ArticleChemical biology & drug design2021
Design and synthesis of isothiocyanate-containing hybrid androgen receptor (AR) antagonist to downregulate AR and induce ferroptosis in GSH-Deficient prostate cancer cells.
Article in Chemical biology & drug design, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 29 citations in OpenAlex.
- Isothiocyanates as Ferroptosis Inducers to Promote Cancer Cell Death.Phytotherapy research : PTR · 2026Review
- Advances in ferroptosis for castration-resistant prostate cancer treatment: novel drug targets and combination therapy strategies.Prostate cancer and prostatic diseases · 2026Review
- Unlocking ferroptosis in prostate cancer - the road to novel therapies and imaging markers.Nature reviews. Urology · 2024Review
- Natural products targeting ferroptosis pathways in cancer therapy (Review).Oncology reports · 2024Review
- Article
- Low androgen levels induce ferroptosis of rat penile cavernous endothelial cells.Sexual medicine · 2023Article
- Prolyl 4-hydroxylase subunit beta (P4HB) could serve as a prognostic and radiosensitivity biomarker for prostate cancer patients.European journal of medical research · 2023Article
- Ferroptosis-modulating small molecules for targeting drug-resistant cancer: Challenges and opportunities in manipulating redox signaling.Medicinal research reviews · 2023Review
- Ferroptosis landscape in prostate cancer from molecular and metabolic perspective.Cell death discovery · 2023Review
- MicroRNA-142-3p promotes renal cell carcinoma progression by targeting RhoBTB3 to regulate HIF-1 signaling and GGT/GSH pathways.Scientific reports · 2023Article
- Inaugurating a novel adjuvant therapy in urological cancers: Ferroptosis.Cancer pathogenesis and therapy · 2023Review
- The role of ferroptosis in prostate cancer: a novel therapeutic strategy.Prostate cancer and prostatic diseases · 2023Review
- Ferroptosis: a new antidepressant pharmacological mechanism.Frontiers in pharmacology · 2023Review
- System XFrontiers in pharmacology · 2022Review
- Ferroptosis and its role in skeletal muscle diseases.Frontiers in molecular biosciences · 2022Review
- Roles of ferroptosis in urologic malignancies.Cancer cell international · 2021Review
- Identifying a Ferroptosis-Related Gene Signature for Predicting Biochemical Recurrence of Prostate Cancer.Frontiers in cell and developmental biology · 2021Article
- Regulated Cell Death in Urinary Malignancies.Frontiers in cell and developmental biology · 2021Review
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
Sustained androgen receptor (AR) signaling and apoptosis evasion are among the main hurdles of castration-resistant prostate cancer (CRPC) treatment. We designed and synthesized isothiocyanate (ITC)-containing hybrid AR antagonist (ITC-ARi) and rationally combined ITC-ARi with GSH synthesis inhibitor buthionine sulfoximine (BSO) to efficiently downregulate AR/AR splice variant and induce ferroptosis in CRPC cells. The representative ITC-ARi 13 is an AR ligand that contains an N-acetyl cysteine-masked ITC moiety and gradually releases parental unconjugated ITC 12b in aqueous solution. The in vitro anti-PCa activities of 13, such as growth inhibition and AR downregulation, are significantly enhanced when combined with BSO. The drug combination caused notable lipid peroxidation and the cell viability was effectively rescued by iron chelator, antioxidants or the inhibitor of heme oxygenase-1, supporting the induction of ferroptosis. 13 and BSO cooperatively downregulate AR and induce ferroptosis likely through increasing the accessibility of 13/12b to cellular targets, escalating free intracellular ferrous iron and attenuating GSH-centered cellular defense and adaptation. Further studies on the combination of ITC-ARi and GSH synthesis inhibitor could result in a new modality against CRPC.
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