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Controlling Androgen receptor nuclea...

Wang, Haoyu.

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Controlling Androgen receptor nuclear localization by dendrimer conjugates.

紀錄類型:	書目-電子資源 : Monograph/item
正題名/作者:	Controlling Androgen receptor nuclear localization by dendrimer conjugates./
作者:	Wang, Haoyu.
出版者:	Ann Arbor : ProQuest Dissertations & Theses, : 2016,
面頁冊數:	144 p.
附註:	Source: Dissertation Abstracts International, Volume: 78-01(E), Section: B.
Contained By:	Dissertation Abstracts International78-01B(E).
標題:	Biochemistry. -
電子資源:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=10156571
ISBN:	9781369116243

Controlling Androgen receptor nuclear localization by dendrimer conjugates.
Wang, Haoyu.

Controlling Androgen receptor nuclear localization by dendrimer conjugates. - Ann Arbor : ProQuest Dissertations & Theses, 2016 - 144 p.

Source: Dissertation Abstracts International, Volume: 78-01(E), Section: B.

Thesis (Ph.D.)--University of Delaware, 2016.

Androgen Receptor (AR) antagonists, such as bicalutamide and flutamide have been used widely in the treatment of prostate cancer. Although initial treatment is effective, prostate cancer cells often acquire antiandrogen resistance with prolonged treatment. AR over-expression and AR mutations contribute to the development of antiandrogen resistant cancer. Second generation antiandrogens such as enzalutamide are more effective and show reduced AR nuclear localization. In this study, derivatives of PAN52, a small molecule antiandrogen previously developed in our lab, were conjugated to the surface of generation 4 and generation 6 PAMAM dendrimers to obtain antiandrogen PAMAM dendrimer conjugates (APDC). APDCs readily enter cells and associate with AR in the cytoplasm. Due to their large size and positive charge, they can not enter the nucleus, thus retaining AR in the cytoplasm. In addition, APDCs are effective in decreasing AR mediated transcription and cell proliferation. APDC is the first AR antagonists that inhibit DHT-induced nuclear localization of AR. By inhibiting AR nuclear localization, APDC represents a new class of antiandrogens that offer an alternative approach to addressing antiandrogen-resistant prostate cancer.

ISBN: 9781369116243Subjects--Topical Terms:

518028
Biochemistry.

Controlling Androgen receptor nuclear localization by dendrimer conjugates.
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520 $a Lysine post-translational modification of AR Nuclear Localization Sequence (NLS) has great impact on AR cellular localization. It is of interest to understand which modifications modulate AR translocation into the nucleus. In this study, we prepared dendrimer-based acetyltransferase mimetic (DATM), DATM is able to catalytically acetylate AR in CWR22Rv1 cells, which will be a useful tool for studying AR modification effect on AR cellular localization. Derivatives of DATM, which transfer other chemical groups to AR, can be prepared similarly, and with more dendrimer based AR modification tools prepared in future, we will be able to understand and control AR cellular localization through AR modification.
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