ArticleMolecular cancer therapeutics2011
High-throughput screen identifies novel inhibitors of cancer biomarker α-methylacyl coenzyme A racemase (AMACR/P504S).
Article in Molecular cancer therapeutics, 2011. 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, 48 citations in OpenAlex.
- Sulforaphane Bioavailability and Chemopreventive Activity in Men Presenting for Biopsy of the Prostate Gland: A Randomized Controlled Trial.Nutrition and cancer · 2020Trial
- α-Methylacyl-CoA Racemase fromBiomolecules · 2024Article
- Comparative Proteomic and Transcriptomic Analysis of the Impact of Androgen Stimulation and Darolutamide Inhibition.Cancers · 2022Article
- Oncogenic Activity of Solute Carrier Family 45 Member 2 and Alpha-Methylacyl-Coenzyme A Racemase Gene Fusion Is Mediated by Mitogen-Activated Protein Kinase.Hepatology communications · 2022Article
- Racemases and epimerases operating through a 1,1-proton transfer mechanism: reactivity, mechanism and inhibition.Chemical Society reviews · 2021Review
- Peroxisome Metabolism in Cancer.Cells · 2020Review
- Current Knowledge on the Function of α-Methyl Acyl-CoA Racemase in Human Diseases.Frontiers in molecular biosciences · 2020Review
- Article
- Selection of aptamers for AMACR detection from DNA libraries with different primers.RSC advances · 2018Article
- AMACR overexpression acts as a negative prognostic factor in oral squamous cell carcinoma.International journal of medical sciences · 2018Article
- Induction of alpha-methylacyl-CoA racemase by miR-138 via up-regulation of β-catenin in prostate cancer cells.Journal of cancer research and clinical oncology · 2017Article
- A combinatorial approach for the discovery of cytochrome P450 2D6 inhibitors from nature.Scientific reports · 2017Article
- Prostate cancer metastasis to the distal phalanx of the left hallux: The first confirmed case and literature review.Oncology letters · 2016Article
- A study on the AMACR catalysed elimination reaction and its application to inhibitor testing.Organic & biomolecular chemistry · 2016Article
- Article
- AMACR overexpression as a poor prognostic factor in patients with nasopharyngeal carcinoma.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2014Article
- Utility of α-methylacyl-coenzyme-A racemase (p504s) immunohistochemistry in distinguishing endometrial clear cell carcinomas from serous and endometrioid carcinomas.Human pathology · 2013Article
- Identification of cetrimonium bromide and irinotecan as compounds with synthetic lethality against NDRG1 deficient prostate cancer cells.Cancer biology & therapy · 2013Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
α-methylacyl coenzyme A racemase (AMACR) is a metabolic enzyme whose overexpression has been shown to be a diagnostic indicator of prostatic adenocarcinoma and other solid tumors. Here, we confirm that attenuation of AMACR expression diminishes the growth of prostate cancer cell lines by using stably expressed short-hairpin RNA constructs. This observation strongly suggests that the AMACR enzyme may be a target for therapeutic inhibition in prostate cancer. To this end, we report here a novel assay capable of screening libraries of diverse small molecules for inhibitors of AMACR activity. This assay facilitated the screening of approximately 5,000 unique compounds and the discovery of 7 distinct chemical entities capable of inhibiting AMACR at low micromolar concentrations. The most potent inhibitor discovered is the seleno-organic compound ebselen oxide [inhibitory concentration (IC(50)): 0.80 μmol/L]. The parent compound, ebselen (IC(50): 2.79 μmol/L), is a covalent inactivator of AMACR (K(I)((inact)): 24 μmol/L). Two of the AMACR inhibitors are selectively toxic to prostate cancer cell lines (LAPC4/LNCaP/PC3) that express AMACR compared to a normal prostate fibroblast cell line (WPMY1) that does not express the protein. This report shows the first high-throughput screen for the discovery of novel AMACR inhibitors, characterizes the first nonsubstrate-based inhibitors, and validates that AMACR is a viable chemotherapeutic target in vitro.
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