Dihydroergotamine ameliorates liver fibrosis by targeting transforming growth factor β type II receptor.

ABSTRACT:

Background

The transforming growth factor β (TGFβ) signaling pathway plays a crucial role in the development of liver fibrosis by activating TGFβ type II receptor (TGFβR2), followed by the recruitment of TGFβR1 finally triggering downstream signaling pathway.

Aim

To find drugs targeting TGFβR2 that inhibit TGFβR1/TGFβR2 complex formation, theoretically inhibit TGFβ signaling pathway, and thereby ameliorate liver fibrosis.

Methods

Food and Drug Administration-approved drugs were screened for binding affinity with TGFβR2 by virtual molecular docking. We identified 6 candidates and further explored their potential by Cell Counting Kit-8 (CCK-8) cell cytotoxic experiment to validate toxicity and titrated the best cellular working concentrations. Next, we further demonstra

SUBMITTER: Zheng KX 

PROVIDER: S-EPMC10280794 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature