Bibliographic Details
| Title: |
New Insights into Conformationally Restricted Carbonic Anhydrase Inhibitors |
| Authors: |
Jacob Combs, Murat Bozdag, Lochlin D. Cravey, Anusha Kota, Robert McKenna, Andrea Angeli, Fabrizio Carta, Claudiu T. Supuran |
| Source: |
Molecules, Vol 28, Iss 2, p 890 (2023) |
| Publisher Information: |
MDPI AG, 2023. |
| Publication Year: |
2023 |
| Collection: |
LCC:Organic chemistry |
| Subject Terms: |
X-ray crystallography, carbonic anhydrase IX, structure activity relationships, Organic chemistry, QD241-441 |
| More Details: |
This paper reports an investigation into the impact of pyridyl functional groups in conjunction with hydroxide-substituted benzenesulfonamides on the inhibition of human carbonic anhydrase (CA; EC 4.2.1.1) enzymes. These compounds were tested in vitro of CA II and CA IX, two physiologically important CA isoforms. The most potent inhibitory molecules against CA IX, 3g, 3h, and 3k, were studied to understand their binding modes via X-ray crystallography in adduct with CA II and CA IX-mimic. This research further adds to the field of CA inhibitors to better understand ligand selectivity between isoforms found in humans. |
| Document Type: |
article |
| File Description: |
electronic resource |
| Language: |
English |
| ISSN: |
1420-3049 |
| Relation: |
https://www.mdpi.com/1420-3049/28/2/890; https://doaj.org/toc/1420-3049 |
| DOI: |
10.3390/molecules28020890 |
| Access URL: |
https://doaj.org/article/d56a5514d26a4d64a108c5634632f7d5 |
| Accession Number: |
edsdoj.56a5514d26a4d64a108c5634632f7d5 |
| Database: |
Directory of Open Access Journals |
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