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首页> 外文期刊>Current topics in medicinal chemistry >Estrogen receptors as therapeutic targets in breast cancer.
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Estrogen receptors as therapeutic targets in breast cancer.

机译：雌激素受体作为乳腺癌的治疗靶标。

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The estrogen receptor alpha (ERalpha) has proven to be the single most important target in breast cancer over the last 30 years. The use of the selective ER modulator (SERM) tamoxifen for the treatment and prevention of breast cancer has changed therapeutics. The SERM raloxifene, approved for the treatment of osteoporosis, lacks tamoxifen's increased risk for endometrial cancer and is being evaluated for the prevention of breast cancer. Other SERMs approved or under development for use against breast cancer or osteoporosis include toremifene, GW5638, GW7604 (the active metabolite of GW5638), idoxifene, lasofoxifene, arzoxifene, bazedoxifene, EM-800 and acolbifene (the active metabolite of EM-800). Aromatase inhibitors (AIs) have recently proven to be more efficacious than tamoxifen as first-line therapy, efficacious for second-line therapy (e.g. against tamoxifen-resistant disease), and useful for extended adjuvant therapy after tamoxifen. The AIs include the non-steroidal agents letrozole and anastrole, and the steroidal agent exemestane. The pure antiestrogen fulvestrant has proven to be just as effective as AIs. Other pure antiestrogens, ZK-703, ZK-253, RU 58668 and TAS-108 show great promise. The development of resistance to endocrine therapy remains a clinically important problem, and laboratory models based on human breast cancer cells grown as tumors in immune-compromised mice have led to important insights into this problem. Progesterone receptor-negative status of ER-positive breast cancers may reflect altered growth factor receptor signaling, and helps to explain why this subclass of tumors exhibits lower response rates to tamoxifen compared to cancers typed progesterone receptor-positive. Crosstalk among plasma membrane-localized ER, growth factor receptor signaling, and nuclear-localized ER provide further insights into antihormonal-resistant breast cancer.
机译：在过去30年中，雌激素受体α（ERalpha）已被证明是乳腺癌中最重要的目标。选择性ER调节剂（SERM）他莫昔芬用于治疗和预防乳腺癌的用途已经改变了治疗方法。已批准用于治疗骨质疏松症的SERM雷洛昔芬缺乏他莫昔芬增加的子宫内膜癌风险，并且正在评估其预防乳腺癌的能力。已批准或正在开发用于抗乳腺癌或骨质疏松症的其他SERM，包括托瑞米芬，GW5638，GW7604（GW5638的活性代谢产物），伊多昔芬，拉索昔芬，阿佐昔芬，巴多昔芬，EM-800和阿可比芬（EM-800的活性代谢产物）。芳香酶抑制剂（AIs）最近已被证明比他莫昔芬更有效作为一线治疗，对二线治疗有效（例如抗他莫昔芬耐药性疾病），并且可用于他莫昔芬后的扩展辅助治疗。认可机构包括非甾体类药物来曲唑和茴香醚，以及甾体类药物依西美坦。事实证明，纯抗雌激素充填剂与AI一样有效。其他纯的抗雌激素药ZK-703，ZK-253，RU 58668和TAS-108前景广阔。对内分泌治疗的抵抗力的发展仍然是一个临床上重要的问题，基于人类乳腺癌细胞生长的免疫细胞受损小鼠的实验室模型已经导致对该问题的重要见解。 ER阳性乳腺癌的孕酮受体阴性状态可能反映了生长因子受体信号的改变，并有助于解释为什么与亚型孕激素受体阳性的癌症相比，该亚类肿瘤对他莫昔芬的反应率较低。质膜定位的ER，生长因子受体信号传导和核定位的ER之间的串扰为抗激素耐药性乳腺癌提供了进一步的见解。

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