Retroviral DNA integration

P Lesbats, AN Engelman, P Cherepanov - Chemical reviews, 2016 - ACS Publications
The integration of a DNA copy of the viral RNA genome into host chromatin is the defining
step of retroviral replication. This enzymatic process is catalyzed by the virus-encoded …

Multidimensional tunneling, recrossing, and the transmission coefficient for enzymatic reactions

J Pu, J Gao, DG Truhlar - Chemical reviews, 2006 - ACS Publications
Although many aspects of enzyme catalysis have been constructively analyzed, 1-52 there
are still many aspects that are imperfectly understood. Of particular interest in this regard are …

Crystal structure of the HIV-1 integrase catalytic core and C-terminal domains: a model for viral DNA binding

JCH Chen, J Krucinski, LJW Miercke… - Proceedings of the …, 2000 - National Acad Sciences
Insolubility of full-length HIV-1 integrase (IN) limited previous structure analyses to individual
domains. By introducing five point mutations, we engineered a more soluble IN that allowed …

Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)

K Shimura, E Kodama, Y Sakagami… - Journal of …, 2008 - Am Soc Microbiol
Integrase (IN), an essential enzyme of human immunodeficiency virus (HIV), is an attractive
antiretroviral drug target. The antiviral activity and resistance profile in vitro of a novel IN …

Structure and function of HIV-1 integrase

TK Chiu, DR Davies - Current topics in medicinal chemistry, 2004 - ingentaconnect.com
HIV-1 integrase is a multidomain enzyme which is required for the integration of viral DNA
into the host genome. It is one of three enzymes of HIV, the others being the Reverse …

Enhanced enzyme stability through site-directed covalent immobilization

JCY Wu, CH Hutchings, MJ Lindsay, CJ Werner… - Journal of …, 2015 - Elsevier
Breakthroughs in enzyme immobilization have enabled increased enzyme recovery and
reusability, leading to significant decreases in the cost of enzyme use and fueling …

Molecular basis of human immunodeficiency virus drug resistance: an update

L Menéndez-Arias - Antiviral research, 2010 - Elsevier
Antiretroviral therapy has led to a significant decrease in human immunodeficiency virus
(HIV)-related mortality. Approved antiretroviral drugs target different steps of the viral life …

Rational design and synthesis of novel dimeric diketoacid-containing inhibitors of HIV-1 integrase: implication for binding to two metal ions on the active site of …

YQ Long, XH Jiang, R Dayam, T Sanchez… - Journal of medicinal …, 2004 - ACS Publications
Discovery of diketoacid-containing compounds as HIV-1 integrase (IN) inhibitors played a
major role in validating this enzyme as an important target for the development of …

[HTML][HTML] Specificity of trypsin and chymotrypsin: loop-motion-controlled dynamic correlation as a determinant

W Ma, C Tang, L Lai - Biophysical journal, 2005 - cell.com
Trypsin and chymotrypsin are both serine proteases with high sequence and structural
similarities, but with different substrate specificity. Previous experiments have demonstrated …

Resistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitors

O Goethals, R Clayton, M Van Ginderen… - Journal of …, 2008 - Am Soc Microbiol
Integration of viral DNA into the host chromosome is an essential step in the life cycle of
retroviruses and is facilitated by the viral integrase enzyme. The first generation of integrase …