The small-molecule protein ligand interface stabiliser E7820 induces differential cell line specific responses of integrin α2 expression.

ABSTRACT:

Background

The mechanism of small-molecule stabilised protein-protein interactions is of growing interest in the pharmacological discovery process. A plethora of different substances including the aromatic sulphonamide E7820 have been identified to act by such a mechanism. The process of E7820 induced CAPERα degradation and the resultant transcriptional down regulation of integrin α2 expression has previously been described for a variety of different cell lines and been made responsible for E7820's antiangiogenic activity. Currently the application of E7820 in the treatment of various malignancies including pancreas carcinoma and breast cancer is being investigated in pre-clinical and clinical trials. It has been shown, that integrin α2 deficiency has beneficial effects on bone hom

SUBMITTER: Hulskamp MD 

PROVIDER: S-EPMC8132423 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature