ArticleFrontiers in drug delivery2024
Induction of P-glycoprotein overexpression in brain endothelial cells as a model to study blood-brain barrier efflux transport.
Article in Frontiers in drug delivery, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- The Role of Hydrogen Bond Donors and Intramolecular Hydrogen Bonding in Modulating Blood-Brain Barrier Permeability: Implications for CNS Drug Design.Molecules (Basel, Switzerland) · 2026Review
- Nanotechnology for efficient delivery of TCM active ingredients in treating brain diseases.Materials today. Bio · 2026Review
- Modeling Blood-Brain Barrier Efflux Transport Using a Breast Cancer Resistance Protein Overexpression Cell Line.Biomedicines · 2026Article
- Nanocarrier Strategies in Glioblastoma: Overcoming Barriers to Effective Brain Tumor Therapy.AAPS PharmSciTech · 2025Review
- Reversing Morphine Induced Tolerance: Insights Into Cetirizine and Green Tea Extract Efficacy.Current therapeutic research, clinical and experimental · 2025Article
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Authors and funding
7 authors.
Funding
Abstract
The blood-brain barrier (BBB) is comprised of specialized brain endothelial cells (BECs) that contribute to maintaining central nervous system (CNS) homeostasis. BECs possess properties such as an array of multi-drug efflux transporters that eject various drugs and toxins, preventing their entry into the CNS. Together, it is estimated that these efflux transporters can eject up to 98% of known xenobiotic compounds. P-glycoprotein (P-gp) is a promiscuous efflux transporter at the BBB and can efflux up to 90 various substrates, representing a major hurdle in CNS drug delivery for therapeutic interventions. This necessitates the study of P-gp to discover drugs that are non-substrates of P-gp as well as to identify novel P-gp inhibitors. Here we report the generation of P-gp overexpressing BECs under the endogenous promoter control that could be used in the screening of P-gp substrates. These cells could provide utility in the design of drugs or identification of novel inhibitors.
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