Targeting tuberculosis using structure guided fragment based drug design

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Fragment-based drug discovery has produced a number of potent inhibitors against multiple tuberculosis targets. Here, we review the successes, opportunities and challenges of this approach in tuberculosis drug discovery.

Fragment-based drug discovery is now widely used in academia and industry to obtain small molecule inhibitors for a given target and is established for many fields of research including antimicrobials and oncology. Many molecules derived from fragment-based approaches are already in clinical trials and two – vemurafenib and venetoclax – are on the market, but the approach has been used sparsely in the

tuberculosis field. Here, we describe the progress of our group and others, and examine the most recent successes and challenges in developing compounds with antimycobacterial activity.

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