Decreased affinity for efflux transporters increases brain penetrance and molecular targeting of a PI3K/mTOR inhibitor in a mouse model of glioblastoma

Neuro-Oncology

Volumn 17, Issue 9, 2015, Pages 1210-1219

  Becker, Chani M ^a   Oberoi, Rajneet K ^a,b,c   McFarren, Stephan J ^a   Muldoon, Daniel M ^a   Pafundi, Deanna H ^a   Pokorny, Jenny L ^a   Brinkmann, Debra H ^a   Ohlfest, John R ^a   Sarkaria, Jann N ^a   Largaespada, David A ^a,c   Elmquist, William F ^a,b  

^a UNIVERSITY OF MINNESOTA   (United States)

^b UNIVERSITY OF MINNESOTA MEDICAL SCHOOL   (United States)

^c MAYO CLINIC   (United States)

Author keywords

blood brain barrier; brain tumors; efflux transport; molecularly targeted agents; p glycoprotein

Indexed keywords

APITOLISIB; BREAST CANCER RESISTANCE PROTEIN; GNE 317; INITIATION FACTOR 4E BINDING PROTEIN 1; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; MULTIDRUG RESISTANCE PROTEIN; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE B; PROTEIN S6; UNCLASSIFIED DRUG; 1-(4-((2-(2-AMINOPYRIMIDIN-5-YL)-7-METHYL-4-MORPHOLINOTHIENO(3,2-D)PYRIMIDIN-6-YL)METHYL)PIPERAZIN-1-YL)-2-HYDROXYPROPAN-1-ONE; ABC TRANSPORTER; ABCG2 PROTEIN, MOUSE; ANTINEOPLASTIC AGENT; FUSED HETEROCYCLIC RINGS; GNE-317; MTOR PROTEIN, MOUSE; PYRIMIDINE DERIVATIVE; TARGET OF RAPAMYCIN KINASE; THIOPHENE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; C57BL 6 MOUSE; CANCER MODEL; CONTINUOUS INFUSION; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG TUMOR LEVEL; ENZYME ACTIVATION; ENZYME INHIBITION; FEMALE; FVB/N MOUSE; GL261 CELL LINE; GLIOBLASTOMA; GLIOBLASTOMA CELL LINE; IMMUNOHISTOCHEMISTRY; KNOCKOUT MOUSE; MOLECULARLY TARGETED THERAPY; MOUSE; MOUSE MODEL; NONHUMAN; TREATMENT DURATION; TUMOR GROWTH; WILD TYPE MOUSE; ANIMAL; ANTAGONISTS AND INHIBITORS; BRAIN; BRAIN NEOPLASMS; C57BL MOUSE; DRUG DELIVERY SYSTEM; DRUG EFFECTS; GENETICS; METABOLISM;

ANIMALS; ANTINEOPLASTIC AGENTS; ATP BINDING CASSETTE TRANSPORTER, SUB-FAMILY G, MEMBER 2; ATP-BINDING CASSETTE TRANSPORTERS; BLOOD-BRAIN BARRIER; BRAIN; BRAIN NEOPLASMS; BRIDGED BICYCLO COMPOUNDS, HETEROCYCLIC; DRUG DELIVERY SYSTEMS; GLIOBLASTOMA; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; P-GLYCOPROTEIN; PHOSPHATIDYLINOSITOL 3-KINASE; PYRIMIDINES; THIOPHENES; TOR SERINE-THREONINE KINASES;

EID: 84940766932     PISSN: 15228517     EISSN: 15235866     Source Type: Journal    
DOI: 10.1093/neuonc/nov081     Document Type: Article

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