Our promise to you:
Guaranteed product quality, expert customer support.
24x7 CUSTOMER SERVICE
CONTACT US TO ORDER
ATP-binding cassette (ABC) transporters are transmembrane proteins that act as drug efflux pumps and are associated with multi-drug resistance (MDR) in cancer. Two specific proteins that belong to this protein superfamily are P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). ABC transporters have a wide range of functions, including transporting a variety of biological molecules and protecting cells from endogenous and exogenous toxins. Efflux pumps from the ABC transporter family can also be expressed by the tumor cells themselves, leading to the development of intrinsic chemoresistance. Therefore, the study of ABC transporters is expected to be helpful in the drug development process.
Stable cell lines are important tools for drug screening, gene function studies, or protein production. Stable cell lines represent a homogeneous population, generated from selected clones, and maintain stable expression of the target protein over generations. With decades of experience in cell line engineering and drug discovery, Creative Biogene has accessioned a large collection of cell lines that possess overexpression ABC transporters. The use of these cell lines allows for a broad set of assays and reduced assay development time.
Key Features of Our ABC Transporter Stable Cell Lines
ABC transporters are expressed by a variety of cell types and have been implicated in drug resistance in some cancer cells. In the brain, they are expressed by microglia, astrocytes, neurons, pericytes, and endothelial cells. Endothelial cells participate in the normal function of the blood-brain barrier (BBB), primarily expressing ABCB1 (P-gp) and ABCG2 (BCRP) to efflux xenobiotics from the brain parenchyma into the bloodstream. In addition, many ABC transporters are involved in cellular metabolism and/or transport of biologic molecules.
Figure 1. Example of a 3-MSDs transporter. (Muriithi W, et al. Cancer biology & medicine, 2020)
To study the mechanisms and effects of ABC transporters, researchers developed stable cell lines that overexpress specific ABC transporters. These cell lines have proven to be valuable tools for understanding the role of ABC transporters in drug efflux and drug resistance, as well as for screening potential drug candidates and assessing their susceptibility to transporter-mediated efflux.
Applications for ABC transporter stable cell lines include:
Case Study 1
Amphotericin B (AmB) belongs to a group of polyene antibiotics commonly used to treat systemic fungal infections. Several ABC transporters, including ABCA1, play critical roles in lipid translocation, cholesterol redistribution, and efflux. Here, researchers propose a novel mechanism of cellular resistance to AmB, in which active cholesterol efflux mediated by the ABCA1 transporter triggers the formation of large cholesterol-AmB structures on the cell surface, preventing AmB from penetrating the plasma membrane and causing cytotoxicity.
Figure 2. FLIM imaging of AmB molecular organization in ABCA1-expressing cell lines. (Wu A, et al., 2019)
Case Study 2
The frequent occurrence of multidrug resistance (MDR) resulting from overexpression of the ABC transporters ABCB1 and ABCG2 in cancer cells remains a therapeutic obstacle for scientists and clinicians. Here, researchers discover avapritinib (BLU-285) is a potent, selective, orally bioavailable tyrosine kinase inhibitor against mutant forms of KIT and platelet-derived growth factor receptor alpha (PDGFRA), can weaken the transport function of ABCB1 and ABCG2.
Figure 3. Avapritinib increases the intracellular drug accumulation in cells overexpressing ABCB1 or ABCG2. (Wu C P, et al., 2019)
Q: What are ABC transporters?
A: ABC (ATP-binding cassette) transporters are a family of membrane proteins that play a vital role in the transport of a wide variety of substances across cellular membranes. These transporters are involved in the efflux of drugs, xenobiotics, toxins, and various endogenous compounds, contributing to the regulation of intracellular concentrations of these substances.
Q: How many human genes have been identified and classified for ABC proteins?
A: To date, 48 human genes and one pseudogene (ABCC13) for ABC proteins have been identified and classified into 7 families ranging from ABCA to ABCG based on their relative sequence homology and domain organization.
Q: What are the functions of ABC transporters?
A: ABC transporters have diverse functions such as protein synthesis and DNA repair, as well as being exporters, ion channels, and non-transporters.
Q: What is the molecular structure of ABC proteins?
A: ABC proteins have a universal molecular structure. A complete transporter consists of two nucleotide-binding domains (NBD) and two or three membrane-spanning domains (MSD, also called transmembrane domains or TMDs).
Copyright © Creative Biogene. All rights reserved.