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10.1021/acs.jmedchem.5b00760

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suck abstract from ncbi


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pmid26039356
      J+Med+Chem 2015 ; 58 (12 ): 4883-7
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  • Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer #MMPMID26039356
  • McDonnell DP ; Wardell SE ; Norris JD
  • J Med Chem 2015[Jun]; 58 (12 ): 4883-7 PMID26039356 show ga
  • Drugs that inhibit estrogen receptor alpha (ER?) or that block the production of estrogens remain frontline interventions in the treatment and management of breast cancer at all stages. However, resistance to endocrine therapies, especially in the setting of advanced disease, remains an impediment to durable clinical responses. Although the mechanisms underlying resistance to existing agents are complex, preclinical studies suggest that selective estrogen receptor downregulators (SERDs), molecules which eliminate ER? expression, may have particular utility in the treatment of breast cancers that have progressed on tamoxifen and/or aromatase inhibitors. The discovery and development of orally bioavailable SERDs provide the opportunity to evaluate the utility of eliminating ER? expression in advanced metastatic breast cancers.
  • |*Drug Discovery [MESH]
  • |Animals [MESH]
  • |Antineoplastic Agents, Hormonal/*chemistry/pharmacology [MESH]
  • |Aromatase Inhibitors/chemistry/pharmacology [MESH]
  • |Breast Neoplasms/*drug therapy/metabolism [MESH]
  • |Breast/drug effects/metabolism [MESH]
  • |Estrogen Receptor alpha/*metabolism [MESH]
  • |Female [MESH]
  • |Humans [MESH]
  • |Selective Estrogen Receptor Modulators/*chemistry/pharmacology [MESH]


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