Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase
Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase
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DOI：
10.1021/jm034206x
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发表时间：
2004-01-01
影响因子：
7.3
通讯作者：
Fazal, G
中科院分区：
文献类型：
--
作者：
Faucher, AM;White, PW;Fazal, G
对勃林格殷格翰公司的化合物系列进行筛选，以抑制人乳头瘤病毒El解旋酶atp酶活性，从而开发出抑制人乳头瘤病毒（HPV） DNA复制的抗病毒药物。通过筛选发现（联苯-4-磺酰基）乙酸1，能抑制HPV 6型E1解旋酶的atp酶活性，IC50值较低。一个触碰铅的练习迅速转化为低纳摩尔铅系列。
The Boehringer Ingelheim compound collection was screened for inhibitors of the ATPase activity of human papillomavirus El helicase to develop antiviral agents that inhibit human papillomavirus (HPV) DNA replication. This screen led to the discovery of (biphenyl-4-sulfonyl)acetic acid 1, which inhibits the ATPase activity of HPV type 6 E1 helicase with a low micromolar IC50 value. A hit-to-lead exercise rapidly converted 1 into a low nanomolar lead series.