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Author Spotlight: A Bicelle Crystallization Setup for ABC Transporter Membrane Proteins to Advance Drug Development
Published on: August 25, 2023
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ABC Family Transporters
1China Pharmaceutical University, Nanjing, China. xdliu@cpu.edu.cn.
Advances in Experimental Medicine and Biology
|October 2, 2019
Summary
ATP-binding cassette (ABC) transporters are crucial for molecule transport across cell membranes. This review details their roles in drug resistance, cellular functions, and associated diseases, highlighting key transporters like P-GP, BCRP, and MRPs.
Area of Science:
- Molecular Biology
- Cell Biology
- Biochemistry
Background:
- ATP-binding cassette (ABC) transporters are a large family of membrane proteins essential for cellular function.
- Over 40 human ABC transporters exist, categorized into 7 subfamilies (ABCA-ABCG).
- At least 11 ABC transporters, including P-glycoprotein (P-GP/ABCB1), multidrug resistance-associated proteins (MRPs/ABCCs), and breast cancer resistance protein (BCRP/ABCG2), are implicated in multidrug resistance (MDR).
Purpose of the Study:
- To provide a comprehensive overview of ABC transporter function and expression.
- To discuss the substrates, inhibitors, and clinical significance of key ABC transporters.
- To highlight the involvement of ABC transporters in drug disposition and human diseases.
Main Methods:
- Review of existing literature on ABC transporter structure, function, and genetics.
- Analysis of gene structure, amino acid sequence, domain organization, and phylogenetic relationships.
- Examination of expression patterns in various human tissues (liver, intestine, kidney, brain).
Main Results:
- ABC transporters play critical roles in drug absorption, distribution, and excretion.
- Dysfunctional ABC transporters are linked to various diseases, including cystic fibrosis and certain liver and retinal disorders.
- Specific ABC transporters like P-GP, BCRP, and MRPs are central to multidrug resistance development.
Conclusions:
- ABC transporters are vital for maintaining cellular homeostasis and organismal health.
- Understanding ABC transporter mechanisms is crucial for developing effective therapeutic strategies against MDR and related diseases.
- Mutations in ABC transporters can lead to significant human pathologies, underscoring their clinical importance.
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