Title : Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid.

Pub. Date : 2009 Jul 15

PMID : 19567673






5 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 Topotecan is a substrate of the ATP-binding cassette transporters P-glycoprotein (P-gp/MDR1) and breast cancer resistance protein (BCRP). Topotecan ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
2 Topotecan is a substrate of the ATP-binding cassette transporters P-glycoprotein (P-gp/MDR1) and breast cancer resistance protein (BCRP). Topotecan ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
3 Preferential active transport of topotecan lactone over topotecan carboxylate was shown in vivo by vCSF lactone-to-carboxylate area under the curve ratios for wild-type, Mdr1a/b(-/-), Bcrp1(-/-), and Mdr1a/b(-/-)Bcrp1(-/-) mice of 5.69 +/- 0.83, 3.85 +/- 0.64, 3.61 +/- 0.46, and 0.78 +/- 0.19, respectively. Topotecan ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
4 Preferential active transport of topotecan lactone over topotecan carboxylate was shown in vivo by vCSF lactone-to-carboxylate area under the curve ratios for wild-type, Mdr1a/b(-/-), Bcrp1(-/-), and Mdr1a/b(-/-)Bcrp1(-/-) mice of 5.69 +/- 0.83, 3.85 +/- 0.64, 3.61 +/- 0.46, and 0.78 +/- 0.19, respectively. Topotecan ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
5 Our results suggest that Bcrp1 and P-gp transport topotecan into vCSF and out of brain parenchyma through the blood-brain barrier. Topotecan ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus