Novel thiadiazole inhibitors of human carbonic anhydrases
نویسندگان
چکیده
منابع مشابه
Human Carbonic Anhydrases
Sequence studies of human erythrocyte carbonic anhydrase B show that it contains 256 residues. A series of relatively small peptides soluble in aqueous solutions obtained by chymotryptic and tryptic digestion of the enzyme, large peptides containing only COOH-terminal lysine or arginine as well as those resulting from more limited cleavage of the enzyme, and cyanogen bromide cleavage products s...
متن کامل4-amino-substituted benzenesulfonamides as inhibitors of human carbonic anhydrases.
A series of N-aryl-β-alanine derivatives and diazobenzenesulfonamides containing aliphatic rings were designed, synthesized, and their binding to carbonic anhydrases (CA) I, II, VI, VII, XII, and XIII was studied by the fluorescent thermal shift assay and isothermal titration calorimetry. The results showed that 4-substituted diazobenzenesulfonamides were more potent CA binders than N-aryl-β-al...
متن کاملAcid Difference Spectra of Human Carbonic Anhydrases.
Human carbonic anhydrase B loses enzymatic activity as it undergoes an irreversible conformational change near pH 4 (1). Riddiford (2) further found that seven of the eleven histidyl groups, which are unreactive in the native protein, become titratable during this change. Also, five or six of the eight tyrosyl groups do not ionize freely and reversibly in the native protein (2, 3). Human carbon...
متن کاملTransport metabolons with carbonic anhydrases
THE CONCEPT OF THE TRANSPORT METABOLON A metabolon has been defined as a “temporary, structural-functional, supramolecular complex of sequential metabolic enzymes and cellular structural elements, in which metabolites are passed from one active site to another without complete equilibration with the bulk cellular fluids” (Srere, 1985, 1987). This substrate channeling should decrease transit tim...
متن کاملBacterial Carbonic Anhydrases as Drug Targets: Toward Novel Antibiotics?
Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes which catalyze the hydration of carbon dioxide to bicarbonate and protons. Many pathogenic bacteria encode such enzymes belonging to the α-, β-, and/or γ-CA families. In the last decade, the α-CAs from Neisseria spp. and Helicobacter pylori as well as the β-class enzymes from Escherichia coli, H. pylori,Mycobacterium tuberculosis, Brucell...
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ژورنال
عنوان ژورنال: Acta Crystallographica Section A Foundations of Crystallography
سال: 2008
ISSN: 0108-7673
DOI: 10.1107/s0108767308088867