8cdx

Human carbonic anhydrase I complexed with 4-(3-ethylureido)benzenesulfonamide

spinqualitylabelsall models 8cdx, resolution 1.33Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 8cdx is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.335Å Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function CAH1_HUMAN Reversible hydration of carbon dioxide. Can hydrates cyanamide to urea. Publication Abstract from PubMed Sulfonamides remain an important class of drugs, especially because of their inhibitory effects on carbonic anhydrases. Herein, we have synthesized several sulfonamides and tested them for their inhibitory activity against carbonic anhydrases hCA I, hCA II, hCA IX, and hCA XII, respectively. Thereby, biphenyl- and benzylphenyl-substituted sulfonamides showed high selectivity against hCA IX and hCA XII; these enzymes are common targets in the treatment of hypoxic cancers, and noteworthy inhibitory activity was observed for several compounds toward hCA I that might be of interest for future applications to treat cerebral edema. Compound 3 (4-[3-(2-benzylphenyl)ureido]benzenesulfonamide) held an exceptionally low K(i) value of 1.0 nM for hCA XII. Ureidobenzenesulfonamides as Selective Carbonic Anhydrase I, IX, and XII Inhibitors.,Denner TC, Angeli A, Ferraroni M, Supuran CT, Csuk R Molecules. 2023 Nov 26;28(23):7782. doi: 10.3390/molecules28237782. PMID:38067512 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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