HDAC Inhibitors: Innovative Strategies for Their Design and Applications

Mateusz Daśko; Beatriz De Pascual-Teresa; Irene Ortín; Ana Ramos

doi:10.3390/molecules27030715

HDAC Inhibitors: Innovative Strategies for Their Design and Applications

Abstrakt

Histone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs and imaging agents that facilitate an early diagnosis of these diseases. Thus, their selective inhibition or degradation are the basis for new therapies. This is supported by the fact that many HDAC inhibitors (HDACis) are currently under clinical research for cancer therapy, and the Food and Drug Administration (FDA) has already approved some of them. In this review, we will focus on the recent advances and latest discoveries of innovative strategies in the development and applications of compounds that demonstrate inhibitory or degradation activity against HDACs, such as PROteolysis-TArgeting Chimeras (PROTACs), tumor-targeted HDACis (e.g., folate conjugates and nanoparticles), and imaging probes (positron emission tomography (PET) and fluorescent ligands).

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Autorzy (4)

Mateusz Daśko dr inż.
Beatriz De Pascual-Teresa
Irene Ortín
Ana Ramos

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Wersja publikacji: Accepted albo Published Version
DOI:: Cyfrowy identyfikator dokumentu elektronicznego (otwiera się w nowej karcie) 10.3390/molecules27030715
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Kategoria:

Publikacja w czasopiśmie

Typ:

artykuły w czasopismach

Opublikowano w:

MOLECULES nr 27,
ISSN: 1420-3049

Język:

angielski

Rok wydania:

2022

Opis bibliograficzny:

Daśko M., De Pascual-Teresa B., Ortín I., Ramos A.: HDAC Inhibitors: Innovative Strategies for Their Design and Applications// MOLECULES -Vol. 27,iss. 3 (2022), s.715-

DOI: