A Structure-Based View on ABC-Transporter Linked to Multidrug Resistance

The discovery of the first ATP-binding cassette (ABC) transporter, whose overexpression in cancer cells is responsible for exporting anticancer drugs out of tumor cells, initiated enormous efforts to overcome tumor cell multidrug resistance (MDR) by inhibition of ABC-transporter. Because of its many physiological functions, diverse studies have been conducted on the mechanism, function and regulation of this important group of transmembrane transport proteins. In this review, we will focus on the structural aspects of this transporter superfamily. Since the resolution revolution of electron microscope, experimentally solved structures increased rapidly. A summary of the structures available and an overview of recent structure-based studies are provided. More specifically, the artificial intelligence (AI)-based predictions from AlphaFold-2 will be discussed.

Automated summary

The discovery of the first ATP-binding cassette (ABC) transporter has led to extensive research efforts in overcoming tumor cell multidrug resistance (MDR) by inhibiting the ABC-transporter. This review focuses on the structural aspects of this important group of transmembrane transport proteins and includes a summary of available structures and recent structure-based studies. The use of artificial intelligence (AI) predictions from AlphaFold-2 is also discussed.