Specificity of adenosine deaminase inhibitors.
Specificity of adenosine deaminase inhibitors.
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DOI：
10.1016/0006-2952(77)90003-x
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发表时间：
1977-11
影响因子：
5.8
通讯作者：
J. Henderson;L. Brox;G. Zombor;D. Hunting;C. A. Lomax
中科院分区：
文献类型：
--
作者：
J. Henderson;L. Brox;G. Zombor;D. Hunting;C. A. Lomax
腺苷脱氨酶抑制剂脱氧共形霉素（covidarabine）、共形霉素和赤霉素-9-（2-羟基-3-壬基）腺嘌呤（EHNA）的特异性已在体外埃利希腹水瘤细胞和培养的小鼠淋巴瘤L5178 Y细胞中进行了评估。EHNA作为腺苷脱氨酶抑制剂的效力低于脱氧coformycin，并且特异性较低。高浓度的脱氧共形霉素和EHNA抑制嘌呤核苷酸合成的所有途径，并抑制肌苷酸转化为腺嘌呤和鸟嘌呤核苷酸。这些药物也抑制纯化的腺苷酸脱氨酶，但在完整细胞中这种酶的抑制只能在腺苷酸的高脱氨率下检测到。脱氧考福霉素增强腺嘌呤对培养细胞的毒性。
The specificity of the potent adenosine deaminase inhibitors deoxycoformycin (covidarabine), coformycin anderythro-9-(2-hydroxy-3-nonyl)adenine (EHNA), has been assessed in Ehrlich ascites tumor cellsin vitroand in cultured mouse lymphoma L5178Y cells. EHNA is both less potent an inhibitor of adenosine deaminase than deoxycoformycin, and is less specific. High concentrations of deoxycoformycin and EHNA inhibit all pathways of purine ribonucleotide synthesis, and inhibit the conversion of inosinate to adenine and guanine nucleotides. These drugs also inhibit purified adenylate deaminase, but inhibition of this enzyme in intact cells can only be detected at high rates of deamination of adenylate. Deoxycoformycin potentiates the toxicity of adenine against cultured cells.