2014
DOI: 10.1042/bst20140043
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A role for the pseudokinase HER3 in the acquired resistance against EGFR- and HER2-directed targeted therapy

Abstract: Specific inhibition of members of the EGFR (epidermal growth factor receptor) family, particularly EGFR and HER2 (human epidermal growth factor receptor 2), are an important therapeutic strategy in many human cancers. Compared with classical chemotherapy, these targeted therapeutics are very specific and initially effective, but acquired resistance against these targeted therapies is a recurring threat. A growing body of recent work has highlighted a pseudokinase in the EGFR family, HER3, and its ligand, NRG (… Show more

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Cited by 23 publications
(19 citation statements)
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References 49 publications
(91 reference statements)
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“…HER3 plays a major role in the survival of HER2+ breast cancers and their resistance to HER2-targeted drugs [20, 21]. It was previously shown that breast cancer cells engineered to overexpress EGFR are sensitized to DDA-induced cell death and Akt dephosphorylation [33], but differential sensitivity to DDA-mediated HER3 downregulation was not examined in that report.…”
Section: Resultsmentioning
confidence: 99%
“…HER3 plays a major role in the survival of HER2+ breast cancers and their resistance to HER2-targeted drugs [20, 21]. It was previously shown that breast cancer cells engineered to overexpress EGFR are sensitized to DDA-induced cell death and Akt dephosphorylation [33], but differential sensitivity to DDA-mediated HER3 downregulation was not examined in that report.…”
Section: Resultsmentioning
confidence: 99%
“…The human epidermal growth factor receptor 3 (HER3 or ErbB3) has recently attracted attention as a candidate target for anticancer therapy (1,2). HER3 is involved in the development of a variety of cancer types such as prostate, breast, lung, and colorectal, as well in the resistance towards tyrosine kinase-targeted therapies (3,4). HER3 has an inactive tyrosine kinase domain, therefore its heterodimerization with other HER-family members is required for activation and signalling (5).…”
Section: Introductionmentioning
confidence: 99%
“…The preferred partner for HER3 heterodimerization is HER2 and together they form one of the most potent units in tumourigenesis that is able to activate downstream signalling pathways, such as MAPK/MEK and PI-3K/Akt (6). The role of HER3 expression in resistance to anti-HER2 therapy in breast cancer is well documented (2,3). Signalling by the HER2/HER3 heterodimer is also critical in hormone-refractory prostate cancer and it was demonstrated that blocking of heterodimerization inhibited the growth of hormonerefractory prostate cancer xenografts (7).…”
Section: Introductionmentioning
confidence: 99%
“…The HER2-HER3 unit activates downstream signalling pathways, such as PI-3K/Akt and MAPK/MEK and is considered as one of the most potent hetero-dimers in tumorigenesis 3 . Strong evidence points to the involvement of HER3 in various cancers, such as breast, prostate and colorectal cancer, and its role in the resistance of these tumours to receptor tyrosine kinase-targeted therapies 4 5 . In response to trastuzumab therapy in HER2 overexpressing breast cancer, HER3 can become upregulated and increase the signalling ability of HER2 as a compensation for its inhibition, which cause resistance to therapy 6 7 .…”
mentioning
confidence: 99%