ArticleThe Journal of pharmacology and experimental therapeutics2022
Is Diminazene an Angiotensin-Converting Enzyme 2 (ACE2) Activator? Experimental Evidence and Implications.
Article in The Journal of pharmacology and experimental therapeutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 5 citations in OpenAlex.
- Discovery of a pyridine-piperazine-based small molecule that enhances the activity of peptidase neurolysin.The Journal of pharmacology and experimental therapeutics · 2026Article
- The dual role of ACE2 in viral infections and neurodegeneration: mechanisms and therapeutic opportunities.Journal of neurovirology · 2025Review
- Molecular dissection of the role of ACE2 in glucose homeostasis.Physiological reviews · 2025Review
- The Missing Enzymes: A Call to Update Pharmacological Profiling Practices for Better Drug Safety Assessment.Journal of medicinal chemistry · 2025Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Antiprotozoal veterinary drug diminazene aceturate (DIZE) has been proposed to be an angiotensin-converting enzyme 2 (ACE2) activator. Since then, DIZE was used in dozens of experimental studies, but its mechanism of action attributed to ACE2 activation and enhanced formation of angiontensin-(1-7) [Ang-(1-7)] from Ang II was not carefully verified. The aim of this study was to confirm the effect of DIZE on catalytic activity of ACE2 and extend it to other peptidases involved in formation and degradation of Ang-(1-7). Concentration-dependent effect of DIZE on the initial rate of a fluorogenic substrate hydrolysis by human and mouse recombinant ACE2 was measured at assay conditions imitating that of the original report, but no activation of ACE2 was documented. Similar results were obtained with a more physiologically relevant assay buffer. In addition, DIZE did not affect activity of recombinant neprilysin, neurolysin, thimet oligopeptidase, and ACE. Efficiency of the fluorogenic substrate hydrolysis (V
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.