Targeting the serine pathway:a promising approach against tuberculosis?
| العنوان: | Targeting the serine pathway:a promising approach against tuberculosis? |
|---|---|
| المؤلفون: | Marie Haufroid, Johan Wouters |
| المصدر: | Haufroid, M & Wouters, J 2019, ' Targeting the serine pathway : a promising approach against tuberculosis? ', Pharmaceuticals, vol. 12, no. 2, 66 . https://doi.org/10.3390/ph12020066 Pharmaceuticals Pharmaceuticals, Vol 12, Iss 2, p 66 (2019) |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | 0301 basic medicine, Opinion, phosphoserine aminotransferase, Tuberculosis, Pharmaceutical Science, lcsh:Medicine, lcsh:RS1-441, SerA1, Sequence alignment, Computational biology, Selective inhibition, Serine, lcsh:Pharmacy and materia medica, phosphoserine phosphatase, 03 medical and health sciences, Drug Discovery, Medicine, Phosphoglycerate dehydrogenase, chemistry.chemical_classification, 030102 biochemistry & molecular biology, business.industry, Drug discovery, lcsh:R, HAD, SerB2, phosphoglycerate dehydrogenase, medicine.disease, Clinical trial, 030104 developmental biology, Enzyme, chemistry, tuberculosis, SerC, Molecular Medicine, Phosphoserine aminotransferase, Phosphoserine phosphatase, business, Infectious agent |
| الوصف: | Tuberculosis is still the leading cause of death by a single infectious agent. Effective chemotherapy has been used and improved since the 1950s, but strains resistant to this therapy and most antibacterial drugs on the market are emerging. Only 10 new drugs are in clinical trials, and two of them have already demonstrated resistance. This paper gives an overview of current treatment options against tuberculosis and points out a promising approach of discovering new effective drugs. The serine production pathway is composed of three enzymes (SerA1, SerC and SerB2), which are considered essential for bacterial growth, and all of them are considered as a therapeutic drug target. Their crystal structure are described and essential regulatory domains pointed out. Sequence alignment with similar enzymes in other host would help to identify key residues to target in order to achieve selective inhibition. Currently, only inhibitors of SerB2 are described in the literature. However, inhibitors of human enzymes are discussed, and could be used as a good starting point for a drug discovery program. The aim of this paper is to give some guidance for the design of new hits for every enzyme in this pathway. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec08e8f800b89035911bc56c12f0f073 https://pure.unamur.be/ws/files/40741849/pharmaceuticals_12_00066_v3.pdf |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....ec08e8f800b89035911bc56c12f0f073 |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |