ABC Transporter Related Drug Discovery Products
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
ATP-binding cassette (ABC) transporters comprise a large and diverse family of membrane proteins that play essential roles in the transport of various substrates across cellular membranes. These proteins utilize the energy derived from ATP hydrolysis to facilitate the movement of molecules, including ions, lipids, peptides, and xenobiotics. Owing to their involvement in numerous physiological processes, ABC transporters have become an area of significant research interest, particularly in the fields of drug discovery and pharmacology.
Creative Biolabs offers a range of ABC transporter tools with our well-established high-efficient drug discovery strategy in a timely and cost-effective manner:
Overview of ABC Transporter
(ABC transporters are widely distributed across all living organisms, from bacteria to humans. In humans, there are 48 identified ABC transporter genes, divided into seven subfamilies (ABCA to ABCG). The primary structure of ABC transporters typically consists of two transmembrane domains (TMDs), responsible for substrate recognition and binding, and two nucleotide-binding domains (NBDs), which bind and hydrolyze ATP to provide energy for substrate translocation. Although the overall architecture is conserved, the individual transporters exhibit considerable diversity in substrate specificity, which enables them to participate in a broad range of biological processes.
Key Subfamilies and Members of Human ABC Transporters:
ABCA: This subfamily primarily focuses on the transport of lipids, playing crucial roles in cholesterol homeostasis and lipid metabolism. For instance, ABCA1 is involved in high-density lipoprotein (HDL) biogenesis, while ABCA4 mediates retinoid transport in the retina.
ABCB: This subfamily includes the well-known multidrug resistance protein 1 (MDR1/ABCB1 or P-glycoprotein), which exports a wide range of structurally diverse compounds, including therapeutic drugs. This efflux activity contributes to drug resistance in cancer and influences drug pharmacokinetics.
ABCC: ABCC subfamily members are involved in various physiological processes, such as ion transport, detoxification, and drug resistance. For example, ABCC1 (multidrug resistance-associated protein 1, MRP1) participates in xenobiotic export, while CFTR (ABCC7) mediates chloride ion transport in epithelial cells.
ABCD: This subfamily is responsible for the transport of long-chain and very long-chain fatty acids into peroxisomes. Dysfunction in ABCD1, for example, is associated with X-linked adrenoleukodystrophy, a neurodegenerative disorder.
ABCE and ABCF: These subfamilies lack TMDs and are not involved in transmembrane transport. Instead, they participate in diverse cellular processes, such as ribosome biogenesis and translation regulation.
ABCG: The ABCG subfamily includes the sterol transporters ABCG5 and ABCG8, which function together in regulating dietary cholesterol absorption and hepatic sterol excretion.
ABC Transporter Drug Discovery
Given their involvement in substrate transport, including endogenous molecules and xenobiotics, ABC transporters represent attractive targets for drug discovery. Modulation of these transporters could potentially improve drug pharmacokinetics, overcome drug resistance in cancer, or ameliorate diseases caused by transporter dysfunction. However, developing effective and selective modulators of ABC transporters remains a challenge due to their diverse substrate specificity and overlapping functions. Further research into the structural and functional properties of these transporters will be critical in advancing the development of novel therapeutic strategies.
References
- Locher, K. Mechanistic diversity in ATP-binding cassette (ABC) transporters. Nature Structural & Molecular Biology. 2016, 23: 487-493.
- Adamska, A.; Falasca, M. ATP-binding cassette transporters in progression and clinical outcome of pancreatic cancer: What is the way forward? World Journal of Gastroenterology. 2018, 24(29): 3222-3238.
