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10.1097/CAD.0000000000000271 http://scihub22266oqcxt.onion/10.1097/CAD.0000000000000271 C4560273!4560273 !26164151     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=26164151 &cmd=llinks): Failed to open stream: HTTP request failed! 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RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models |pdf=|usr=}}{{26164151 }} gab.com Text RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models JO: Anticancer Drugs http://www.kidney.de/pget.php?&tw=1&pmid=26164151 #FOAvip Agents that inhibit estrogen production, such as aromatase inhibitors or those that directly block estrogen receptor (ER) activity, such as selective estrogen receptor modulators and selective estrogen receptor degraders, are routinely used in the treatment of ER-positive breast cancers. However, although initial treatment with these agents is often successful, many women eventually relapse with drug-resistant breast cancers. To overcome some of the challenges associated with current endocrine therapies and to combat the development of resistance, there is a need for more durable and more effective ER-targeted therapies. Here we describe and characterize a novel, orally bioavailable small-molecule selective estrogen receptor degrader, RAD1901, and evaluate its therapeutic potential for the treatment of breast cancer. RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. Importantly, RAD1901 produced a robust and profound inhibition of tumor growth in MCF-7 xenograft models. In an intracranial MCF-7 model, RAD1901-treated animals survived longer than those treated with either control or fulvestrant, suggesting the potential benefit of RAD1901 in the treatment of ER-positive breast cancer that has metastasized to the brain. Finally, RAD1901 preserved ovariectomy-induced bone loss and prevented the uterotropic effects of E2, suggesting that it may act selectively as an agonist in bone but as an antagonist in breast and uterine tissues. RAD1901 is currently under clinical study in postmenopausal women with ER-positive advanced breast cancer. Twit Text FOAVip RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models ????Anticancer Drugs http://www.kidney.de/pget.php?&tw=1&pmid=26164151 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=26164151 #FOAvip English Wikipedia <ref>{{Cite pmid|26164151 }}</ref> RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models #MMPMID26164151 Garner F ; Shomali M ; Paquin D ; Lyttle CR ; Hattersley G Anticancer Drugs 2015[Oct]; 26 (9 ): 948-56 PMID26164151 show ga Agents that inhibit estrogen production, such as aromatase inhibitors or those that directly block estrogen receptor (ER) activity, such as selective estrogen receptor modulators and selective estrogen receptor degraders, are routinely used in the treatment of ER-positive breast cancers. However, although initial treatment with these agents is often successful, many women eventually relapse with drug-resistant breast cancers. To overcome some of the challenges associated with current endocrine therapies and to combat the development of resistance, there is a need for more durable and more effective ER-targeted therapies. Here we describe and characterize a novel, orally bioavailable small-molecule selective estrogen receptor degrader, RAD1901, and evaluate its therapeutic potential for the treatment of breast cancer. RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. Importantly, RAD1901 produced a robust and profound inhibition of tumor growth in MCF-7 xenograft models. In an intracranial MCF-7 model, RAD1901-treated animals survived longer than those treated with either control or fulvestrant, suggesting the potential benefit of RAD1901 in the treatment of ER-positive breast cancer that has metastasized to the brain. Finally, RAD1901 preserved ovariectomy-induced bone loss and prevented the uterotropic effects of E2, suggesting that it may act selectively as an agonist in bone but as an antagonist in breast and uterine tissues. RAD1901 is currently under clinical study in postmenopausal women with ER-positive advanced breast cancer. |Administration, Oral [MESH] |Animals [MESH] |Antineoplastic Agents/*therapeutic use [MESH] |Binding, Competitive [MESH] |Bone Density/drug effects [MESH] |Brain Neoplasms/*drug therapy/metabolism/secondary [MESH] |Breast Neoplasms/*drug therapy/metabolism/pathology [MESH] |Cell Proliferation/drug effects [MESH] |Estrogen Receptor alpha/*metabolism [MESH] |Female [MESH] |Heterografts [MESH] |MCF-7 Cells [MESH] |Mice, Nude [MESH] |Neoplasm Transplantation [MESH] |Osteoporosis/pathology/physiopathology/prevention & control [MESH] |Ovariectomy [MESH] |Phenylurea Compounds/*pharmacology [MESH] |Rats, Sprague-Dawley [MESH] |Uterus/drug effects/metabolism [MESH]RAD1901: a novel, orally bioavailable selective estrogen receptor degr(epmc).pdf DeepDyve Pubget Overpricing