HDAC Inhibitors: Innovative Strategies for Their Design and Applications.

dc.centroUniversidad San Pablo-CEU
dc.contributor.authorDasko, Mateusz
dc.contributor.authorRamos González, Ana María
dc.contributor.authorCoderch Boué, Claire
dc.contributor.authorPascual-Teresa Fernández, Beatriz de
dc.date2022
dc.date.accessioned2022-02-15T05:00:18Z
dc.date.available2022-02-15T05:00:18Z
dc.date.issued2022-02-15
dc.descriptionMolecules, e-ISSN 1420-3049, 2022, 27, 715
dc.description.abstractHistone 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).en_EN
dc.formatapplication/pdf
dc.identifier000000726410
dc.identifier.doihttps://doi.org/10.3390/molecules27030715
dc.identifier.urihttp://hdl.handle.net/10637/13385
dc.language.isoen
dc.relationThis research was funded by MINECO/FEDER, UE, grant number RTI2018-093539-B-I00. M.D. was supported by a fellowship in the Bekker programme (PPN/BEK/2020/1/00096/U/00001), funded by the Polish National Agency for Academic Exchange.en_EN
dc.rightsopen access
dc.rights.cchttps://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subjectHistone deacetylases (HDACs)en_EN
dc.subjectPROTACsen_EN
dc.subjectFolate conjugatesen_EN
dc.subjectPositron emission tomography (PET)en_EN
dc.subjectFluorescent probesen_EN
dc.subjectDendrimersen_EN
dc.subjectNanoparticlesen_EN
dc.titleHDAC Inhibitors: Innovative Strategies for Their Design and Applications.
dc.typeArtículo
dspace.entity.typePublicationes
relation.isAuthorOfPublicationac3c2128-fa85-4881-a056-bbeb0e359a4b
relation.isAuthorOfPublicationb53fd6d8-f048-4aae-b7ee-4114407db5f2
relation.isAuthorOfPublicationd7fb1206-a4e0-4fe5-8508-38114fa5bbcf
relation.isAuthorOfPublication.latestForDiscoveryac3c2128-fa85-4881-a056-bbeb0e359a4b

Files

Original bundle

Now showing 1 - 1 of 1
Thumbnail Image
Name:
HDAC_Dasko_et_al_Molecules_2022.pdf
Size:
993.89 KB
Format:
Adobe Portable Document Format