes mellitus (T2D) shows a paradoxical association with prostate cancer risk, the prognostic role of T2D-related genetic variants remains unclear. Methods: We analyzed 113 common T2D susceptibility-related single-nucleotide polymorphisms (SNPs) in 644 Taiwanese men with localized prostate cancer (D'Amico risk classification: 12% low, 34% intermediate, and 54% high) treated with RP. Associations between SNPs and BCR were assessed using Cox regression, adjusting for key clinicopathological factors. Functional annotation was performed using HaploReg and FIVEx, while The Cancer Genome Atlas transcriptomic data were analyzed for C2 calcium-dependent domain-containing 4A (C2CD4A) expression. Gene set enrichment analysis (GSEA) and gene set variation analysis (GSVA) were applied to explore related biological pathways. Results:C2CD4A SNP rs4502156 was independently associated with a reduced risk of BCR (hazard ratio = 0.80, p = 0.035). The protective C allele correlated with higher C2CD4A expression. Low C2CD4A expression is associated with advanced pathological stages, higher Gleason scores, and disease progression. GSEA revealed negative enrichment of mitotic and chromatid segregation pathways in high-C2CD4A-expressing tumors, with E2F targets being the most suppressed. GSVA confirmed an inverse correlation between C2CD4A expression and E2F pathway activity, with CDKN2C as a co-expressed functional gene. Conclusions: The T2D-related variant rs4502156 in C2CD4A independently predicts a lower risk of BCR, potentially via suppression of the E2F pathway, and may serve as a germline biomarker for postoperative risk stratification.
    Keywords:  C2CD4A; prognostic biomarker; prostate cancer; recurrence; type 2 diabetes
    DOI:  https://doi.org/10.3390/diagnostics15212767
  21. Cancer Epidemiol Biomarkers Prev. 2025 Nov 13.
       BACKGROUND: Healthy dietary patterns have been linked to reduced cancer risk, but evidence for prostate cancer (PCa) remains inconsistent, especially across diverse populations.
    METHODS: In the Multiethnic Cohort Study, we examined the associations between 11 diet scores and PCa risk among 79,930 men (White, African American, Japanese American, Latino, or Native Hawaiian). Hazard ratios (HRs) and 95% confidence intervals (CIs) per one standard deviation (SD) increase in each score were estimated from Cox proportional hazards models for total PCa and by grade, stage, and aggressiveness. Analyses were conducted in the overall population and within racial/ethnic groups. A significance threshold of p<0.003 was used to adjust for multiple testing.
    RESULTS: Over a mean follow-up of 18.8 years, 9,759 PCa cases were identified. No significant associations were observed in the hypothesized direction between dietary scores and PCa risk in the overall population. However, among African Americans, higher Dietary Approaches to Stop Hypertension (DASH) scores were suggestively associated with a 14% lower risk of advanced PCa (95% CI: 0.77-0.98, p=0.02). Among Japanese Americans, higher Empirical Dietary Index for Insulin Resistance (EDIR) scores were linked to an increased risk of low-grade (HR=1.09, 95% CI: 1.02-1.17, p=0.01) and non-aggressive PCa (HR=1.10, 95% CI: 1.02-1.19, p=0.02).
    CONCLUSIONS: Although no strong associations were found overall, our findings suggested that specific dietary patterns may influence PCa risk differently by race/ethnicity and tumor subtype, warranting further investigation in large and diverse populations.
    IMPACT: These findings highlight the need for future studies to explore disease-specific and culturally informed dietary patterns that may inform PCa prevention across diverse populations.
    DOI:  https://doi.org/10.1158/1055-9965.EPI-25-1247
  22. Cancer Res Commun. 2025 Nov 11.
      Metastatic hormone-sensitive prostate cancer (mHSPC) often progresses to castration-resistant prostate cancer despite current therapies, necessitating the use of reliable biomarkers. This study aimed to develop a novel model for predicting progression-free survival (PFS) using circulating tumor DNA (ctDNA) sequencing. We analyzed 127 patients with mHSPC and compared ctDNA mutations with those in matched primary tumor tissues. A four-gene signature (TRPC: TP53, RB1, PTEN, and CDK12) was identified, forming the basis of the blood-based TRPC (b.TRPC) model. The b.TRPC model demonstrated high specificity and sensitivity in predicting PFS, outperforming ctDNA markers. Internal and external validation confirmed that b.TRPC is an independent prognostic factor with superior predictive performance for 0.5-, 1-, and 2-year PFS. The model also showed significant clinical relevance, with bTRPC-positive patients exhibiting shorter survival times under ADT and doublet therapy, although this disparity diminished with triplet therapy. These findings highlight the potential of ctDNA-based gene mutation analysis to guide personalized treatment strategies for mHSPC, offering a non-invasive alternative to tissue-based analyses and improving prognostic accuracy.
    DOI:  https://doi.org/10.1158/2767-9764.CRC-25-0384
  23. Diagnostics (Basel). 2025 Oct 28. pii: 2737. [Epub ahead of print]15(21):
      Prostate-specific membrane antigen (PSMA) targeting agents have been the cornerstone of advanced prostate cancer (PCa) management in theranostics due to their high sensitivity for detecting and treating metastatic disease. However, approximately one-third of metastatic castration-resistant PCa (mCRPC) lesions may exhibit low or absent PSMA expression due to tumor heterogeneity, prior androgen deprivation therapy, or loss of androgen receptor expression, subsequently altering their response to PSMA-targeted therapy. The molecular and biological mechanisms underlying PSMA downregulation remain elusive but may include neuroendocrine differentiation or epithelial-to-mesenchymal transition (EMT). This review addresses this knowledge gap by examining recent preclinical and clinical evidence on novel radiotracers with the potential to provide alternative strategies beyond PSMA for imaging and treating PCa. The diagnostic performance and therapeutic potential of three emerging radiotracer classes are discussed, including gastrin-releasing peptide receptor (GRPR) ligands, androgen receptor (AR) ligands, and amino acid analogs. This article further highlights the complementary roles of these radiotracers along with their utility in specific patient populations, such as those with low prostate-specific antigen (PSA), biochemical recurrence (BCR), or confirmed PSMA-negative disease. For instance, GRPR-targeted radiotracers have achieved sensitivity of up to 88% and specificity of up to 90% for detecting primary tumors in PCa. The radiolabeled androgen agonist, fluorine-18 (18F)-fluoro-5α-dihydrotestosterone (FDHT), has demonstrated 98% true-positive rate in predicting lesions on positron emission tomography (PET) scans of mCRPC patients. On the other hand, the synthetic amino acid analog 18F-fluciclovine demonstrated a lesion detection rate of 84% for PSA levels at or above 5, and 62.5% for PSA levels ranging from 0.7 to less than 1. This review concludes with future directions on the paradigm of multi-tracer and dual-targeting strategies, which can effectively address challenges associated with PCa tumor heterogeneity and facilitate personalized approaches in theranostics.
    Keywords:  GRPR; PET/CT; PSMA-negative; androgen receptor; bombesin; fluciclovine; molecular imaging; prostate cancer; radionuclide therapy; theranostics
    DOI:  https://doi.org/10.3390/diagnostics15212737
  24. Cell Death Dis. 2025 Nov 10. 16(1): 817
      Thioredoxin-Interacting Protein (TXNIP) is an arrestin at the crossroad of redox and glycolytic metabolisms. Prostate cancer (PCa) exhibits a unique metabolic profile due to the glycolytic nature of healthy prostate tissue. We hypothesize that TXNIP plays a pivotal role in the progression of PCa to castration-resistant prostate cancer (CRPC), an incurable stage of the disease characterized by profound metabolic reprogramming and independence from androgens. Only a subset of patients progresses to CRPC, and current stratification tools lack robust biomarkers. TXNIP expression is directly suppressed by androgens and diminishes during tumor initiation and progression, as demonstrated in both human samples and a prostate adenocarcinoma mouse model (TRAMP). TXNIP regulates glucose metabolism by sequestering the glucose transporter GLUT1 away from the membrane, shifting metabolism from glycolysis to glutaminolysis. Nuclear-localized TXNIP induces cell cycle arrest through the upregulation of p27kip1 which is downregulated together with TXNIP in CRPC. The response to androgen deprivation therapy (ADT) strongly depends on TXNIP expression. In the murine model, TXNIP levels were significantly higher in ADT responders compared to non-responders. Furthermore, TRAMP-Txnip-/- prostate tumors exhibited a poorer response to ADT, with increased Ki67 and enhanced viability. In clinical samples, all patients on relapse showed low levels of TXNIP and progressed to CRPC. Our findings identify TXNIP as a critical regulator of cell cycle and glucose metabolism in PCa and emphasize for the first time its essential role in mediating therapeutic responses to ADT.
