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New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action
Background: Competitors of LEDGF binding to HIV-1 integrase could prevent targeted integration to chromatin. Results: LEDGF competitors like tBPQAs were also found to inhibit integrase enzymeExpand
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Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.
It has been shown that L-731988, a potent integrase inhibitor, targets a conformation of the integrase enzyme formed when complexed to viral DNA, with the 3'-end dinucleotide already cleaved. It hasExpand
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Affinities between the Binding Partners of the HIV-1 Integrase Dimer-Lens Epithelium-derived Growth Factor (IN Dimer-LEDGF) Complex
The interaction between lens epithelium-derived growth factor/transcriptional co-activator p75 (LEDGF) and human immunodeficiency virus type 1 (HIV-1) integrase (IN) is essential for HIV-1Expand
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Catalytically-active complex of HIV-1 integrase with a viral DNA substrate binds anti-integrase drugs
HIV-1 integration into the host cell genome is a multistep process catalyzed by the virally-encoded integrase (IN) protein. In view of the difficulty of obtaining a stable DNA-bound IN at highExpand
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Evidence that a nereistoxin metabolite, and not nereistoxin itself, reduces neuronal nicotinic receptors: studies in the whole chick ciliary ganglion, on isolated neurons and immunoprecipitated
Nereistoxin (100 microM, 2-10 min) blocks nicotinic receptors in the intact chick ciliary ganglion. This effect mimics blockade by the reducing agent dithiothreitol (2 mM, 20 min), which is notExpand
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Combinatorial fluorescence energy transfer tags for multiplex biological assays
We report an approach for developing combinatorial fluorescence energy transfer (CFET) tags by tuning the tags' fluorescence emission signatures. The tags can all be excited at a single wavelengthExpand
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Aromatic trivalent arsenicals: covalent yet reversible reagents for the agonist binding site of nicotinic receptors.
The agonist binding site of nicotinic acetylcholine receptors (AChRs) includes a disulfide bond that is easily reduced with dithiothreitol to a pair of thiols, and can be then either reoxidized withExpand
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Dithiothreitol causes HIV-1 integrase dimer dissociation while agents interacting with the integrase dimer interface promote dimer formation.
We have developed a homogeneous time-resolved fluorescence resonance energy transfer (FRET)-based assay that detects the formation of HIV-1 integrase (IN) dimers. The assay utilizes IN monomers thatExpand
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Comparison of 316LVM and MP35N alloys as charge injection electrodes.
An In vitro comparison of the corrosion response of 316LVM stainless steel and MP35N (a CoNiCrMo alloy) electrodes under conditions appropriate to applications in functional electrical stimulationExpand
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Cyclophosphamide potentiation and aldehyde oxidase inhibition by phosphorylated aldehydes and acetals.
Fourteen phosphorylated acetals and aldehydes were synthesized for testing in vitro as inhibitors or substrates of aldehyde oxidase, an enzyme involved in the conversion of aldophosphamide toExpand
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