类维生素a的医学前景(综述)

Q3 Pharmacology, Toxicology and Pharmaceutics
L. V. Kovalenko, A. G. Polivanova, A. P. Ilyin, I. N. Solovieva, E. I. Gorbacheva, M. S. Oshchepkov
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引用次数: 0

摘要

介绍。类维生素a是一组内源性和合成的物质,在正常发育中调节许多重要的生物过程。新型类维生素a生物活性的合成和研究是化学生物学研究的热点。文本。类维甲酸的基因组功能是由其核受体RAR(α, β, γ)和RXR(α, β, γ)介导的,它们通过募集辅抑制因子和辅激活因子来调节基因转录。类维生素a还通过酰化蛋白质和其他生物分子而具有非基因组功能。再生医学和干细胞生物学是类维生素a生物活性研究的前沿领域。内源性和合成类维甲酸用于治疗皮肤病变和肿瘤学。有证据表明它们在治疗肺部疾病方面有潜在的用途。对特定受体和组织具有高选择性的类维生素a的开发可能为治疗和预防神经退行性疾病(如阿尔茨海默病、帕金森病等)开辟新的途径。类维生素a是免疫系统运作所必需的,是强大的免疫调节剂。此外,类维生素a具有治疗各种增生性疾病的潜力。结论。长期研究维甲酸及其结构类似物的药理活性,旨在研究和建立其作用的确切机制,以及它们参与各种疾病的发病机制。类维生素a的合成旨在设计对特定受体具有高选择性的化合物,从而排除天然调节分子的多靶点作用和相关副作用。合成类维生素a没有致畸和其他副作用,可以作为治疗代谢性疾病、各种恶性肿瘤以及肾、肺和中枢神经系统疾病的治疗剂。此外,基于类维生素a的活性分子控释前药的开发也是该药物化学领域的一个有前景的方向。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Medicinal Perspectives of Retinoids (Review)
Introduction. Retinoids are a group of endogenous and synthetic substances that regulate numerous important biological processes in normal development. The synthesis and study of the biological activity of new retinoids are a promising area of chemical biology. Text. The genomic functions of retinoids are mediated by their nuclear receptors RAR(α, β, γ) and RXR(α, β, γ), which regulate gene transcription by recruiting corepressors and coactivators. Retinoids also possess non-genomic functions by acylating proteins and other biomolecules. Regenerative medicine and stem cell biology are advanced areas of research in the biological activity of retinoids. Endogenous and synthetic retinoids are used for the treatment of skin pathologies and in oncology. There is evidence of their potential use in the therapy of lung diseases. The development of retinoids with high selectivity towards specific receptors and tissues may open new approaches to the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and others. Retinoids are necessary for the functioning of the immune system and are powerful immunomodulators. Additionally, retinoids have the potential for the therapy of various proliferative diseases. Conclusion. Long-term studies of the pharmacological activity of retinoic acid and its structural analogs aim to investigate and establish the precise mechanisms of their actions, as well as their involvement in the pathogenesis of various diseases. The synthesis of retinoids aims to design compounds with high selectivity towards specific receptors, which would exclude the multitarget action of natural regulatory molecules and the associated side effects. Synthetic retinoids devoid of teratogenic and other side effects can find application as therapeutic agents for the treatment of metabolic disorders, various malignancies, as well as kidney, lung, and CNS diseases. Furthermore, the development of prodrugs based on retinoids with controlled release of active molecules is also a promising direction in this field of medicinal chemistry.
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来源期刊
Drug Development and Registration
Drug Development and Registration Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
1.20
自引率
0.00%
发文量
61
审稿时长
8 weeks
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