A novel colorimetric assay for α-methylacyl-CoA racemase 1A (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate.
نویسندگان
چکیده
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.
منابع مشابه
A study on the AMACR catalysed elimination reaction and its application to inhibitor testing.
α-Methylacyl-CoA racemase (AMACR; P504S) catalyses a key step in the degradation of branched-chain fatty acids and is important for the pharmacological activation of Ibuprofen and related drugs. Levels of AMACR are increased in prostate and other cancers, and it is a drug target. Development of AMACR as a drug target is hampered by lack of a convenient assay. AMACR irreversibly catalyses the el...
متن کاملHigh-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 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...
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 کاملDiagnostic utility of α-methylacyl CoA racemase (P504S) & HMWCK in morphologically difficult prostate cancer
BACKGROUND To evaluate the diagnostic utility of alpha-methylacyl CoA racemase (P504S) & HMWCK (34beta E12) in morphologically difficult prostate cancer. METHODS A total of 1034 cases were reviewed and divided into benign (585) malignant (399) and suspicious (50). Immunohistochemistry with HMWCK and AMACR was done on the 50 suspicious cases along with controls. RESULTS Forty nine suspicious...
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ورودعنوان ژورنال:
- Chemical communications
دوره 53 37 شماره
صفحات -
تاریخ انتشار 2017