Title : Insight into the cooperation of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) at the blood-brain barrier: a case study examining sorafenib efflux clearance.

Pub. Date : 2012 Mar 5

PMID : 22335402






6 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Insight into the cooperation of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) at the blood-brain barrier: a case study examining sorafenib efflux clearance. Sorafenib ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
2 The brain efflux index method, combined with the organotypic brain slices, was used to determine the net contribution of P-gp and BCRP to the total clearance of sorafenib out of the brain and show that its efflux at the BBB is mediated primarily by BCRP. Sorafenib ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
3 The brain efflux index method, combined with the organotypic brain slices, was used to determine the net contribution of P-gp and BCRP to the total clearance of sorafenib out of the brain and show that its efflux at the BBB is mediated primarily by BCRP. Sorafenib ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
4 Sorafenib clearance out of the brain decreased 2-fold in the Bcrp1(-/-) mice and 2.5-fold in the Mdr1a/1b(-/-)Bcrp1(-/-) mice. Sorafenib ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
5 Sorafenib clearance out of the brain decreased 2-fold in the Bcrp1(-/-) mice and 2.5-fold in the Mdr1a/1b(-/-)Bcrp1(-/-) mice. Sorafenib ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
6 In conclusion, this study explains the cooperation of P-gp and BCRP by analysis of the efflux clearance of sorafenib and correlating it to the "mechanisms" that determine the clearance, i.e., affinity and capacity. Sorafenib ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus