A historical sketch of the discovery and development of HIV-1 integrase inhibitors

A Savarino - Expert opinion on investigational drugs, 2006 - Taylor & Francis
The long process of HIV-1 integrase inhibitor discovery and development can be attributed
to both the complexity of HIV-1 integration and poor 'integration'of these researches into …

Novel aryl diketo-containing inhibitors of HIV-1 integrase

GCG Pais, TR Burke - Drugs Future, 2002 - access.portico.org
HIV-1 integrase is a promising therapeutic target for the development of drugs to treat HIV
infection. Aryl diketo-based analogs, disclosed independently by scientists from Merck and …

HIV-1 integrase inhibitors: a decade of research and two drugs in clinical trial

AA Johnson, C Marchand… - Current Topics in …, 2004 - ingentaconnect.com
AIDS is currently treated with a combination therapy of reverse transcriptase and protease
inhibitors. Recently, the FDA approved a drug targeting HIV-1 entry into cells. There are …

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 …

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 …

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 integrase inhibitors as therapeutic agents in AIDS

V Nair, G Chi - Reviews in medical virology, 2007 - Wiley Online Library
HIV‐1 integrase is a protein of Mr 32 000 encoded at the 3′‐end of the pol gene.
Integration of HIV DNA into the host cell chromosomal DNA apparently occurs by a carefully …

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 …

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 …

Patented small molecule inhibitors of HIV-1 integrase: a 10-year saga

N Neamati - Expert Opinion on Therapeutic Patents, 2002 - Taylor & Francis
Validation of integrase as a suitable therapeutic target for the development of drugs against
HIV infection; discovery of diketo acid derivatives as bona fide inhibitors of integrase and the …