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Updated: Aug 24, 2025
Author Spotlight: A Bicelle Crystallization Setup for ABC Transporter Membrane Proteins to Advance Drug Development
Published on: August 25, 2023
Implication of ABC transporters in non-proliferative diseases
Tatyana A Grigoreva1, Aleksandra V Sagaidak1, Daria S Novikova1
1Laboratory of Molecular Pharmacology, St. Petersburg State Institute of Technology (Technical University), Moskovskii pr., 26, St. Petersburg, 190013, Russia.
Abstract:
ABC transporters play an essential role in the development of multidrug resistance and thus are of interest in the context of anticancer therapy. However, MDR1, BCRP and MRP1 are involved in a number of key processes that maintain the viability of the body as a whole, as well as individual organs and cells. These transporters support protective properties of anatomical and histohematic barriers, determining the entry of both toxins and drugs into organs and tissues, as well as facilitating their elimination. This review discusses the main areas in which the use of modulators of the ABC exporter activity may be relevant due to either an initial imbalance in their activity or the need for the temporary change in the efflux rate for therapeutic purposes. Controlled modulation of the activity of the ABC family efflux transporters opens up broad prospects in the treatment of various diseases associated both with universal difficulties in the delivery of drugs that are transporter substrates and with the characteristics of individual patients caused by single nucleotide polymorphisms. Both activators and inhibitors of the transporters will find their application.
Insights
Modulating ATP-binding cassette (ABC) transporters, like MDR1, BCRP, and MRP1, is crucial for cancer therapy. Their controlled activity can overcome drug resistance and improve treatment for various diseases.
Area of Science:
- Biochemistry
- Pharmacology
- Molecular Biology
Background:
- ATP-binding cassette (ABC) transporters are vital for cellular and organ viability.
- These transporters maintain protective barriers, influencing toxin and drug entry and elimination.
- Multidrug resistance (MDR) development involves key ABC transporters such as MDR1, BCRP, and MRP1.
Purpose of the Study:
- To review the therapeutic potential of modulating ABC transporter activity.
- To explore applications where altering efflux rates is beneficial for treatment.
- To discuss the role of ABC transporter modulators in overcoming drug delivery challenges.
Main Methods:
- Literature review of ABC transporter function and modulation.
- Analysis of therapeutic strategies involving ABC transporter activators and inhibitors.
- Examination of the impact of single nucleotide polymorphisms on transporter activity.
Main Results:
- ABC transporter modulators show promise in treating diseases with efflux-related drug delivery issues.
- Controlled modulation can address both general drug delivery challenges and patient-specific genetic variations.
- Both activators and inhibitors of ABC transporters are identified as potential therapeutic agents.
Conclusions:
- Targeting ABC transporters offers a promising avenue for enhancing anticancer therapy and treating other diseases.
- Modulating ABC transporter activity can personalize drug delivery based on individual genetic profiles.
- Further research into ABC transporter modulators will expand therapeutic options for various conditions.
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