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Published in 2020 at "Pharmaceutical research"
DOI: 10.1007/s11095-020-02895-9
Abstract: PURPOSE We characterized three canine P-gp (cP-gp) deficient MDCKII cell lines. Their relevance for identifying efflux transporter substrates and predicting limitation of brain penetration were evaluated. In addition, we discuss how compound selection can be…
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Keywords:
deficient;
cell lines;
brain penetration;
cell ... See more keywords
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Published in 2019 at "Journal of pharmaceutical sciences"
DOI: 10.1016/j.xphs.2019.02.005
Abstract: It is of great challenge to predict human brain penetration for substrates of multidrug resistance protein 1 (MDR1) and breast cancer resistance protein (BCRP), 2 major efflux transporters at blood-brain barrier. Thus, a physiologically based…
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Keywords:
mdck;
bcrp;
brain penetration;
mdr1 ... See more keywords
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Published in 2022 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.2c00412
Abstract: Assessing whether compounds penetrate the brain can become critical in drug discovery, either to prevent adverse events or to reach the biological target. Generally, pre-clinical in vivo studies measuring the ratio of brain and blood…
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Keywords:
brain penetration;
vivo compound;
brain;
task ... See more keywords
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Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00759
Abstract: Peptidase neurolysin (Nln) is an enzyme that functions to cleave various neuropeptides. Upregulation of Nln after stroke has identified the enzyme as a critical endogenous cerebroprotective mechanism and validated target for the treatment of ischemic…
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Keywords:
discovery;
neurolysin;
brain penetration;
nln ... See more keywords
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Published in 2018 at "ACS applied materials & interfaces"
DOI: 10.1021/acsami.8b11782
Abstract: The unsatisfactory therapeutic outcome for glioma is mainly due to the poor blood-brain barrier (BBB) permeability and inefficient accumulation in the glioma area of chemotherapeutic agents. The existing drug delivery strategies can increase drug transport…
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Keywords:
glioma;
albumin nanoparticles;
delivery;
modified albumin ... See more keywords
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Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3582
Abstract: Purpose: There remains an unmet need to provide effective treatment therapy for patients with primary and metastatic brain tumors; lack of drug penetration across the blood brain barrier (BBB) is a key factor. Synthetic lethality…
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Keywords:
olaparib;
control;
brain;
brain penetration ... See more keywords