Jameera Begam A, Jubie S, Nanjan M J
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Udhagamandalam, India; A Constituent College of JSS University, Mysore, India.
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Udhagamandalam, India; A Constituent College of JSS University, Mysore, India.
Bioorg Chem. 2017 Apr;71:257-274. doi: 10.1016/j.bioorg.2017.02.011. Epub 2017 Feb 23.
Estrogens display intriguing tissue selective action that is of great biomedical importance in the development of optimal therapeutics for the prevention and treatment of breast cancer. There are also strong evidences to show that both endogenous and exogenous estrogens are involved in the pathogenesis of breast cancer. Tamoxifen has been the only drug of choice for more than 30years to treat patients with estrogen related (ER) positive breast tumors. There is a need therefore, for identifying newer, potential and novel candidates for breast cancer. Keeping this in view, the present review focuses on selective estrogen receptor modulators and estrogen antagonists such as sulfatase and aromatase inhibitors involved in breast cancer therapy. A succinct and critical overview of the structure of estrogen receptors, their signaling and involvement in breast carcinogenesis are herein described.
雌激素表现出引人关注的组织选择性作用，这在开发预防和治疗乳腺癌的最佳疗法方面具有重大生物医学意义。也有强有力的证据表明，内源性和外源性雌激素都参与了乳腺癌的发病机制。在过去30多年里，他莫昔芬一直是治疗雌激素相关（ER）阳性乳腺肿瘤患者的唯一首选药物。因此，有必要确定治疗乳腺癌的更新颖、有潜力和新颖的候选药物。鉴于此，本综述重点关注参与乳腺癌治疗的选择性雌激素受体调节剂以及雌激素拮抗剂，如硫酸酯酶和芳香化酶抑制剂。本文简要且批判性地概述了雌激素受体的结构、其信号传导以及在乳腺癌发生中的作用。
