Drug Repurposing: Deferasirox Inhibits the Anti-Apoptotic Activity of Mcl-1.

ABSTRACT:

Introduction

With the aim of repositioning commercially available drugs for the inhibition of the anti-apoptotic myeloid cell leukemia protein, Mcl-1, implied in various cancers, five molecules, highlighted from a published theoretical screening, were selected to experimentally validate their affinity toward Mcl-1.

Results

A detailed NMR study revealed that only two of the five tested drugs, Torsemide and Deferasirox, interacted with Mcl-1. NMR data analysis allowed the complete characterization of the binding mode of both drugs to Mcl-1, including the estimation of their affinity for Mcl-1. Biological assays evidenced that the biological activity of Torsemide was lower as compared to the Deferasirox, which was able to efficiently and selectively inhibit the anti-apoptotic a

SUBMITTER: Bourafai-Aziez A 

PROVIDER: S-EPMC8688747 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature