ArticleJournal of enzyme inhibition and medicinal chemistry2018
Nitroimidazole-based inhibitors DTP338 and DTP348 are safe for zebrafish embryos and efficiently inhibit the activity of human CA IX in Xenopus oocytes.
Article in Journal of enzyme inhibition and medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 20 citations in OpenAlex.
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- Anti-Tumor Active Isopropylated Fused Azaisocytosine-Containing Congeners Are Safe for DevelopingMolecules (Basel, Switzerland) · 2022Article
- Carbonic anhydrase inhibitor induces otic hair cell apoptosis via an intrinsic pathway and ER stress in zebrafish larvae.Toxicology reports · 2021Article
- Article
- Design, synthesis,Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Toxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Visible Light Mediated Bidirectional Control over Carbonic Anhydrase Activity in Cells andJournal of the American Chemical Society · 2020Article
- Hypoxia-Activated Prodrug Derivatives of Carbonic Anhydrase Inhibitors in Benzenesulfonamide Series: Synthesis and Biological Evaluation.Molecules (Basel, Switzerland) · 2020Article
- Experimental Carbonic Anhydrase Inhibitors for the Treatment of Hypoxic Tumors.Journal of experimental pharmacology · 2020Review
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Authors and funding
12 authors at 5 institutions in 5 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Carbonic anhydrase (CA) IX is a hypoxia inducible enzyme that is highly expressed in solid tumours. Therefore, it has been considered as an anticancer target using specific chemical inhibitors. The nitroimidazoles DTP338 and DTP348 have been shown to inhibit CA IX in nanomolar range in vitro and reduce extracellular acidification in hypoxia, and impair tumour growth. We screened these compounds for toxicity using zebrafish embryos and measured their in vivo effects on human CA IX in Xenopus oocytes. In the toxicity screening, the LD
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