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Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors

Darby, Richard A. J.; Unsworth, Amanda; Knapp, Stefan; Kerr, Ian; Callaghan, Richard


Purpose: Multidrug efflux pumps such as ABCG2 confer drug resistance to a number of cancer types, leading to poor prognosis and outcome. To date, the strategy of directly inhibiting multidrug efflux pumps in order to overcome drug resistance in cancer has been unsuccessful. An alternative strategy is to target proteins involved in the regulation of multidrug efflux pump activity or expression. Pim1 kinase has been demonstrated to phosphorylate ABCG2, promote its oligomerisation and contribute...[Show more]

CollectionsANU Research Publications
Date published: 2015
Type: Journal article
Source: Cancer Chemotherapy and Pharmacology
DOI: 10.1007/s00280-015-2858-9


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