Insights into the Design of Inhibitors of the Urease Enzyme - A Major Target for the Treatment of Helicobacter pylori Infections
| Autor: | Ana Thereza Fiori-Duarte, Rodrigo Rezende Kitagawa, Daniel Fábio Kawano, Ricardo Pereira Rodrigues |
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| Rok vydání: | 2018 |
| Předmět: |
Urease
medicine.drug_class Gastrointestinal Diseases Antibiotics Context (language use) 01 natural sciences Biochemistry Virulence factor Microbiology Helicobacter Infections 03 medical and health sciences Antibiotic resistance Drug Discovery medicine Humans Enzyme Inhibitors 030304 developmental biology Pharmacology chemistry.chemical_classification 0303 health sciences biology Helicobacter pylori 010405 organic chemistry Organic Chemistry biology.organism_classification 0104 chemical sciences Anti-Bacterial Agents Enzyme chemistry biology.protein Molecular Medicine Bacteria |
| Zdroj: | Current medicinal chemistry. 27(23) |
| ISSN: | 1875-533X |
| Popis: | Expressed by a variety of plants, fungi and bacteria, the urease enzyme is directly associated with the virulence factor of many bacteria, including Helicobacter pylori, a gram-negative bacterium related to several gastrointestinal diseases and responsible for one of the most frequent bacterial infections throughout the world. The Helicobacter pylori Urease (HPU) is a nickel-dependent metalloenzyme expressed in response to the environmental stress caused by the acidic pH of the stomach. The enzyme promotes the increase of gastric pH through acid neutralization by the products of urea hydrolysis, then critically contributing to the colonization and pathogenesis of the microorganism. At the same time, standard treatments for Helicobacter pylori infections have limitations such as the increasing bacterial resistance to the antibiotics used in the clinical practice. As a strategy for the development of novel treatments, urease inhibitors have proved to be promising, with a wide range of chemical compounds, including natural, synthetic and semisynthetic products to be researched and potentially developed as new drugs. In this context, this review highlights the advances in the field of HPU inhibition, presenting and discussing the basis for the research of new molecules aiming at the identification of more efficient therapeutic entities. |
| Databáze: | OpenAIRE |
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