D M Brown, A G Netting, B K Chun, Y Choi, C K Chu, A M Gero
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引用次数: 15
摘要
D-coformycin的l -立体异构体类似物选择性地抑制恶性疟原虫腺苷脱氨酶(ADA)在皮摩尔范围内(L-isocoformycin, Ki 7 pM;L-coformycin, Ki 250 pM)。而l -核苷类似物、l -腺苷、2,6-二氨基-9-(l -核呋喃基)嘌呤和4-氨基-1-(l -核呋喃基)吡唑啉[3,4-d]-嘧啶被恶性疟原虫ADA选择性地脱胺，l -硫代氨基和l -硫代鸟苷则没有被选择性地脱胺。这是“非生理”l -核苷作为疟疾ADA的底物或抑制剂而不被哺乳动物ADA利用的第一个例子。
L-nucleoside analogues as potential antimalarials that selectively target Plasmodium falciparum adenosine deaminase.
The L-stereoisomer analogues of D-coformycin selectively inhibited P. falciparum adenosine deaminase (ADA) in the picomolar range (L-isocoformycin, Ki 7 pM; L-coformycin, Ki 250 pM). While the L-nucleoside analogues, L-adenosine, 2,6-diamino-9-(L-ribofuranosyl)purine and 4-amino-1-(L-ribofuranosyl)pyrazolo[3,4-d]-pyrimidine were selectively deaminated by P. falciparum ADA, L-thioinosine and L-thioguanosine were not. This is the first example of 'non-physiological' L-nucleosides that serve as either substrates or inhibitors of malarial ADA and are not utilised by mammalian ADA.
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