Unlocking estrogen receptor: Structural insights into agonists and antagonists for glioblastoma therapy.
Adv Protein Chem Struct Biol
; 142: 1-24, 2024.
Article
em En
| MEDLINE
| ID: mdl-39059983
ABSTRACT
Glioblastoma (GBM), a malignant brain tumor originating in glial cells, is one of the most common primary brain malignancies, affecting one in 100,000 people, typically in the frontal lobe. Estrogens, like estradiol-17 (E2), significantly influence GBM progression, metastasis, and angiogenesis. Estrogen receptors (ERs) are crucial in signal transduction and physiology, making them potential therapeutic targets. However, their roles in GBM pathogenesis remain unclear. This review explores ERs in GBM, focusing on their involvement in tumor immune evasion, modulation of the tumor microenvironment, and the mechanisms underlying GBM progression. Additionally, therapeutic opportunities targeting ERs for GBM treatment are discussed. Estrogen, synthesized primarily in ovaries and in smaller amounts by adrenal glands and fat tissues, regulates reproductive systems, bone density, skin health, and cardiovascular function. The invasive nature and heterogeneity of GBM complicate therapy development. Preclinical findings suggest that endocrine therapy with hormone receptor agonists or antagonists can extend patient survival and improve post-treatment quality of life. The ERß pathway, in particular, shows tumor-suppressive potential, limiting glioma progression with fewer side effects. ERß agonists could become a novel drug class for GBM treatment. Identifying biomarkers and specific therapeutic targets is crucial for early detection and improved prognosis. Estrogen and its receptors are advantageous for GBM treatment due to their regulation of numerous biological processes, ability to penetrate the blood-brain barrier, and genomic and non-genomic control of transcription, making them promising targets for GBM therapy.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
/
Tipos_de_cancer
/
Outros_tipos
Base de dados:
MEDLINE
Assunto principal:
Neoplasias Encefálicas
/
Receptores de Estrogênio
/
Glioblastoma
Limite:
Humans
Idioma:
En
Revista:
Adv Protein Chem Struct Biol
Assunto da revista:
BIOLOGIA
/
BIOQUIMICA
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Índia