| pubmed-article:18794799 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C0376358 | lld:lifeskim |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C0006141 | lld:lifeskim |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C0597519 | lld:lifeskim |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C1519751 | lld:lifeskim |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C0699900 | lld:lifeskim |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C0243125 | lld:lifeskim |
| pubmed-article:18794799 | lifeskim:mentions | umls-concept:C0599894 | lld:lifeskim |
| pubmed-article:18794799 | pubmed:issue | 57 | lld:pubmed |
| pubmed-article:18794799 | pubmed:dateCreated | 2008-12-4 | lld:pubmed |
| pubmed-article:18794799 | pubmed:abstractText | Proteolysis targeting chimeric molecules (Protacs) target proteins for destruction by exploiting the ubiquitin-dependent proteolytic system of eukaryotic cells. We designed two Protacs that contain the peptide 'degron' from hypoxia-inducible factor-1alpha, which binds to the Von-Hippel-Lindau (VHL) E3 ubiquitin ligase complex, linked to either dihydroxytestosterone that targets the androgen receptor (AR; Protac-A), or linked to estradiol (E2) that targets the estrogen receptor-alpha (ERalpha; Protac-B). We hypothesized that these Protacs would recruit hormone receptors to the VHL E3 ligase complex, resulting in the degradation of receptors, and decreased proliferation of hormone-dependent cell lines. Treatment of estrogen-dependent breast cancer cells with Protac-B induced the degradation of ERalpha in a proteasome-dependent manner. Protac-B inhibited the proliferation of ERalpha-dependent breast cancer cells by inducing G(1) arrest, inhibition of retinoblastoma phosphorylation and decreasing expression of cyclin D1, progesterone receptors A and B. Protac-B treatment did not affect the proliferation of estrogen-independent breast cancer cells that lacked ERalpha expression. Similarly, Protac-A treatment of androgen-dependent prostate cancer cells induced G(1) arrest but did not affect cells that do not express AR. Our results suggest that Protacs specifically inhibit the proliferation of hormone-dependent breast and prostate cancer cells through degradation of the ERalpha and AR, respectively. | lld:pubmed |
| pubmed-article:18794799 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:18794799 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:18794799 | pubmed:language | eng | lld:pubmed |
| pubmed-article:18794799 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18794799 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:18794799 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18794799 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18794799 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:18794799 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18794799 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:18794799 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:18794799 | pubmed:issn | 1476-5594 | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:KimKK | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:SakamotoK MKM | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:CrewsC MCM | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:DeshaiesR JRJ | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:Rodriguez-Gon... | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:CyrusKK | lld:pubmed |
| pubmed-article:18794799 | pubmed:author | pubmed-author:SalciusMM | lld:pubmed |
| pubmed-article:18794799 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:18794799 | pubmed:day | 4 | lld:pubmed |
| pubmed-article:18794799 | pubmed:volume | 27 | lld:pubmed |
| pubmed-article:18794799 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:18794799 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:18794799 | pubmed:pagination | 7201-11 | lld:pubmed |
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| pubmed-article:18794799 | pubmed:year | 2008 | lld:pubmed |
| pubmed-article:18794799 | pubmed:articleTitle | Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer. | lld:pubmed |
| pubmed-article:18794799 | pubmed:affiliation | Department of Pediatrics, Gwynne Hazen Cherry Laboratories, Jonsson Comprehensive Cancer Center, David Geffen School of Medicine at UCLA, Los Angeles, CA 90095-1752, USA. | lld:pubmed |
| pubmed-article:18794799 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:18794799 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:18794799 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:18794799 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
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