HIV‐1 integrase inhibitors: 2003–2004 update

R Dayam, J Deng, N Neamati - Medicinal research reviews, 2006 - Wiley Online Library
The integration of viral cDNA into the host genome is an essential step in the HIV‐1‐life
cycle and is mediated by the virally encoded enzyme, integrase (IN). Inhibition of this …

HIV‐1 integrase inhibitors: 2005–2006 update

R Dayam, R Gundla, LQ Al‐Mawsawi… - Medicinal Research …, 2008 - Wiley Online Library
Abstract HIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome,
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …

HIV-1 integrase inhibitors: an emerging clinical reality

R Dayam, LQ Al-Mawsawi, N Neamati - Drugs in R & D, 2007 - Springer
From the discovery of HIV-1 integrase (IN) inhibitors using enzyme-based assays in 1992, it
has taken 15 years to achieve success in human clinical trials. Currently available …

HIV‐1 integrase inhibitors: 2007–2008 update

K Ramkumar, E Serrao, S Odde… - Medicinal research …, 2010 - Wiley Online Library
In recent years, HIV‐1 integrase (IN) has become an attractive target for designing
antiretroviral agents. The first IN inhibitor approved for clinical use, raltegravir, has validated …

Development of integrase inhibitors for treatment of AIDS: An overview

S Dubey, YD Satyanarayana, H Lavania - European journal of medicinal …, 2007 - Elsevier
HIV-1 integrase (IN) is an essential enzyme for retroviral replication. It is involved in the
integration of HIV DNA into host chromosomal DNA. The unique properties of IN makes it an …

Design of second generation HIV-1 integrase inhibitors

J Deng, R Dayam, LQ Al-Mawsawi… - Current …, 2007 - ingentaconnect.com
The prospect of HIV-1 integrase (IN) as a therapeutically viable retroviral drug target is on
the verge of realization. The observed preclinical and clinical performance of β-diketo …

Small-molecule HIV-1 integrase inhibitors: the 2001-2002 update

R Dayam, N Neamati - Current pharmaceutical design, 2003 - ingentaconnect.com
Integration of viral DNA into host cell chromosomal DNA to form a provirus is an essential
step in the viral life cycle. This process is mediated by integrase (IN), a 32 KDa viral enzyme …

Designing HIV integrase inhibitors-shooting the last arrow

MT Makhija - Current medicinal chemistry, 2006 - ingentaconnect.com
The arsenal of drugs in the fight against AIDS is rapidly diminishing as the HIV becomes
resistant to the available reverse transcriptase and protease inhibitors. After killing millions …

Mining the NCI antiviral compounds for HIV-1 integrase inhibitors

J Deng, JA Kelley, JJ Barchi, T Sanchez… - Bioorganic & medicinal …, 2006 - Elsevier
HIV-1 integrase (IN) is an essential enzyme for effective viral replication and is a validated
target for the development of antiretroviral drugs. Currently, there are no approved drugs …

Anti-infectives clinical progress of HIV-1 integrase inhibitors

LQ Al-Mawsawi, RI Al-Safi… - Expert opinion on …, 2008 - Taylor & Francis
Background: HIV-1 integrase (IN) represents a therapeutically advantageous viral target to
treat HIV/AIDS in the clinic. Over a decade of progress in the field has resulted in IN inhibitor …