ABCG2 transports Cipro from intestinal cell to extracellular space

Stable Identifier
Reaction [transition]
Homo sapiens
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Inhibition studies with Caco-2 cells show there may be a number of transport proteins involved in the transport of ciprofloxacin (Cipro) through GI cells (Cavet et al, 1997). Secretion of Cipro into the GI lumen involves two distinct transport steps: at the basolateral cell membrane, Cipro is accumulated within the cytosol, with secretion then occurring across the apical membrane (Lowes & Simmons, 2002; Xia et al, 2005; Haslam et al, 2011; reviewed by Alvarez et al, 2008). The importance of this process relative to the main excretion pathways (renal and biliary) is unclear, however.
Literature References
PubMed ID Title Journal Year
11877335 Multiple pathways for fluoroquinolone secretion by human intestinal epithelial (Caco-2) cells

Lowes, S, Simmons, NL

Br J Pharmacol 2002
15716365 Expression, localization, and functional characteristics of breast cancer resistance protein in Caco-2 cells

Gan, LS, Xia, CQ, Yang, D, Liu, N, Miwa, G

Drug Metab Dispos 2005
9283689 Fluoroquinolone (ciprofloxacin) secretion by human intestinal epithelial (Caco-2) cells

Simmons, NL, Cavet, ME, West, M

Br J Pharmacol 1997
18200507 Fluoroquinolone efflux mediated by ABC transporters

Molina, AJ, Alvarez, AI, Prieto, JG, Merino, G, Real, R, PĂ©rez, M

J Pharm Sci 2008
21930826 Intestinal ciprofloxacin efflux: the role of breast cancer resistance protein (ABCG2)

O'Reilly, DA, Simmons, NL, Sherlock, DJ, Haslam, IS, Coleman, T, Wright, JA

Drug Metab Dispos 2011
Catalyst Activity

ATPase-coupled transmembrane transporter activity of ABCG2 tetramer [apical plasma membrane ]

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