    DOI:  https://doi.org/10.1038/s41419-025-08128-4
  25. Discov Oncol. 2025 Nov 11. 16(1): 2091
       BACKGROUND: Prostate cancer (PCa) is the most common tumor in the male urogenital system. Radical prostatectomy, radiation, chemotherapy and endocrine therapy are common clinical treatment methods. Oncogene-induced senescence (OIS) is a special type of cellular senescence believed to have anti-tumor effects, may serve as an initial barrier for preventing tumor growth and development. As of yet, the effects of OIS on the occurrence, development, prognosis of prostate cancer and its related mechanisms are poorly understood, so further study is urgently needed.
    MATERIALS AND METHODS: Gene transcriptomic data and clinical information data for PCa were downloaded from TCGA and GEO databases, OISGs were obtained from the Reactome database. We identified OIS-related subtypes based on consistent cluster analysis. Univariate Cox regression analysis was performed to identify PR-OISGs. LASSO regression analysis finally screened prognosis-related key genes and constructed a risk score model. Patients were classified into high-/ low-risk groups based on the median risk score. We assessed the TMB, immune cell infiltration level, immune checkpoint expression and drug sensitivity between high-/ low-risk groups. A nomogram was constructed and validated using calibration curves and clinical decision curves. RT-qPCR and IHC staining analysis were performed to verify the mRNA and protein expression levels of target genes.
    RESULTS: The study identified two OIS-associated subtypes of PCa. We screened seven PRGs and established a risk model for PCa patients. It was found that BFS (biochemical recurrence-free survival) was significantly lower in high-risk group. Patients in the high-risk group showed greater immune infiltration and high expression of immune checkpoint, as well as higher TMB. Furthermore, stratifying the risk score appropriately allowed the predictive nomogram model to accurately predict the outcome of prostate cancer patients. Also, docetaxel and Olaparib sensitivity was higher in the high-risk group, whereas bicalutamide was more sensitive in the low-risk group. IHC and PCR confirmed CDK6 was highly upregulated in PCa.
    CONCLUSION: Our study screened seven genes with potential value for predicting long-term survival of patients with PCa and developed a prognostic model. These findings are expected to guide future development of effective therapies.
    Keywords:  Biochemical recurrence ; Immune microenvironment; Oncogene-induced senescence; Prognostic model; Prostate cancer
    DOI:  https://doi.org/10.1007/s12672-025-03893-2
  26. Cancers (Basel). 2025 Oct 27. pii: 3441. [Epub ahead of print]17(21):
      Despite advances in diagnostic and therapeutic technology, prostate cancer remains a leading cause of morbidity and mortality among men. While androgen deprivation therapy and next-generation androgen receptor pathway inhibitors offer durable responses, the emergence of the lethal phenotype, metastatic castration-resistant prostate cancer (mCRPC) eventually develops for most. A growing body of evidence points to the tumor microenvironment (TME) as a key driver of immune evasion and therapeutic failure. This review focuses on the current knowledge of immune suppression in the prostate TME, including cancer-associated fibroblasts, myeloid-derived suppressor cells, tumor-associated macrophages, immune checkpoint pathways, and several associated key metabolic alterations. These cellular and molecular networks contribute to therapeutic resistance and disease progression and may be used as therapeutic targets. We will also examine emerging treatment strategies aimed at reprogramming the TME, as well as combination approaches incorporating immunotherapies with other signaling inhibitors. Future success in clinical therapeutic development for mCRPC will depend on rational combinations that address both tumor-intrinsic resistance and extrinsic immune suppression, with emphasis on biomarker-driven patient and treatment selection.
    Keywords:  biomarker-driven treatment; immune evasion; metastatic castration-resistant prostate cancer; prostate cancer; tumor microenvironment
    DOI:  https://doi.org/10.3390/cancers17213441