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 …

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 integrase inhibitors

MA Walker, TD Johnson, OK Kim, Y Zhang - US Patent 6,548,546, 2003 - Google Patents
BACKGROUND Human immunodeficiency virus (HIV) has been identi fied as the etiological
agent responsible for acquired immune deficiency Syndrome (AIDS), a fatal disease …

Update on HIV integrase inhibitors for the treatment of HIV-1 infection

B Max - Future Virology, 2019 - Taylor & Francis
It has been over 30 years since the first antiretroviral agent was approved for treatment of
HIV-1 infection and its impact on morbidity and mortality has been dramatic. However, early …

Advances in the development of HIV integrase strand transfer inhibitors

Y Wang, SX Gu, Q He, R Fan - European Journal of Medicinal Chemistry, 2021 - Elsevier
Abstract HIV-1 integrase (IN) is a key enzyme in viral replication that catalyzes the covalent
integration of viral cDNA into the host genome. Currently, five HIV-1 IN strand transfer …

The future of integrase inhibitors of HIV-1

I Malet, V Calvez, AG Marcelin - Current opinion in virology, 2012 - Elsevier
Integration of the HIV-1 DNA is required and essential to maintain the viral DNA in the
infected cell. Integration process occurs in several events, mainly endonucleolytic …

Authentic HIV-1 integrase inhibitors

C Liao, C Marchand, TR Burke Jr… - Future medicinal …, 2010 - Taylor & Francis
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 …

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 …

Novel integrase inhibitors for HIV

N Prada, M Markowitz - Expert Opinion on Investigational Drugs, 2010 - Taylor & Francis
Importance of the field: Integrase inhibitors are the newest class of antiretroviral agents
developed to treat HIV-1 infection. Raltegravir (RAL), the only integrase inhibitor (INI) …

Role of integrase inhibitors in the treatment of HIV disease

L Palmisano - Expert review of anti-infective therapy, 2007 - Taylor & Francis
The introduction of highly active antiretroviral therapy (HAART) has produced a dramatic
reduction in HIV-related mortality and morbidity among populations with widespread access …