ArticleJournal of enzyme inhibition and medicinal chemistry2022
Acipimox inhibits human carbonic anhydrases.
Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 12 citations in OpenAlex.
- Covalent Targeting and Thermostabilization of Oncogenic R280K and R273H Mutants p53 by Small Molecule RVJB59.ChemMedChem · 2026Article
- Fragment-Derived Nicotinic Acid Analogues Inhibit hCA III and DownregulateBiomolecules · 2026Article
- Hidden targets in dermatology:Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Tetrazole Is a Novel Zinc Binder Chemotype for Carbonic Anhydrase Inhibition.ACS medicinal chemistry letters · 2025Article
- The Antiepileptic Drug Levetiracetam Inhibits Carbonic Anhydrase:ACS medicinal chemistry letters · 2024Article
- Structure based exploration of mitochondrial alpha carbonic anhydrase inhibitors as potential leads for anti-obesity drug development.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024Review
- Medicinal Chemistry of Drugs withJournal of medicinal chemistry · 2024Review
- Inhibition studies with simple and complex (in)organic anions of the γ-carbonic anhydrase fromJournal of enzyme inhibition and medicinal chemistry · 2023Article
- Natural Products-Pyrazine Hybrids: A Review of Developments in Medicinal Chemistry.Molecules (Basel, Switzerland) · 2023Review
- Small Structural Differences Govern the Carbonic Anhydrase II Inhibition Activity of Cytotoxic Triterpene Acetazolamide Conjugates.Molecules (Basel, Switzerland) · 2023Article
- Inhibition studies of the protozoan α-carbonic anhydrase fromJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities.Journal of enzyme inhibition and medicinal chemistry · 2022Review
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Authors and funding
2 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Acipimox, a nicotinic acid derivative in clinical use for the treatment of hyperlipidaemia, incorporates a free carboxylic acid and an N-oxide moiety, functionalities known to interact with the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) and inhibit its activity. Herein we report that acipimox acts as a low micromolar CA inhibitor (CAI) against most human (h) isoforms possessing catalytic activity, hCA I - XIV. By using computational techniques (docking and molecular dynamics simulations), we propose that acipimox coordinates through its carboxylate group to the zinc ion from the enzyme active site cavity, whereas the N-oxide group is hydrogen-bonded to the proton shuttle His residue in some isoforms (hCA I) or to active site Thr or Gln residues in other isoforms (hCA II, III, IV, VII, etc). As some CA isoforms are involved in lipogenesis, these data may be useful for the design of more effective CAIs with antiobesity activity.
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