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Novel Inhibitors Of Mycobacterium Tuberculosis Complex Cytochrome P450 Cyp121


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The present invention relates to the identification of the cyclodipeptide cyclo(L-Tyr-L-Tyr) as substrate of CYP121 from Mycobacterium tuberculosis, to the crystal structures of CYP121 complexed either with cyclo(L-Tyr-L-Tyr) or with other cyclodipeptides, to the use of these structures in rational drug design methods to generate cyclodipeptide-based molecules that could inhibit CYP121 activity, and to the design of new anti- Mycobacterium tuberculosis agents based on the DKP scaffold.


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