Characterization and Validation of Canine P-Glycoprotein-Deficient MDCK II Cell Lines for Efflux Substrate Screening.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: deficient; cell lines; brain penetration; cell ... See more keywords
Validation of Human MDR1-MDCK and BCRP-MDCK Cell Lines to Improve the Prediction of Brain Penetration.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: mdck; bcrp; brain penetration; mdr1 ... See more keywords
Predicting In Vivo Compound Brain Penetration Using Multi-task Graph Neural Networks
Sign Up to like & getrecommendations! 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… read more here.
Keywords: brain penetration; vivo compound; brain; task ... See more keywords
Discovery of First-in-Class Peptidomimetic Neurolysin Activators Possessing Enhanced Brain Penetration and Stability.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: discovery; neurolysin; brain penetration; nln ... See more keywords
Natural Brain Penetration Enhancer-Modified Albumin Nanoparticles for Glioma Targeting Delivery.
Sign Up to like & getrecommendations! 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… read more here.
Keywords: glioma; albumin nanoparticles; delivery; modified albumin ... See more keywords
Abstract 3582: Differentiation of niraparib and olaparib brain penetration in a mouse brain metastatic tumor model
Sign Up to like & getrecommendations! 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… read more here.
Keywords: olaparib; control; brain; brain penetration ... See more keywords