Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design

…, S Suresh, FS Buckner, WC Van Voorhis…

文献索引：Bressi; Verlinde; Aronov; Shaw; Shin; Nguyen; Suresh; Buckner; van Voorhis; Kuntz; Hol; Gelb Journal of Medicinal Chemistry, 2001 , vol. 44, # 13 p. 2080 - 2093

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被引用次数: 109

摘要

In our continuation of the structure-based design of anti-trypanosomatid drugs, parasite- selective adenosine analogues were identified as low micromolar inhibitors of glyceraldehyde-3-phosphate dehydrogenase (GAPDH). Crystal structures of Trypanosoma brucei, Trypanosoma cruzi, Leishmania mexicana, and human GAPDH's provided details of how the adenosyl moiety of NAD+ interacts with the proteins, and this facilitated the ...