A new chemical probe for phosphatidylinositol kinase activity

Par Conseil national de recherches du Canada

DOI	Trouver le DOI : https://doi.org/10.1002/cbic.201402155
Auteur	Rechercher : Sherratt, Allison R.¹; Rechercher : Nasheri ardakan, Neda¹; Rechercher : McKay, Craig S.¹; Rechercher : O'Hara, Shifawn¹; Rechercher : Hunt, Ashly¹; Rechercher : Ning, Zhibin; Rechercher : Figeys, Daniel; Rechercher : Goto, Nathalie K.; Rechercher : Pezacki, John Paul¹
Affiliation	Conseil national de recherches du Canada. Dispositifs médicaux
Format	Texte, Article
Sujet	phosphatidylinositol 3 kinase; phosphatidylinositol 3 kinase 110alpha; phosphatidylinositol kinase; phosphatidylinositol kinase 2alpha; phosphatidylinositol kinase 3alpha; phosphatidylinositol kinase 3beta; unclassified drug; wortmannin; breast cancer cell line; cancer cell line; chemical labeling; competitive inhibition; enzyme activity; enzyme inhibition; female; genotype; hepatitis C; Hepatitis C virus; human cell; liver cell carcinoma; liver disease; liver transplantation; molecular probe; photoactivation; photoreactivation; PIK BPyne; primed in situ labeling; protein analysis; protein function; uterine cervix cancer; virus replication; Western blotting; Hepatitis C virus
Résumé	Phosphatidylinositol kinases (PIKs) are key enzymatic regulators of membrane phospholipids and membrane environments that control many aspects of cellular function, from signal transduction to secretion, through the Golgi apparatus. Here, we have developed a photoreactive "clickable" probe, PIK-BPyne, to report the activity of PIKs. We investigated the selectivity and efficiency of the probe to both inhibit and label PIKs, and we compared PIK-BPyne to a wortmannin activity-based probe also known to target PIKs. We found that PIK-BPyne can act as an effective in situ activity-based probe, and for the first time, report changes in PI4K-IIIβ activity induced by the hepatitis C virus. These results establish the utility of PIK-BPyne for activity-based protein profiling studies of PIK function in native biological systems. Active PIKs: Phosphatidylinositol kinases (PIKs) are key enzymatic regulators of membrane phospholipids and environments that control many aspects of cellular function, from signal transduction to secretion. We developed a photoreactive "clickable" probe, PIK-BPyne, to assess activity of PIKs in native biological systems and demonstrated its ability to monitor hepatitis C virus-induced changes in PIK-IIIβ activity.
Date de publication	2014
Dans	ChemBioChem 15, nº 9 (2014) : 1253–1256.
Langue	anglais
Publications évaluées par des pairs	Oui
Numéro NPARC	21272798
Exporter la notice	Exporter en format RIS
Signaler une correction	Signaler une correction (s'ouvre dans un nouvel onglet)
Identificateur de l’enregistrement	4f44d72f-257a-4b1e-b423-346b838f0840
Enregistrement créé	2014-12-03
Enregistrement modifié	2020-04-22

Date de modification :: 2024-04-19