Drug transport to the brain: key roles for the efflux pump P-glycoprotein in the blood-brain barrier
- PMID: 12529928
- DOI: 10.1016/s1537-1891(02)00201-x
Drug transport to the brain: key roles for the efflux pump P-glycoprotein in the blood-brain barrier
Abstract
1. The blood-brain barrier (BBB) contributes to brain homeostastis and fulfills a protective function by controlling the access of solutes and toxic substances to the central nervous system (CNS). The efflux transporter P-glycoprotein (P-gp) is a key element of the molecular machinery that confers special permeability properties to the BBB. 2. P-gp, which was initially recognized for its ability to expel anticancer drugs from multidrug-resistant cancer cells, is strongly expressed in brain capillaries. Its expression in the BBB limits the accumulation of many hydrophobic molecules and potentially toxic substances in the brain. 3. The purpose of this review is to summarize the current state of knowledge about the expression of P-gp, its cellular localization as well as its possible functions in the BBB.
Similar articles
-
P-glycoprotein-mediated efflux transport of anticancer drugs at the blood-brain barrier.Ther Drug Monit. 1998 Oct;20(5):588-90. doi: 10.1097/00007691-199810000-00024. Ther Drug Monit. 1998. PMID: 9780140 Review.
-
Multidrug resistance in brain tumors: roles of the blood-brain barrier.Cancer Metastasis Rev. 2001;20(1-2):13-25. doi: 10.1023/a:1013104423154. Cancer Metastasis Rev. 2001. PMID: 11831641 Review.
-
P-glycoprotein in blood-brain barrier endothelial cells: interaction and oligomerization with caveolins.J Neurochem. 2003 Nov;87(4):1010-23. doi: 10.1046/j.1471-4159.2003.02081.x. J Neurochem. 2003. PMID: 14622130
-
Characterisation of the brain multidrug resistance protein (BMDP/ABCG2/BCRP) expressed at the blood-brain barrier.Brain Res. 2003 May 9;971(2):221-31. doi: 10.1016/s0006-8993(03)02401-6. Brain Res. 2003. PMID: 12706238
-
Impact of Zn2+ on ABC Transporter Function in Intact Isolated Rat Brain Microvessels, Human Brain Capillary Endothelial Cells, and in Rat in Vivo.Mol Pharm. 2019 Jan 7;16(1):305-317. doi: 10.1021/acs.molpharmaceut.8b00987. Epub 2018 Nov 29. Mol Pharm. 2019. PMID: 30422662
Cited by
-
Brain endothelial cells as pharmacological targets in brain tumors.Mol Neurobiol. 2004 Oct;30(2):157-83. doi: 10.1385/MN:30:2:157. Mol Neurobiol. 2004. PMID: 15475625 Review.
-
Pathways and progress in improving drug delivery through the intestinal mucosa and blood-brain barriers.Ther Deliv. 2014 Oct;5(10):1143-63. doi: 10.4155/tde.14.67. Ther Deliv. 2014. PMID: 25418271 Free PMC article. Review.
-
Breaking barriers: Neurodegenerative repercussions of radiotherapy induced damage on the blood-brain and blood-tumor barrier.Free Radic Biol Med. 2022 Jan;178:189-201. doi: 10.1016/j.freeradbiomed.2021.12.002. Epub 2021 Dec 4. Free Radic Biol Med. 2022. PMID: 34875340 Free PMC article. Review.
-
Diesel exhaust particles induce oxidative stress, proinflammatory signaling, and P-glycoprotein up-regulation at the blood-brain barrier.FASEB J. 2008 Aug;22(8):2723-33. doi: 10.1096/fj.08-106997. Epub 2008 May 12. FASEB J. 2008. PMID: 18474546 Free PMC article.
-
Role of P-glycoprotein in limiting the brain penetration of glabridin, an active isoflavan from the root of Glycyrrhiza glabra.Pharm Res. 2007 Sep;24(9):1668-90. doi: 10.1007/s11095-007-9297-1. Epub 2007 Jun 6. Pharm Res. 2007. PMID: 17551811
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Miscellaneous