Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
11 Jun 2020
11 Jun 2020
Historique:
received:
21
11
2019
accepted:
07
05
2020
entrez:
20
6
2020
pubmed:
20
6
2020
medline:
20
6
2020
Statut:
epublish
Résumé
TGF-β has been a target of interest for the treatment of fibrotic diseases and certain cancers. Approaches to target TGF-β include antagonists of the active ligand or TGF-β receptor kinase activity. These approaches have failed in clinical trials due to a lack of effectiveness and a limited therapeutic window. In this context, newer and more selective approaches to target TGF-β are needed. We previously reported that the matricellular protein, thrombospondin 1, activates the latent TGF-β complex and that antagonism of this pathway using tri/tetrapeptides in various animal models reduces fibrosis. The tripeptide, SRI-31277 (
Identifiants
pubmed: 32550992
doi: 10.1021/acsmedchemlett.9b00540
pmc: PMC7294719
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1130-1136Subventions
Organisme : NIDDK NIH HHS
ID : P30 DK079626
Pays : United States
Informations de copyright
Copyright © 2020 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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