Fluorescent Inhibitors as Tools To Characterize Enzymes: Case Study of the Lipid Kinase Phosphatidylinositol 4-Kinase IIIβ (PI4KB).
Identifieur interne : 000E31 ( Main/Exploration ); précédent : 000E30; suivant : 000E32Fluorescent Inhibitors as Tools To Characterize Enzymes: Case Study of the Lipid Kinase Phosphatidylinositol 4-Kinase IIIβ (PI4KB).
Auteurs : Jana Humpolickova [République tchèque] ; Ivana Mejdrová [République tchèque] ; Marika Matousova [République tchèque] ; Radim Nencka [République tchèque] ; Evzen Boura [République tchèque]Source :
- Journal of medicinal chemistry [ 1520-4804 ] ; 2017.
Descripteurs français
- KwdFr :
- MESH :
- antagonistes et inhibiteurs : Phosphotransferases (Alcohol Group Acceptor).
- pharmacologie : Antienzymes, Colorants fluorescents.
- Antienzymes, Cellules HeLa, Colorants fluorescents, Humains, Simulation de docking moléculaire.
English descriptors
- KwdEn :
- MESH :
- chemical , antagonists & inhibitors : Phosphotransferases (Alcohol Group Acceptor).
- chemical , chemistry : Enzyme Inhibitors, Fluorescent Dyes.
- chemical , pharmacology : Enzyme Inhibitors, Fluorescent Dyes.
- HeLa Cells, Humans, Molecular Docking Simulation.
Abstract
The lipid kinase phosphatidylinositol 4-kinase IIIβ (PI4KB) is an essential host factor for many positive-sense single-stranded RNA (+RNA) viruses including human pathogens hepatitis C virus (HCV), Severe acute respiratory syndrome (SARS), coxsackie viruses, and rhinoviruses. Inhibitors of PI4KB are considered to be potential broad-spectrum virostatics, and it is therefore critical to develop a biochemical understanding of the kinase. Here, we present highly potent and selective fluorescent inhibitors that we show to be useful chemical biology tools especially in determination of dissociation constants. Moreover, we show that the coumarin-labeled inhibitor can be used to image PI4KB in cells using fluorescence-lifetime imaging microscopy (FLIM) microscopy.
DOI: 10.1021/acs.jmedchem.6b01466
PubMed: 28004946
Affiliations:
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& inhibitors" xml:lang="en"><term>Phosphotransferases (Alcohol Group Acceptor)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Enzyme Inhibitors</term><term>Fluorescent Dyes</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Enzyme Inhibitors</term><term>Fluorescent Dyes</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Phosphotransferases (Alcohol Group Acceptor)</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antienzymes</term><term>Colorants fluorescents</term></keywords><keywords scheme="MESH" xml:lang="en"><term>HeLa Cells</term><term>Humans</term><term>Molecular Docking Simulation</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Antienzymes</term><term>Cellules HeLa</term><term>Colorants fluorescents</term><term>Humains</term><term>Simulation de docking moléculaire</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The lipid kinase phosphatidylinositol 4-kinase IIIβ (PI4KB) is an essential host factor for many positive-sense single-stranded RNA (+RNA) viruses including human pathogens hepatitis C virus (HCV), Severe acute respiratory syndrome (SARS), coxsackie viruses, and rhinoviruses. Inhibitors of PI4KB are considered to be potential broad-spectrum virostatics, and it is therefore critical to develop a biochemical understanding of the kinase. Here, we present highly potent and selective fluorescent inhibitors that we show to be useful chemical biology tools especially in determination of dissociation constants. Moreover, we show that the coumarin-labeled inhibitor can be used to image PI4KB in cells using fluorescence-lifetime imaging microscopy (FLIM) microscopy.</div></front></TEI><affiliations><list><country><li>République tchèque</li></country></list><tree><country name="République tchèque"><noRegion><name sortKey="Humpolickova, Jana" sort="Humpolickova, Jana" uniqKey="Humpolickova J" first="Jana" last="Humpolickova">Jana Humpolickova</name></noRegion><name sortKey="Boura, Evzen" sort="Boura, Evzen" uniqKey="Boura E" first="Evzen" last="Boura">Evzen Boura</name><name sortKey="Matousova, Marika" sort="Matousova, Marika" uniqKey="Matousova M" first="Marika" last="Matousova">Marika Matousova</name><name sortKey="Mejdrova, Ivana" sort="Mejdrova, Ivana" uniqKey="Mejdrova I" first="Ivana" last="Mejdrová">Ivana Mejdrová</name><name sortKey="Nencka, Radim" sort="Nencka, Radim" uniqKey="Nencka R" first="Radim" last="Nencka">Radim Nencka</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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