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Discovery of Mycobacterium Tuberculosis Protein Tyrosine Phosphatase A (MptpA) Inhibitors Based on Natural Products and a Fragment‐Based Approach
Author(s) -
Manger Michael,
Scheck Michael,
Prinz Heino,
von Kries Jens Peter,
Langer Thomas,
Saxena Krishna,
Schwalbe Harald,
Fürstner Alois,
Rademann Jörg,
Waldmann Herbert
Publication year - 2005
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200500171
Subject(s) - fragment (logic) , mycobacterium tuberculosis , protein tyrosine phosphatase , phosphatase , computational biology , tuberculosis , tyrosine , biochemistry , biology , chemistry , enzyme , computer science , algorithm , medicine , pathology
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.