Discovery of Selective Transforming Growth Factor β Type II Receptor Inhibitors as Antifibrosis Agents.

ABSTRACT: Historically, modulation of transforming growth factor β (TGF-β) signaling has been deemed a rational strategy to treat many disorders, though few successful examples have been reported to date. This difficulty could be partially attributed to the challenges of achieving good specificity over many closely related enzymes that are implicated in distinct phenotypes in organ development and in tissue homeostasis. Recently, fresolimumab and disitertide, two peptidic TGF-β blockers, demonstrated significant therapeutic effects toward human skin fibrosis. Therefore, the selective blockage of TGF-β signaling assures a viable treatment option for fibrotic skin disorders such as systemic sclerosis (SSc). In this report, we disclose selective TGF-β type II receptor (TGF-βRII) inhibitors that exhibit

SUBMITTER: Miwa S 

PROVIDER: S-EPMC8155245 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature