دورية أكاديمية
A Therapeutic Perspective of HDAC8 in Different Diseases: An Overview of Selective Inhibitors
| العنوان: | A Therapeutic Perspective of HDAC8 in Different Diseases: An Overview of Selective Inhibitors |
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| المؤلفون: | Anna Fontana, Ilaria Cursaro, Gabriele Carullo, Sandra Gemma, Stefania Butini, Giuseppe Campiani |
| المصدر: | International Journal of Molecular Sciences, Vol 23, Iss 17, p 10014 (2022) |
| بيانات النشر: | MDPI AG, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Biology (General) LCC:Chemistry |
| مصطلحات موضوعية: | histone deacetylase, HDAC8, HDAC8 inhibitor, fibrosis, cancer, polypharmacology, Biology (General), QH301-705.5, Chemistry, QD1-999 |
| الوصف: | Histone deacetylases (HDACs) are epigenetic enzymes which participate in transcriptional repression and chromatin condensation mechanisms by removing the acetyl moiety from acetylated ε-amino group of histone lysines and other non-histone proteins. In recent years, HDAC8, a class I HDAC, has emerged as a promising target for different disorders, including X-linked intellectual disability, fibrotic diseases, cancer, and various neuropathological conditions. Selective HDAC8 targeting is required to limit side effects deriving from the treatment with pan-HDAC inhibitors (HDACis); thus, many endeavours have focused on the development of selective HDAC8is. In addition, polypharmacological approaches have been explored to achieve a synergistic action on multi-factorial diseases or to enhance the drug efficacy. In this frame, proteolysis-targeting chimeras (PROTACs) might be regarded as a dual-targeting approach for attaining HDAC8 proteasomal degradation. This review highlights the most relevant and recent advances relative to HDAC8 validation in various diseases, providing a snapshot of the current selective HDAC8is, with a focus on polyfunctional modulators. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1422-0067 1661-6596 |
| Relation: | https://www.mdpi.com/1422-0067/23/17/10014; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067 |
| DOI: | 10.3390/ijms231710014 |
| URL الوصول: | https://doaj.org/article/f5b6f32a35a74aa997a5942e4d94c1ab |
| رقم الأكسشن: | edsdoj.f5b6f32a35a74aa997a5942e4d94c1ab |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 14220067 16616596 |
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| DOI: | 10.3390/ijms231710014 |