Ribonuclease A Inhibition by Carboxymethylsulfonyl-Modified Xylo-and Arabinopyrimidines
Ribonuclease A Inhibition by Carboxymethylsulfonyl-Modified Xylo-and Arabinopyrimidines
复制标题
DOI：
10.1002/cmdc.201402179
复制
发表时间：
2014-09-01
期刊：
影响因子：
3.4
通讯作者：
Pathak, Tanmaya
中科院分区：
文献类型：
--
作者：
Datta, Dhrubajyoti;Dasgupta, Swagata;Pathak, Tanmaya
合成了一组酸性核苷类化合物以开发一类新的核糖核酸酶A（RNase A）抑制剂。我们最近对羧甲基磺酰基修饰的核苷的研究揭示了一些有趣的RNase A抑制结果。这一积极的结果引发了对二级糖羟基在抑制RNA酶A活性中所起作用的研究。在2 ′-和3 ′-位上用-SO_2CH_2COOH基团修饰的尿苷和胞苷显示出良好的抑制特性，抑制常数（Ki）值在109-17 mm范围内。
A group of acidic nucleosides were synthesized to develop a new class of ribonuclease A (RNase A) inhibitors. Our recent study on carboxymethylsulfonyl-modified nucleosides revealed some interesting results in RNase A inhibition. This positive outcome triggered an investigation of the role played by secondary sugar hydroxy groups in inhibiting RNase A activity. Uri-dines and cytidines modified with -SO2CH2COOH groups at the 2'-and 3'-positions show good inhibitory properties with low inhibition constant (Ki) values in the range of 109-17 mm. The present work resulted in a set of inhibitors that undergo more effective interactions with the RNase A active site, as visualized by docking studies.