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Multimodal Functionalities of HIV-1 Integrase
Viruses, 2022 Integrase is the retroviral protein responsible for integrating reverse transcripts into cellular genomes. Co-packaged with viral RNA and reverse transcriptase into capsid-encased viral cores, human immunodeficiency virus 1 (HIV-1) integrase has long been implicated in reverse transcription and virion maturation.
Alan N. Engelman, Mamuka Kvaratskhelia
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Pharmacology of HIV integrase inhibitors [PDF]
Current Opinion in HIV and AIDS, 2012 The purpose of this paper is to review recent and relevant pharmacology data for three HIV integrase inhibitors: raltegravir (marketed), dolutegravir and elvitegravir (both in Phase III drug development).
Angela D. M. Kashuba +2 more
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Integrase and integration: biochemical activities of HIV-1 integrase [PDF]
Retrovirology, 2008 Integration of retroviral DNA is an obligatory step of retrovirus replication because proviral DNA is the template for productive infection. Integrase, a retroviral enzyme, catalyses integration. The process of integration can be divided into two sequential reactions.
Ali Saïb +4 more
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The Molecular Biology of HIV Integrase [PDF]
Future Virology, 2012 Integration of viral DNA into cellular DNA is an essential step in the replication cycle of HIV and other retroviruses. The first antiviral drugs that target integrase, the viral enzyme that catalyzes DNA integration, have recently been approved and more are in the pipeline. These drugs bind to an intermediate in DNA integration called the intasome, in
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Authentic HIV-1 Integrase Inhibitors [PDF]
Future Medicinal Chemistry, 2010 HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Terrence R. Burke +4 more
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HIV Dynamics and Integrase Inhibitors
Antiviral Chemistry and Chemotherapy, 2009 The integrase inhibitor (INI) raltegravir has shown promising results in clinical trials to date, reducing second phase HIV RNA levels by 70% in comparison with standard regimens. These trial results have been limited by the 50 copies/ml detection limit of the HIV RNA assay and have not investigated the effect of an INI regimen on levels of latently ...
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Elvitegravir: A New HIV Integrase Inhibitor [PDF]
Antiviral Chemistry and Chemotherapy, 2009 Integration is a distinctive and essential process in the HIV infection cycle and thus represents an attractive antiviral drug target. Integrase inhibitors combined with other classes of drug might contribute to long-lasting suppression of HIV type-1 (HIV-1) replication for many patients.
Kazuya Shimura +2 more
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Integrase, LEDGF/p75 and HIV replication [PDF]
Cellular and Molecular Life Sciences, 2008 HIV integrates a DNA copy of its genome into a host cell chromosome in each replication cycle. The essential DNA cleaving and joining chemistry of integration is known, but there is less understanding of the process as it occurs in a cell, where two complex and dynamic macromolecular entities are joined: the viral pre-integration complex and chromatin.
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HIV-1 Integrase: From Biology to Chemotherapeutics [PDF]
Current HIV Research, 2007 AIDS has claimed the lives of 25 million people worldwide, an additional 40 million people are HIV-infected and new cases are being diagnosed every year. Despite the fact that HAART has moved AIDS from the category of terminal diseases to that of treatable chronic illnesses, its long-term therapeutic success may be compromised by the development of ...
Zeinalipour-Loizidou, E. +7 more
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