Differential Effects of the Oncogenic BRAF Inhibitor PLX4032 (Vemurafenib) and its Progenitor PLX4720 on ABCB1 Function

• Main Authors: Martin Michaelis (Author), Florian Rothweiler (Author), Thomas Nerreter (Author), Marijke van Rikxoort (Author), Mohsen Sharifi (Author), Michael Wiese (Author), Taravat Ghafourian (Author), Jindrich Cinatl (Author)
• Format: Book
• Published: Frontiers Media S.A., 2014-04-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

PURPOSE: The clinically approved oncogenic BRAF inhibitor PLX4032 (vemurafenib) was shown to be a substrate of the ATP-binding cassette (ABC) transporter ABCB1. Here, we compared PLX4032 and its structurally closely related precursor compound PLX4720 for their interference with ABCB1 and the ABCB1-m...