标题:Update on Recent Developments in Small Molecular HIV-1 RNase H Inhibitors (2013-2016): Opportunities and Challenges
作者:Wang, Xueshun; Gao, Ping; Menendez-Arias, Luis; Liu, Xinyong; Zhan, Peng
作者机构:[Wang, Xueshun; Gao, Ping; Liu, Xinyong; Zhan, Peng] Shandong Univ, Minist Educ, Sch Pharmaceut Sci, Key Lab Chem Biol,Dept Med Chem, 44 West Culture 更多
通讯作者:Liu, XY;Zhan, P
通讯作者地址:[Liu, XY; Zhan, P]Shandong Univ, Minist Educ, Sch Pharmaceut Sci, Key Lab Chem Biol,Dept Med Chem, 44 West Culture Rd, Jinan 250012, Shandong, Peoples 更多
来源:CURRENT MEDICINAL CHEMISTRY
出版年:2018
卷:25
期:14
页码:1682-1702
DOI:10.2174/0929867324666170113110839
关键词:AIDS; HIV-1; RNase H inhibitors; dual inhibitors; drug design; SAR;; antiviral; metalloenzyme
摘要:Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority. The ribonuclease H (RNase H) activity of the HIV-1 reverse transcriptase catalyzes the selective hydrolysis of the RNA strand of RNA: DNA heteroduplex replication intermediates, and represents an attractive unexploited target for drug development. This review reports on recent progress in the characterization of HIV-1 RNase H inhibitors from 2013 to 2016, describing their chemical structures, structureactivity relationship and binding modes. Focus is given to emerging medicinal chemistry principles and insights into the discovery and development of RNase H inhibitors.
收录类别:SCOPUS;SCIE
Scopus被引频次:1
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85048810247&doi=10.2174%2f0929867324666170113110839&partnerID=40&md5=c101cc40a4825661e789fd315cdd13b0
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