Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis
| العنوان: | Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis |
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| المؤلفون: | Mange Ram Yadav, Rupesh V. Chikhale, Prashant R. Murumkar, Mahesh A. Barmade |
| المصدر: | Journal of Medicinal Chemistry. 61:8563-8593 |
| بيانات النشر: | American Chemical Society (ACS), 2018. |
| سنة النشر: | 2018 |
| مصطلحات موضوعية: | 0301 basic medicine, High-throughput screening, 030106 microbiology, Antitubercular Agents, Druggability, 03 medical and health sciences, Bacterial Proteins, Drug Development, Arabinogalactan, Drug Discovery, Humans, Tuberculosis, chemistry.chemical_classification, Lipoarabinomannan, biology, Chemistry, Mycobacterium tuberculosis, Ligand (biochemistry), biology.organism_classification, Alcohol Oxidoreductases, 030104 developmental biology, Enzyme, Drug development, Biochemistry, Molecular Medicine, Mycobacterium |
| الوصف: | Decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It was first reported as a druggable target on the basis of inhibitors discovered in high throughput screening of a drug library. Since then, inhibitors with different types of chemical scaffolds have been reported for their activity against this enzyme. Formation of a covalent or noncovalent bond by the interacting ligand with the enzyme causes loss of its catalytic activity which ultimately leads to the death of the mycobacterium. This Perspective describes various DprE1 inhibitors as anti-TB agents reported to date. |
| تدمد: | 1520-4804 0022-2623 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f695ce793f0b728170ebec1f2d311b31Test https://doi.org/10.1021/acs.jmedchem.8b00281Test |
| رقم الانضمام: | edsair.doi.dedup.....f695ce793f0b728170ebec1f2d311b31 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204804 00222623 |
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