Pharmacology of HIV integrase inhibitors [PDF]
The purpose of this paper is to review recent and relevant pharmacology data for three HIV integrase inhibitors: raltegravir (marketed), dolutegravir and elvitegravir (both in Phase III drug development).
Angela D. M. Kashuba+2 more
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Making serine integrases work for us [PDF]
DNA site-specific recombinases are enzymes (often associated with mobile DNA elements) that catalyse breaking and rejoining of DNA strands at specific points, thereby bringing about precise genetic rearrangements.
Stark, W. Marshall
core +1 more source
Antiretroviral drugs to prevent integration of the HIV viral genome into chromosomes are undergoing clinical trials, yet they have been developed with an imperfect understanding of their mechanism of action. The recent crystal structure of the major viral protein integrase from a related, little‐known retrovirus, has finally provided insight into how ...
openaire +2 more sources
Gated rotation mechanism of site-specific recombination by ϕC31 integrase [PDF]
Integrases, such as that of the Streptomyces temperate bacteriophage ϕC31, promote site-specific recombination between DNA sequences in the bacteriophage and bacterial genomes to integrate or excise the phage DNA.
A. R. McEwan+28 more
core +1 more source
Mathematical model of a serine integrase-controlled toggle switch with a single input [PDF]
Dual-state genetic switches that can change their state in response to input signals can be used in synthetic biology to encode memory and control gene expression.
Colloms, Sean D.+3 more
core +1 more source
An Allosteric Mechanism for Inhibiting HIV-1 Integrase with a Small Molecule [PDF]
HIV-1 integrase (IN) is a validated target for developing antiretroviral inhibitors. Using affinity acetylation and mass spectrometric (MS) analysis, we previously identified a tetra-acetylated inhibitor (2E)-3-[3,4-bis(acetoxy)phenyl]-2-propenoate-N ...
Burke, Terrence R., Jr.+7 more
core +3 more sources
Substrate specificity of Ty1 integrase [PDF]
Integration of the Saccharomyces cerevisiae retrotransposon Ty1 requires the element-encoded integrase (IN) protein, which is a component of cytoplasmic virus-like particles (VLPs). Using purified recombinant Ty1 IN and an oligonucleotide integration assay based on Ty1 long terminal repeat sequences, we have compared IN activity on substrates having ...
S P Moore, D J Garfinkel, M Powers
openaire +2 more sources
Rapid metabolic pathway assembly and modification using serine integrase site-specific recombination [PDF]
Synthetic biology requires effective methods to assemble DNA parts into devices and to modify these devices once made. Here we demonstrate a convenient rapid procedure for DNA fragment assembly using site-specific recombination by ϕC31 integrase.
Colloms, S.D.+7 more
core +4 more sources
Viral Hybrid Vectors for Somatic Integration - Are They the Better Solution? [PDF]
The turbulent history of clinical trials in viral gene therapy has taught us important lessons about vector design and safety issues. Much effort was spent on analyzing genotoxicity after somatic integration of therapeutic DNA into the host genome. Based
Ehrhardt, Anja+2 more
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Weight gain among treatment-naïve persons with HIV starting integrase inhibitors compared to non-nucleoside reverse transcriptase inhibitors or protease inhibitors in a large observational cohort in the United States and Canada. [PDF]
IntroductionWeight gain following antiretroviral therapy (ART) initiation is common, potentially predisposing some persons with HIV (PWH) to cardio-metabolic disease.
Altoff, Keri N+23 more
core +1 more source