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Active efflux of Dasatinib from the brain limits efficacy against murine glioblastoma: broad implications for the clinical use of molecularly targeted agents.
Agarwal, Sagar; Mittapalli, Rajendar K; Zellmer, David M; Gallardo, Jose L; Donelson, Randy; Seiler, Charlie; Decker, Stacy A; Santacruz, Karen S; Pokorny, Jenny L; Sarkaria, Jann N; Elmquist, William F; Ohlfest, John R.
Affiliation
  • Agarwal S; Corresponding Author: John Ohlfest, Department of Pediatrics, University of Minnesota, 420 Delaware St. SE, MMC 366, Minneapolis, MN 55455, USA.
Mol Cancer Ther ; 11(10): 2183-92, 2012 Oct.
Article in En | MEDLINE | ID: mdl-22891038
Subject(s)
Brain/metabolism; Glioblastoma/drug therapy; Molecular Targeted Therapy; Pyrimidines/metabolism; Pyrimidines/therapeutic use; Thiazoles/metabolism; Thiazoles/therapeutic use; ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors; ATP Binding Cassette Transporter, Subfamily B, Member 1/deficiency; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters/antagonists & inhibitors; ATP-Binding Cassette Transporters/deficiency; ATP-Binding Cassette Transporters/metabolism; Acridines/chemistry; Acridines/pharmacology; Acridines/therapeutic use; Animals; Blood-Brain Barrier/drug effects; Blood-Brain Barrier/metabolism; Blood-Brain Barrier/pathology; Brain/drug effects; Brain/pathology; Dasatinib; Disease Models, Animal; Endothelium, Vascular/drug effects; Endothelium, Vascular/metabolism; Endothelium, Vascular/pathology; Glioblastoma/blood supply; Glioblastoma/pathology; Humans; Mice; Mice, Knockout; Oncogenes; Permeability/drug effects; Pyrimidines/chemistry; Pyrimidines/pharmacology; Signal Transduction/drug effects; Survival Analysis; Tetrahydroisoquinolines/chemistry; Tetrahydroisoquinolines/pharmacology; Tetrahydroisoquinolines/therapeutic use; Thiazoles/chemistry; Thiazoles/pharmacology; Tight Junctions/drug effects; Tight Junctions/metabolism; Tight Junctions/pathology; Tissue Distribution/drug effects; Treatment Outcome; Xenograft Model Antitumor Assays
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Thiazoles / Brain / Glioblastoma / Molecular Targeted Therapy Language: En Journal: Mol Cancer Ther Journal subject: ANTINEOPLASICOS Year: 2012 Document type: Article Affiliation country: Estados Unidos Country of publication: Estados Unidos
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Thiazoles / Brain / Glioblastoma / Molecular Targeted Therapy Language: En Journal: Mol Cancer Ther Journal subject: ANTINEOPLASICOS Year: 2012 Document type: Article Affiliation country: Estados Unidos Country of publication: Estados Unidos