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Different roles for the acyl chain and the amine leaving group in the substrate selectivity of N-Acylethanolamine acid amidase

Andrea Ghidini, Laura Scalvini, Francesca Palese, Alessio Lodola, Marco Mor, Daniele Piomelli. J Enzyme Inhib Med Chem. 2021 Dec;36(1):1411-1423.

Laboratory studyOther animals

Design
Laboratory study
Subjects
Enzyme assays and molecular dynamics simulations; no animals or people
Dose used in the study
Not applicable; substrates were tested against the NAAA enzyme in vitro
Duration
Not stated in the abstract
What was measured
Catalytic efficiency of NAAA, the enzyme that breaks down palmitoylethanolamide, against fatty acid ethanolamides with different acyl chain lengths and polar head groups, matched to modelled enzyme-substrate stability.

What the authors reported

Catalytic efficiency depended strictly on fatty acyl chain length in both saturated and monounsaturated substrates, while the enzyme tolerated a wider range of polar head changes. This matched the stability of enzyme-substrate complexes in simulations.

Limits of this study

An enzyme and computer-modelling study; it cannot show any effect in people or animals treated in practice. Two authors are inventors on patents covering NAAA inhibitors.

Source

PubMed 34256657 · doi:10.1080/14756366.2021.1912035

Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.