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Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity

Nathubhai, Amit, Haikarainen, T., Koivunen, J., Murthy, S., Koumanov, F., Lloyd, M.D., Holman, J.D., Pihlajaniemi, T., Tosh, D., Lehtiö, L. and Threadgill, M.D. (2017) Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity. Journal of Medicinal Chemistry, 60 (2). pp. 814-820. ISSN 0022-2623

Item Type: Article

Abstract

Compounds 13 and 14 were evaluated against 11 PARP isoforms to reveal that both 13 and 14 were more potent
and isoform selective toward inhibiting tankyrases (TNKSs) than the “standard” inhibitor 1 (XAV939)5, i.e., IC50 = 100 pM vs TNKS2 and IC50 = 6.5 μM vs PARP1 for 14. In cellular assays, 13 and 14 inhibited Wnt-signaling, enhanced insulin-stimulated glucose uptake, and inhibited the proliferation of DLD-1 colorectal adenocarcinoma cells to a greater extent than 1.

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More Information

Depositing User: Amit Nathubhai

Identifiers

Item ID: 9787
Identification Number: https://doi.org/10.1021/acs.jmedchem.6b01574
ISSN: 0022-2623
URI: http://sure.sunderland.ac.uk/id/eprint/9787
Official URL: https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem....

Users with ORCIDS

ORCID for Amit Nathubhai: ORCID iD orcid.org/0000-0003-3686-2799

Catalogue record

Date Deposited: 10 Aug 2018 08:24
Last Modified: 04 Feb 2021 17:00

Contributors

Author: Amit Nathubhai ORCID iD
Author: T. Haikarainen
Author: J. Koivunen
Author: S. Murthy
Author: F. Koumanov
Author: M.D. Lloyd
Author: J.D. Holman
Author: T. Pihlajaniemi
Author: D. Tosh
Author: L. Lehtiö
Author: M.D. Threadgill

University Divisions

Faculty of Health Sciences and Wellbeing
Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences

Subjects

Sciences > Chemistry
Sciences

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