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See detailThiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.
Vahter, Jurgen; Viht, Kaido; Uri, Asko et al

in Bioorganic & medicinal chemistry (2018), 26(18), 5062-5068

A previously disclosed protein kinase (PK) CK2-selective inhibitor 4-(2-amino-1,3-thiazol-5-yl)benzoic acid (ATB) and its selenium-containing counterpart (ASB) revealed remarkable room temperature ... [more ▼]

A previously disclosed protein kinase (PK) CK2-selective inhibitor 4-(2-amino-1,3-thiazol-5-yl)benzoic acid (ATB) and its selenium-containing counterpart (ASB) revealed remarkable room temperature phosphorescence when bound to the ATP pocket of the protein kinase CK2. Conjugation of these fragments with a mimic of CK2 substrate peptide resulted in bisubstrate inhibitors with increased affinity towards the kinase. Attachment of the fluorescent acceptor dye 5-TAMRA to the conjugates led to significant enhancement of intensity of long-lifetime (microsecond-scale) photoluminescence of both sulfur- and selenium-containing compounds. The developed photoluminescent probes make possible selective determination of the concentration of CK2 in cell lysates and characterization of CK2 inhibitors by means of time-gated measurement of photoluminescence. [less ▲]

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See detailBifunctional Ligands for Inhibition of Tight-Binding Protein–Protein Interactions
Ivan, Taavi; Enkvist, Erki; Viira, Birgit et al

in Bioconjugate Chemistry (2016), 27(8), 1900-1910

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See detailPhosphorylation of Notch1 by Pim kinases promotes oncogenic signaling in breast and prostate cancer cells
Santio, Niina M.; Landor, Sebastian K.-J.; Vahtera, Laura et al

in Oncotarget (2016), 7(28), 43220-43238

Tumorigenesis is a multistep process involving co-operation between several deregulated oncoproteins. In this study, we unravel previously unrecognized interactions and crosstalk between Pim kinases and ... [more ▼]

Tumorigenesis is a multistep process involving co-operation between several deregulated oncoproteins. In this study, we unravel previously unrecognized interactions and crosstalk between Pim kinases and the Notch signaling pathway, with implications for both breast and prostate cancer. We identify Notch1 and Notch3, but not Notch2, as novel Pim substrates and demonstrate that for Notch1, the serine residue 2152 is phosphorylated by all three Pim family kinases. This target site is located in the second nuclear localization sequence (NLS) of the Notch1 intracellular domain (N1ICD), and is shown to be important for both nuclear localization and transcriptional activity of N1ICD. Phosphorylation-dependent stimulation of Notch1 signaling promotes migration of prostate cancer cells, balances glucose metabolism in breast cancer cells, and supports in vivo growth of both types of cancer cells on chick embryo chorioallantoic membranes. Furthermore, Pim-induced growth of orthotopic prostate xenografts in mice is associated with enhanced nuclear Notch1 activity. Finally, simultaneous inhibition of Pim and Notch abrogates the cellular responses more efficiently than individual treatments, opening up new vistas for combinatorial cancer therapy. [less ▲]

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See detailCombining chemical and genetic approaches for development of responsive FRET-based sensor systems for protein kinases
Manoharan, Ganesh Babu UL; Enkvist, Erki; Uri, Asko

in Biophysical Chemistry (2016), 211

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See detailFRET-based screening assay using small-molecule photoluminescent probes in lysate of cells overexpressing RFP-fused protein kinases
Manoharan, Ganesh Babu UL; Enkvist, Erki; Kasari, Marje et al

in Analytical Biochemistry (2015)

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See detailPIM kinase-responsive microsecond-lifetime photoluminescent probes based on selenium-containing heteroaromatic tricycle
Ekambaram, Ramesh; Manoharan, Ganesh Babu UL; Enkvist, Erki et al

in RSC Advances (2015)

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See detailBenzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases
Ekambaram, Ramesh; Enkvist, Erki; Manoharan, Ganesh Babu UL et al

in Chemical Communications (2014)

Detailed reference viewed: 37 (0 UL)