Discovery of Mycobacterium Tuberculosis Protein Tyrosine Phosphatase A (MptpA) Inhibitors Based on Natural Products and a Fragment-Based Approach

Naturally inspired or fragment based. Mcyobacterium tuberculosis has two functional phosphatases, protein tyrosine phosphates A and B (MptpA and B), which are thought to mediate mycobacterial survival in the host. Here we describe the first inhibitors of MptpA (see scheme). Initial hits were identif...

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Veröffentlicht in:Chembiochem : a European journal of chemical biology 2005-10, Vol.6 (10), p.1749-1753
Hauptverfasser: Manger, Michael, Scheck, Michael, Prinz, Heino, von Kries, Jens Peter, Langer, Thomas, Saxena, Krishna, Schwalbe, Harald, Fürstner, Alois, Rademann, Jörg, Waldmann, Herbert
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Sprache:eng
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Zusammenfassung:Naturally inspired or fragment based. Mcyobacterium tuberculosis has two functional phosphatases, protein tyrosine phosphates A and B (MptpA and B), which are thought to mediate mycobacterial survival in the host. Here we describe the first inhibitors of MptpA (see scheme). Initial hits were identified in screening collections that were inspired by natural products and composed by fragment‐based approach.
ISSN:1439-4227
1439-7633
1439-4227
DOI:10.1002/cbic.200500171