Benzylaminoethylureido‐Tailed Benzenesulfonamides Show Potent Inhibitory Activity against Bacterial Carbonic Anhydrases
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DOI: 10.1002/cmdc.202000680
Abstract: A series of benzylaminoethylureido‐tailed benzenesulfonamides was analyzed for their inhibition potential against bacterial carbonic anhydrases (CAs) such as VhCA α, β, and γ from Vibrio cholerae, and BpsCA β and γ‐CAs from Burkholderia pseudomallei. Growing… read more here.
Keywords: tailed benzenesulfonamides; benzylaminoethylureido tailed; carbonic anhydrases; bacterial carbonic ... See more keywords
Carbonic Anhydrases II, IX, and XII in Reflux Esophagitis
Sign Up to like & getrecommendations! Published in 2021 at "Digestive Diseases and Sciences"
DOI: 10.1007/s10620-021-06985-5
Abstract: The pathogenesis of gastroesophageal reflux disease (GERD) has not been resolved in detail. Esophageal epithelial cells provide resistance to acidic reflux via several mechanisms, many of which involve buffering acid with bicarbonate and transporting protons.… read more here.
Keywords: caxii; reflux; squamous epithelium; carbonic anhydrases ... See more keywords
New insights into the selective inhibition of the β-carbonic anhydrases of pathogenic bacteria Burkholderia pseudomallei and Francisella tularensis: a proteochemometrics study
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Diversity"
DOI: 10.1007/s11030-018-9869-5
Abstract: Nowadays, antibiotic resistance has turned into one of the most important worldwide health problems. Biological end point of critical enzymes induced by potent inhibitors is recently being considered as a highly effective and popular strategy… read more here.
Keywords: carbonic anhydrase; carbonic anhydrases; selective inhibition; insights selective ... See more keywords
Extending the γ-class carbonic anhydrases inhibition profiles with phenolic compounds.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103336
Abstract: γ-Class carbonic anhydrases (CAs; EC 4.2.1.1) lack of extended inhibition characterization in comparison to α- and β-class isozymes. For this reason, a panel of 22 phenols was investigated here for the inhibition of the γ-CAs… read more here.
Keywords: class; carbonic anhydrases; inhibition; extending class ... See more keywords
Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.11.061
Abstract: Coumarin derivatives are a peculiar class of inhibitors of the family of metalloenzymes carbonic anhydrases (CA, EC 4.2.1.1). Several coumarins display higher affinity and selectivity toward most relevant and druggable CA isoforms. By decorating the… read more here.
Keywords: coumarin based; coumarin; series coumarin; carbonic anhydrases ... See more keywords
The structural basis of the low catalytic activities of the two minor β-carbonic anhydrases of the filamentous fungus Aspergillus fumigatus.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of structural biology"
DOI: 10.1016/j.jsb.2019.07.011
Abstract: The β -carbonic anhydrases (β -CAs) are widely distributed zinc-metalloenzymes that play essential roles in growth, survival, development and virulence in fungi. The majority of filamentous ascomycetes possess multiple β -CA isoforms among which major… read more here.
Keywords: structural basis; aspergillus fumigatus; zinc; carbonic anhydrases ... See more keywords
Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.0c00733
Abstract: The “tail approach” has become a milestone in human carbonic anhydrase inhibitor (hCAI) design for various therapeutics, including antiglaucoma agents. Besides the classical hydrophobic/hydrophilic division of hCAs active site, several subpockets have been identified at… read more here.
Keywords: human carbonic; inhibitors human; carbonic anhydrases; sulfonamide inhibitors ... See more keywords
Development of Hydrogen Sulfide-Releasing Carbonic Anhydrases IX- and XII-Selective Inhibitors with Enhanced Antihyperalgesic Action in a Rat Model of Arthritis
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00982
Abstract: An effective therapeutic approach based on the anti-inflammatory action of hydrogen sulfide (H2S) and inhibition of carbonic anhydrases (CAs) IX and XII is proposed here for the management of arthritis. H2S is a human gasotransmitter… read more here.
Keywords: carbonic anhydrases; arthritis; enhanced antihyperalgesic; rat model ... See more keywords
4-(Pyrazolyl)benzenesulfonamide Ureas as Carbonic Anhydrases Inhibitors and Hypoxia-Mediated Chemo-Sensitizing Agents in Colorectal Cancer Cells
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.4c01894
Abstract: Hypoxia in tumors contributes to chemotherapy resistance, worsened by acidosis driven by carbonic anhydrases (hCA IX and XII). Targeting these enzymes can mitigate acidosis, thus enhancing tumor sensitivity to cytotoxic drugs. Herein, novel 4-(pyrazolyl)benzenesulfonamide ureas… read more here.
Keywords: colorectal cancer; cancer cells; hca xii; carbonic anhydrases ... See more keywords
Protein-Labeling Fluorescent Probe Reveals Ectodomain Shedding of Transmembrane Carbonic Anhydrases.
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DOI: 10.1021/acschembio.2c00679
Abstract: Ectodomain shedding is a form of limited proteolysis in which a protease cleaves a transmembrane protein, releasing the extracellular domain from the cell surface. Cells use this process to regulate a wide variety of biological… read more here.
Keywords: protein labeling; ectodomain shedding; carbonic anhydrases; cell surface ... See more keywords
Exploring the Polypharmacological Potential of PCI-27483: A Selective Inhibitor of Carbonic Anhydrases IX and XII.
Sign Up to like & getrecommendations! Published in 2024 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.4c00443
Abstract: PCI-27483, originally developed as a potent and selective inhibitor of the serine protease Factor VIIa (FVIIa) in complex with tissue factor (TF), has demonstrated significant promise in cancer therapy. In addition to its primary mechanism… read more here.
Keywords: polypharmacological potential; pci 27483; carbonic anhydrases; selective inhibitor ... See more keywords