Identification of novel small-molecule inhibitors of α-methylacyl-CoA racemase (AMACR; P504S) and structure-activity relationships
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چکیده
منابع مشابه
High-throughput screen identifies novel inhibitors of cancer biomarker α-methylacyl coenzyme A racemase (AMACR/P504S).
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 enzym...
متن کاملA novel colorimetric assay for α-methylacyl-CoA racemase 1A (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate.
α-Methylacyl-CoA racemase (AMACR; P504S) regulates branched-chain fatty acid degradation, activates Ibuprofen and is a recognised cancer drug target. A novel, facile colorimetric assay was developed based on elimination of 2,4-dinitrophenolate. The assay was used to test 5 known inhibitors, determining IC50 and Ki values, reversibility and characterizing irreversible inhibition.
متن کاملIncreased expression of α-methylacyl-coenzyme A racemase (AMACR; p504s) and p16 in distal hyperplastic polyps
BACKGROUND Hyperplastic polyps (HP) and sessile serrated adenomas (SSA) share morphological similarities. In this immunohistochemical study we chose a panel of potential relevant and promising biomarkers including α-methylacyl-coenzyme A racemase (AMACR; p504s), which is involved in the degradation of branched chained fatty acids derivates, and analysed a cohort of HPs and SSAs in order to iden...
متن کاملTherapeutic Discovery High-Throughput Screen Identifies Novel Inhibitors of Cancer Biomarker a-Methylacyl Coenzyme A Racemase (AMACR/P504S)
a-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 enzym...
متن کاملDiagnostic Value of Cytokeratin 34 beta E12 (Ck34βE12) and α-Methylacyl-CoA racemase (AMACR) Immunohistochemical Expression in Prostatic Lesions
Background & Objective: Some prostatic lesions contain small suspicious foci for prostatic carcinoma in which the morphological features are equivocal. Two immunohistochemical markers namely, cytokeratin 34 beta E12 (Ck34βE12) and α-Methylacyl-CoA racemase (AMACR), were evaluated in these lesions for a definitive diagnosis and avoiding misdiagnosis or overdiagnosis of prostatic...
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ژورنال
عنوان ژورنال: Bioorganic Chemistry
سال: 2019
ISSN: 0045-2068
DOI: 10.1016/j.bioorg.2019.103264