![]() The C region corresponds to the DNA binding domain (DBD), contributing to the estrogen receptor dimerization. The A/B region represents the amino-terminal domain (NTD) which is involved in transcriptional transactivation of gene. ![]() ![]() The main functional domains are termed A/B, C, D, and E/F are present in both receptors’ full-length structures ( 4). These receptors bind to specific sequences in gene promoters or through mechanisms that do not involve DNA binding (genomic and non-genomic effects) ( 8).ĮRs are comprised of various domains and have several structural regions in common. Structural Diversity of Estrogen ReceptorsĮRα and ERβ are nuclear ERs, although both receptors interact with 17β- estradiol with high affinity, with the difference being in respect of the level of induction that may relate to the ligand (co-activation/repressors) ( 7). Therefore, it is important to improve this information so it can develop into potential tools for further investigation. A specific ligand can exert an agonistic effect with an affinity depending upon the ER, implicated in non-receptor tyrosine kinase (Src) activation and phosphoinositol 3-kinase (PI3K) signaling pathway ( 6). Moreover, before nuclear translocation, ligand-bound steroid hormone receptors, both AR and ER can bind to homologous or heterologous ligands in the cytoplasm and exert biological effects ( 4).ĮRs are activated by steroid hormones, such as estrogens, and mediate important physiological effects by binding to ERs ( 5). Although studies with an androgen receptor (AR) suggest that before ligand binding the receptor is located in the cytoplasm, that may in fact be a nucleus like downregulation of ERβ mRNA expression in hormone-refractory tumors, which provokes the acquisition of mesenchymal characteristics and aggressive behavior of the PCa cells ( 3) which could influence clinical symptomatic cancer and the initiation of PCa. This disease at the early stage can often be cured, however, those patients with metastasis need to undergo androgen deprivation therapy (ADT) ( 2), which progresses into a drug resistance stage, termed castration-resistant prostate cancer (CRPC). Prostate cancer (PCa), is the second leading cancer-related disease among men and the fifth leading cause of death worldwide ( 1). Finally, we also assessed the contribution of molecular simulation which can help us to search and predict potential estrogenic activities. Subsequently, the structures of the ERs and their splice variants, the binding of ligands to ERs, and the effect on PCa are provided. The expression and regulation of the estrogen receptors (ERs) ERα, ERβ, and GPER stimulated by agonists and antagonists, and related to prostate cancer cells are herein reviewed. Despite the historical use of estrogens in the pathogenesis of prostate cancer (PCa), their biological effect is not well known, nor their role in carcinogenesis or the mechanisms used to carry their therapeutic effects of neoplastic in prostate transformation. 5Departamento de Urología, Hospital de Especialidades Centro Médico Nacional de Occidente, Guadalajara, MexicoĮstrogens are hormones that have been extensively presented in many types of cancer such as breast, uterus, colorectal, prostate, and others, due to dynamically integrated signaling cascades that coordinate cellular growth, differentiation, and death which can be potentially new therapeutic targets.4Departamentos de Clínicas Quirúrgicas y Salud Pública, Centro Universitario de Ciencias de la Salud, Universidad de Guadalajara, Guadalajara, Mexico.3Centro Universitario de los Altos, Universidad de Guadalajara, Tepatitlán de Morelos, Mexico. ![]()
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