| People | Locations | Statistics |
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| Naji, M. |
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| Motta, Antonella |
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| Aletan, Dirar |
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| Mohamed, Tarek |
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| Ertürk, Emre |
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| Taccardi, Nicola |
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| Kononenko, Denys |
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| Petrov, R. H. | Madrid |
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| Alshaaer, Mazen | Brussels |
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| Bih, L. |
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| Casati, R. |
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| Muller, Hermance |
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| Kočí, Jan | Prague |
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| Šuljagić, Marija |
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| Kalteremidou, Kalliopi-Artemi | Brussels |
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| Azam, Siraj |
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| Ospanova, Alyiya |
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| Blanpain, Bart |
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| Ali, M. A. |
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| Popa, V. |
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| Rančić, M. |
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| Ollier, Nadège |
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| Azevedo, Nuno Monteiro |
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| Landes, Michael |
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| Rignanese, Gian-Marco |
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James, Tony D.
University of Bath
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (7/7 displayed)
- 2023Polymer Indicator Displacement Assay (PIDA) with Boronic Acid Receptors on Graphene Foam Electrodes for Self-Optimised Impedimetric Lactic Acid Determinationcitations
- 2020A simple, azulene-based colorimetric probe for the detection of nitrite in watercitations
- 2018A quick and selective rhodamine based “smart probe” for “signal-on” optical detection of Cu2+ and Al3+ in water, cell imaging, computational studies and solid state analysiscitations
- 2018A quick and selective rhodamine based “smart probe” for “signal-on” optical detection of Cu 2+ and Al 3+ in water, cell imaging, computational studies and solid state analysiscitations
- 2016A study on the AMACR catalysed elimination reaction and its application to inhibitor testingcitations
- 2015Hierarchical supramolecules and organization using boronic acid building blockscitations
- 2010N,N-Butyl-decamethylferrocenyl-amine reactivity at liquid vertical bar liquid interfaces: electrochemically driven anion transfer vs. pH driven proton transfercitations
Places of action
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article
A study on the AMACR catalysed elimination reaction and its application to inhibitor testing
Abstract
α-Methylacyl-CoA racemase (AMACR; P504S) catalysesa keystep in the degradation of branched-chain fatty acids and is important for the pharmacological activation of Ibuprofen and related drugs.Levels of the enzyme 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 elimination of HF from 3-fluoro-2-methylacyl-CoA substrates, and this reaction was investigated for use as an assay. Several known inhibitors and alternative substrates reduced substrate conversion by AMACR, as determined by 1H NMR. The greatest reduction of activity was observed for known potent inhibitors. A series of novel acyl-CoA esters with aromatic side chains were synthesised for testing as chromophoric substrates. These acyl-CoA esters were converted to unsaturated products by AMACR, but their use was limited by non-enzymatic elimination. Fluoridesensors were also investigated as a method of quantifying released fluoride and thus AMACR activity. These sensors generally suffered from high background signal and lacked reproducibility under the assay conditions. In summary, the elimination reaction can be used to characterise inhibitors, but it was not possible to develop a convenient colorimetric or fluorescent assay using 3-fluoro-2-methylacyl-CoA substrates.