Hansen's disease (HD), or leprosy, continues to be endemic in many parts of the world. Although multidrug therapy (MDT) is successful in curing a large number of patients, some of them abandon it because it is a long-term treatment. Therefore, identification of new drug targets in Mycobacterium leprae is considered of high importance. Here, we introduce an overview of in silico and in vitro studies that might be of help in this endeavor. The essentiality of M. leprae proteins is reviewed with discussion of flux balance analysis, gene expression, and knockout articles. Finally, druggability techniques are proposed for the validation of new M. leprae protein targets. Teaser: How to identify new therapeutic targets for leprosy with limited structural data for Mycobacterium leprae? A step-by-step approach with a combination of in silico and in vitro experiments.
BT - Drug discovery today C1 - https://www.ncbi.nlm.nih.gov/pubmed/33798649 DA - 03/2021 DO - 10.1016/j.drudis.2021.03.026 J2 - Drug Discov Today LA - eng N2 -Hansen's disease (HD), or leprosy, continues to be endemic in many parts of the world. Although multidrug therapy (MDT) is successful in curing a large number of patients, some of them abandon it because it is a long-term treatment. Therefore, identification of new drug targets in Mycobacterium leprae is considered of high importance. Here, we introduce an overview of in silico and in vitro studies that might be of help in this endeavor. The essentiality of M. leprae proteins is reviewed with discussion of flux balance analysis, gene expression, and knockout articles. Finally, druggability techniques are proposed for the validation of new M. leprae protein targets. Teaser: How to identify new therapeutic targets for leprosy with limited structural data for Mycobacterium leprae? A step-by-step approach with a combination of in silico and in vitro experiments.
PY - 2021 T2 - Drug discovery today TI - Strategies for drug target identification in Mycobacterium leprae. UR - https://www.sciencedirect.com/science/article/pii/S1359644621001616?via%3Dihub SN - 1878-5832 ER -