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Article Dans Une Revue Mini-Reviews in Medicinal Chemistry Année : 2021

An Update on Arginase Inhibitors and Inhibitory Assays

Jason Muller
Rym Attia
Andy Zedet
Corine Girard

Résumé

Abstract: Arginase, which converts arginine into ornithine and urea, is a promising therapeutic target. Arginase is involved in cardiovascular diseases, parasitic infections and, through a critical role in immunity, in some cancers. There is a need to develop effective arginase inhibitors and therefore efforts to identify and optimize new inhibitors are increasing. Several methods of evaluating arginase activity are available, but few directly measure the product. Radiometric assays need to separate urea and dying reactions require acidic conditions and sometimes heating. Hence, there are a variety of different approaches available, and each approach has its own limits and benefits. In this review, we provide an update on arginase inhibitors, followed by a discussion on available arginase assays and alternative methods, with a focus on the intrinsic biases and parameters that are likely to impact results.

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Chimie
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Dates et versions

hal-03581420 , version 1 (19-02-2022)

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Citer

Jason Muller, Rym Attia, Andy Zedet, Corine Girard, M. Pudlo. An Update on Arginase Inhibitors and Inhibitory Assays. Mini-Reviews in Medicinal Chemistry, 2021, 22, ⟨10.2174/1389557522666211229105703⟩. ⟨hal-03581420⟩

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