The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation
blood–brain barrier
bromodomain
epigenetics
inflammation
microvascular disease
Journal
Translational neuroscience
ISSN: 2081-3856
Titre abrégé: Transl Neurosci
Pays: Germany
ID NLM: 101550327
Informations de publication
Date de publication:
01 Jan 2023
01 Jan 2023
Historique:
received:
25
09
2023
revised:
15
12
2023
accepted:
19
12
2023
medline:
15
1
2024
pubmed:
15
1
2024
entrez:
15
1
2024
Statut:
epublish
Résumé
Brain vascular inflammation is characterized by endothelial activation and immune cell recruitment to the blood vessel wall, potentially causing a breach in the blood - brain barrier, brain parenchyma inflammation, and a decline of cognitive function. The clinical-stage small molecule, apabetalone, reduces circulating vascular endothelial inflammation markers and improves cognitive scores in elderly patients by targeting epigenetic regulators of gene transcription, bromodomain and extraterminal proteins. However, the effect of apabetalone on cytokine-activated brain vascular endothelial cells (BMVECs) is unknown. Here, we show that apabetalone treatment of BMVECs reduces hallmarks of
Identifiants
pubmed: 38222824
doi: 10.1515/tnsci-2022-0332
pii: tnsci-2022-0332
pmc: PMC10787226
doi:
Types de publication
Journal Article
Langues
eng
Pagination
20220332Informations de copyright
© 2023 the author(s), published by De Gruyter.
Déclaration de conflit d'intérêts
Conflict of interest: S.W., L.F, E.D., D.G., B.D.R., S.C.S, L.M.T., C.D.S., R.J., J.O.J., M.S., N.C.W.W., and E.K. were employed by Resverlogix Corp. at the time of the study and hold company’s shares and stock options. All other authors state no conflict of interest.