Segura-Uribe Julia J, Pinto-Almazán Rodolfo, Coyoy-Salgado Angélica, Fuentes-Venado Claudia E, Guerra-Araiza Christian
Unidad de Investigación Médica en Enfermedades Neurológicas, Hospital de Especialidades, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Mexico City, Mexico.
Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Mexico City, Mexico.
Neural Regen Res. 2017 Aug;12(8):1231-1240. doi: 10.4103/1673-5374.213536.
Estrogen receptor modulators are compounds of interest because of their estrogenic agonistic/antagonistic effects and tissue specificity. These compounds have many clinical applications, particularly for breast cancer treatment and osteoporosis in postmenopausal women, as well as for the treatment of climacteric symptoms. Similar to estrogens, neuroprotective effects of estrogen receptor modulators have been described in different models. However, the mechanisms of action of these compounds in the central nervous system have not been fully described. We conducted a systematic search to investigate the effects of estrogen receptor modulators in the central nervous system, focusing on the modulation of cytoskeletal proteins. We found that raloxifene, tamoxifen, and tibolone modulate some cytoskeletal proteins such as tau, microtuble-associated protein 1 (MAP1), MAP2, neurofilament 38 (NF38) by different mechanisms of action and at different levels: neuronal microfilaments, intermediate filaments, and microtubule-associated proteins. Finally, we emphasize the importance of the study of these compounds in the treatment of neurodegenerative diseases since they present the benefits of estrogens without their side effects.
雌激素受体调节剂因其雌激素激动/拮抗作用和组织特异性而备受关注。这些化合物有许多临床应用，特别是用于治疗绝经后女性的乳腺癌和骨质疏松症，以及缓解更年期症状。与雌激素类似，在不同模型中已描述了雌激素受体调节剂的神经保护作用。然而，这些化合物在中枢神经系统中的作用机制尚未完全阐明。我们进行了一项系统检索，以研究雌激素受体调节剂在中枢神经系统中的作用，重点关注细胞骨架蛋白的调节。我们发现雷洛昔芬、他莫昔芬和替勃龙通过不同的作用机制和在不同水平（神经元微丝、中间丝和微管相关蛋白）调节一些细胞骨架蛋白，如tau、微管相关蛋白1（MAP1）、MAP2、神经丝38（NF38）。最后，我们强调研究这些化合物在治疗神经退行性疾病中的重要性，因为它们具有雌激素的益处而无其副作用。
