Targeting γ-secretase in breast cancer
Jianxun Han,1 Qiang Shen21Department of Chemical Engineering and Applied Chemistry, University of Toronto, 2Campbell Family Institute for Breast Cancer Research, Princess Margaret Hospital, University Health Network, Toronto, Ontario, CanadaAbstract: γ-secretase complexes are multisubu...
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Dove Medical Press
2012
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oai:doaj.org-article:b77bf96fafb04026b62e089787da0c0e2021-12-02T01:19:29ZTargeting γ-secretase in breast cancer1179-1314https://doaj.org/article/b77bf96fafb04026b62e089787da0c0e2012-06-01T00:00:00Zhttp://www.dovepress.com/targeting-gamma-secretase-in-breast-cancer-a10190https://doaj.org/toc/1179-1314Jianxun Han,1 Qiang Shen21Department of Chemical Engineering and Applied Chemistry, University of Toronto, 2Campbell Family Institute for Breast Cancer Research, Princess Margaret Hospital, University Health Network, Toronto, Ontario, CanadaAbstract: γ-secretase complexes are multisubunit protease complexes that perform the intramembrane cleavage of more than 60 type-I transmembrane proteins, including Notch receptors. Since dysregulated Notch signaling has been implicated in the tumorigenesis and progression of breast cancer, small molecule γ-secretase inhibitors (GSIs) are being tested for their therapeutic potential in breast cancer treatment in several clinical trials. Here, the structure of γ-secretase complex and the development of GSIs are briefly reviewed, the roles of Notch and several other γ-secretase substrates in breast cancer are discussed, and the difference between γ-secretase inhibition and Notch inhibition, as well as the side effects associated with GSIs, are described. A better understanding of molecular mechanisms that affect the responsiveness of breast cancer to GSI might help to develop strategies to enhance the antitumor activity and, at the same time, alleviate the side effects of GSI.Keywords: γ-secretase, GSI, Notch, breast cancerHan JShen QDove Medical PressarticleNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENBreast Cancer: Targets and Therapy, Vol 2012, Iss default, Pp 83-90 (2012) |
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DOAJ |
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DOAJ |
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EN |
| topic |
Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 |
| spellingShingle |
Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Han J Shen Q Targeting γ-secretase in breast cancer |
| description |
Jianxun Han,1 Qiang Shen21Department of Chemical Engineering and Applied Chemistry, University of Toronto, 2Campbell Family Institute for Breast Cancer Research, Princess Margaret Hospital, University Health Network, Toronto, Ontario, CanadaAbstract: γ-secretase complexes are multisubunit protease complexes that perform the intramembrane cleavage of more than 60 type-I transmembrane proteins, including Notch receptors. Since dysregulated Notch signaling has been implicated in the tumorigenesis and progression of breast cancer, small molecule γ-secretase inhibitors (GSIs) are being tested for their therapeutic potential in breast cancer treatment in several clinical trials. Here, the structure of γ-secretase complex and the development of GSIs are briefly reviewed, the roles of Notch and several other γ-secretase substrates in breast cancer are discussed, and the difference between γ-secretase inhibition and Notch inhibition, as well as the side effects associated with GSIs, are described. A better understanding of molecular mechanisms that affect the responsiveness of breast cancer to GSI might help to develop strategies to enhance the antitumor activity and, at the same time, alleviate the side effects of GSI.Keywords: γ-secretase, GSI, Notch, breast cancer |
| format |
article |
| author |
Han J Shen Q |
| author_facet |
Han J Shen Q |
| author_sort |
Han J |
| title |
Targeting γ-secretase in breast cancer |
| title_short |
Targeting γ-secretase in breast cancer |
| title_full |
Targeting γ-secretase in breast cancer |
| title_fullStr |
Targeting γ-secretase in breast cancer |
| title_full_unstemmed |
Targeting γ-secretase in breast cancer |
| title_sort |
targeting γ-secretase in breast cancer |
| publisher |
Dove Medical Press |
| publishDate |
2012 |
| url |
https://doaj.org/article/b77bf96fafb04026b62e089787da0c0e |
| work_keys_str_mv |
AT hanj targetingampgammasecretaseinbreastcancer AT shenq targetingampgammasecretaseinbreastcancer |
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1718403158242230272 |