ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors

International Journal of Cancer

Volumn 137, Issue 8, 2015, Pages 2007-2018

  Zhang, Ping ^a,b   De Gooijer, Mark C ^b   Buil, Levi C M ^b   Beijnen, Jos H ^c,d   Li, Gang ^a   Van Tellingen, Olaf ^b  

^a SHANDONG UNIVERSITY   (China)

^b NETHERLANDS CANCER INSTITUTE   (Netherlands)

^c SLOTERVAART HOSPITAL   (Netherlands)

^d UTRECHT UNIVERSITY   (Netherlands)

Author keywords

ABCB1; ABCG2; Brain penetration; EZH2 inhibitor; Pharmacokinetics

Indexed keywords

ANTINEOPLASTIC AGENT; BREAST CANCER RESISTANCE PROTEIN; ELACRIDAR; EPZ 005687; GSK 126; GSK 343; MULTIDRUG RESISTANCE PROTEIN 1; TAZEMETOSTAT; TRANSCRIPTION FACTOR EZH2; UNC 1999; UNCLASSIFIED DRUG; ABC TRANSPORTER; BENZAMIDE DERIVATIVE; ENZYME INHIBITOR; EPZ-6438; EPZ005687; EZH2 PROTEIN, HUMAN; GSK126; GSK343; INDAZOLE DERIVATIVE; INDOLE DERIVATIVE; MULTIDRUG RESISTANCE PROTEIN; POLYCOMB REPRESSIVE COMPLEX 2; PYRIDONE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; BRAIN REGION; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG RETENTION; DRUG SCREENING; DRUG STRUCTURE; DRUG TARGETING; DRUG TISSUE LEVEL; DRUG TRANSPORT; GLIOMA; IN VITRO STUDY; IN VIVO STUDY; KNOCKOUT MOUSE; MAXIMUM PLASMA CONCENTRATION; MEMBRANE PERMEABILITY; MOUSE; NONHUMAN; PRIORITY JOURNAL; TIME TO MAXIMUM PLASMA CONCENTRATION; WILD TYPE; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOAVAILABILITY; CELL LINE; DOG; DRUG EFFECTS; GENETICS; HUMAN; MDCK CELL LINE; METABOLISM; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BENZAMIDES; BIOLOGICAL AVAILABILITY; BLOOD-BRAIN BARRIER; CELL LINE; DOGS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; INDAZOLES; INDOLES; MADIN DARBY CANINE KIDNEY CELLS; MICE; MICE, KNOCKOUT; P-GLYCOPROTEINS; POLYCOMB REPRESSIVE COMPLEX 2; PYRIDONES;

EID: 84938955658     PISSN: 00207136     EISSN: 10970215     Source Type: Journal    
DOI: 10.1002/ijc.29566     Document Type: Article

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