Dissemin is shutting down on January 1st, 2025

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American Chemical Society, Journal of Medicinal Chemistry, 2(60), p. 814-820, 2017

DOI: 10.1021/acs.jmedchem.6b01574

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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

Journal article published in 2017 by Amit Nathubhai ORCID, Teemu Haikarainen, Jarkko Koivunen ORCID, Sudarshan Murthy, Françoise Koumanov, Matthew D. Lloyd, Geoffrey D. Holman, Taina Pihlajaniemi, David Tosh, Lari Lehtiö ORCID, Michael D. Threadgill
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Compounds 13 and 14 were evaluated against eleven PARP isoforms to reveal that both 13 and 14 were more potent and isoform-selective towards 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.