Retroviral Integrase: Difference between revisions

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==Mechanism for strand-transfer inhibition action==

HIV integrase type 1 is a relatively new and novel target for inhibitors. In 2007, the first HIV-1 integrase inhibitor, Raltegravir, was approved by the FDA (6). Strand-transfer inhibitors work by preventing the concerted integration of the viral DNA into the host chromosome. After viral entry into the host cell, the reverse transcriptase converts the viral ssRNA into dsDNA. At this point, the integrase forms a complex with the viral DNA, creating the pre-integration complex (intasome). The pre-integration complex is then chaperoned into the nucleus, where two nucleotides are excised from the 3' end. Next, the DNA is then covalently integrated into the host DNA. The strand=transfer inhibitors interrupt this process, preventing the integration of the viral DNA into the host chromosome.

[[Image:478_integrase_fig1.jpg]]

==Integrase Inhibitors==

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4. [http://www.aidsinfo.nih.gov AIDS Info]

5. Krishan K. Pandey and Duane P. Grandgenett (2008) HIV-1 Integrase Strand Transfer Inhibitors: Novel Insights into their Mechanism of Action. ''Retrovirology: Research and Treatment" 2008:2 11-16

6.James F. Braun, DO, Ruth J. Cronje, PhD, Marnie G. Henderson (2008) HIV-1 Integrase Inhibitors. www.prn.org Volume 13, Pages 1–9

==Further Reading==

* GEN News Highlights [http://www.genengnews.com/news/bnitem.aspx?name=74423430&nc=1 "Scientists Solve 3-D Crystal Structure of Retroviral Integrase Bound to Viral DNA"], [http://www.genengnews.com Genetic Engineering & Biotechnology News] February 1, 2010.

Retroviral Integrase: Difference between revisions

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@@ Line 57: / Line 57: @@
 ==Mechanism for strand-transfer inhibition action==
+HIV integrase type 1 is a relatively new and novel target for inhibitors.  In 2007, the first HIV-1 integrase inhibitor, Raltegravir, was approved by the FDA (6).  Strand-transfer inhibitors work by preventing the concerted integration of the viral DNA into the host chromosome.  After viral entry into the host cell, the reverse transcriptase converts the viral ssRNA into dsDNA. At this point, the integrase forms a complex with the viral DNA, creating the pre-integration complex (intasome).  The pre-integration complex is then chaperoned into the nucleus, where two nucleotides are excised from the 3' end.  Next, the DNA is then covalently integrated into the host DNA.  The strand=transfer inhibitors interrupt this process, preventing the integration of the viral DNA into the host chromosome.
+[[Image:478_integrase_fig1.jpg]]
 ==Integrase Inhibitors==
@@ Line 83: / Line 87: @@
 . [http://www.aidsinfo.nih.gov AIDS Info]
+.  Krishan K. Pandey and Duane P. Grandgenett (2008)  HIV-1 Integrase Strand Transfer Inhibitors: Novel Insights into their Mechanism of Action.  ''Retrovirology:  Research and Treatment"  2008:2 11-16
+.James F. Braun, DO, Ruth J. Cronje, PhD, Marnie G. Henderson (2008) HIV-1 Integrase Inhibitors.  www.prn.org  Volume 13, Pages 1–9
 ==Further Reading==
 * GEN News Highlights [http://www.genengnews.com/news/bnitem.aspx?name=74423430&nc=1 "Scientists Solve 3-D Crystal Structure of Retroviral Integrase Bound to Viral DNA"], [http://www.genengnews.com Genetic Engineering & Biotechnology News] February 1, 2010.