Abstract:
:Emergence of drug-resistant viral strains is one of the major milestones and the main cause for the failure of antiretroviral therapy. Combination of different anti-HIV agents has become the standard clinical practice to keep the viral load at low or even undetectable levels and to prevent emergence of virus-drug resistance. Among the human immunodeficiency virus (HIV) reverse transcriptase (RT) inhibitors, the so called nonnucleoside RT inhibitors (NNRTIs) have gained a definitive place in the treatment of HIV infections in combination with nucleoside analogue RT inhibitors (NRTIs) and HIV protease inhibitors (PIs). The virus can be markedly suppressed for a relatively long period of time when exposed to multiple drug combination therapy (highly active antiretroviral therapy, HAART). TSAO derivatives are a peculiar group of highly functionalized nucleosides that belong to the so-called nonnucleoside RT inhibitors (NNRTIs). They exert their unique selectivity for HIV-1 through a specific interaction with the p51 subunit of HIV-1 RT. They are the first small molecules that seem to interfere with the dimerization process of the enzyme. This review covers the work carried out with this unique class of specific inhibitors of HIV-1 reverse transcriptase, including structure activity relationship studies (SAR), its mechanism of action, resistance studies, model of interaction with the enzyme, etc.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Camarasa MJ,San-Félix A,Velázquez S,Pérez-Pérez MJ,Gago F,Balzarini Jdoi
10.2174/1568026043388600keywords:
subject
Has Abstractpub_date
2004-01-01 00:00:00pages
945-63issue
9eissn
1568-0266issn
1873-4294journal_volume
4pub_type
杂志文章,评审abstract::The problem in this work is the computational characterization of cyclodextrins, crown ethers and hyaluronan (HA) as hosts of inclusion complexes for nanosized drug delivery vehicles in pharmaceutical formulations. The difficulty is addressed through a computational study of some thermodynamic, geometric and topologic...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1568026615666150506145619
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pub_type: 杂志文章,评审
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/156802607782194671
更新日期:2007-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026615666150413153717
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pub_type: 杂志文章,评审
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026053828394
更新日期:2005-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2001-09-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1568026611313050002
更新日期:2013-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,meta分析,评审
doi:10.2174/156802612805289917
更新日期:2012-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1568026619666191121123926
更新日期:2020-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802612802652466
更新日期:2012-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/15680266113136660185
更新日期:2013-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802612799078919
更新日期:2012-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802607780487623
更新日期:2007-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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journal_title:Current topics in medicinal chemistry
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journal_title:Current topics in medicinal chemistry
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doi:10.2174/1568026614666140506124442
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abstract:: ...
journal_title:Current topics in medicinal chemistry
pub_type: 社论
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2019-01-01 00:00:00
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journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/156802612800166800
更新日期:2012-01-01 00:00:00
abstract::Protein kinases (Ser/Thr and Tyr) play a key role in signal transduction pathways. It has been shown that deregulation of the Cdk activity is linked to cell proliferation and cancer. Inhibition of cyclin-dependent kinases (Cdks) is an important target for potential new anti-cancer drugs. Following the discovery of Olo...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2002-09-01 00:00:00
abstract::The serotonin receptor subtype 5 HT(1A) was one of the first serotonin receptor subtypes pharmacologically characterized. Over the last twenty years the 5 HT(1A) receptor has been the object of intense research efforts as witnessed by the 5 HT(1A) acting drugs marketed as anxiolytics. In recent years, several new chem...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2008-01-01 00:00:00
abstract::Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章
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更新日期:2016-01-01 00:00:00
abstract::Recent advances in DNA microarray technology have great impact on many areas of biomedical research and pharmacogenomics: discovering novel targets and genes, elucidating signatures of complex diseases, transcriptional profiling of models for diseases, and the development of individually optimized drugs based on diffe...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2004-01-01 00:00:00
abstract::Compared with the increasing and widespread bacterial resistance to clinical medicines and the urgent need for cures of intractable diseases, there is a dramatic decline in the numbers of drugs reaching the market or clinical trials. Accordingly, it has become imperative to discover more rational and efficient strateg...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2016-01-01 00:00:00
abstract::The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...
journal_title:Current topics in medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2013-01-01 00:00:00