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10.1038/s41598-018-29062-w http://scihub22266oqcxt.onion/10.1038/s41598-018-29062-w C6050274!6050274!30018387     free     free     free       Sci+Rep 2018 ; 8 (ä): ä Nephropedia Template TP {{tp|p=30018387|t=2018. Buparlisib is a brain penetrable pan-PI3K inhibitor |pdf=|usr=}}{{30018387}} gab.com Text Buparlisib is a brain penetrable pan-PI3K inhibitor JO: Sci Rep http://www.kidney.de/pget.php?&tw=1&pmid=30018387 #FOAvip Characterization of the genomic landscapes of intracranial tumours has revealed a clear role for the PI3K-AKT-mTOR pathway in tumorigenesis and tumour maintenance of these malignancies, making phosphatidylinositol 3-kinase (PI3K) inhibition a promising therapeutic strategy for these tumours. Buparlisib is a novel pan-PI3K inhibitor that is currently in clinical development for various cancers, including primary and secondary brain tumours. Importantly however, earlier studies have revealed that sufficient brain penetration is a prerequisite for antitumor efficacy against intracranial tumours. We therefore investigated the brain penetration of buparlisib using a comprehensive set of in vitro and in vivo mouse models. We demonstrate that buparlisib has an excellent brain penetration that is unaffected by efflux transporters at the blood-brain barrier, complete oral bioavailability and efficient intracranial target inhibition at clinically achievable plasma concentrations. Together, these characteristics make buparlisib the ideal candidate for intracranially-targeted therapeutic strategies that involve PI3K inhibition. Twit Text FOAVip Buparlisib is a brain penetrable pan-PI3K inhibitor ????Sci Rep http://www.kidney.de/pget.php?&tw=1&pmid=30018387 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=30018387 #FOAvip English Wikipedia <ref>{{Cite pmid|30018387}}</ref> Buparlisib is a brain penetrable pan-PI3K inhibitor #MMPMID30018387 de Gooijer MC; Zhang P; Buil LCM; Çitirikkaya CH; Thota N; Beijnen JH; van Tellingen O Sci Rep 2018[]; 8 (ä): ä PMID30018387show ga Characterization of the genomic landscapes of intracranial tumours has revealed a clear role for the PI3K-AKT-mTOR pathway in tumorigenesis and tumour maintenance of these malignancies, making phosphatidylinositol 3-kinase (PI3K) inhibition a promising therapeutic strategy for these tumours. Buparlisib is a novel pan-PI3K inhibitor that is currently in clinical development for various cancers, including primary and secondary brain tumours. Importantly however, earlier studies have revealed that sufficient brain penetration is a prerequisite for antitumor efficacy against intracranial tumours. We therefore investigated the brain penetration of buparlisib using a comprehensive set of in vitro and in vivo mouse models. We demonstrate that buparlisib has an excellent brain penetration that is unaffected by efflux transporters at the blood-brain barrier, complete oral bioavailability and efficient intracranial target inhibition at clinically achievable plasma concentrations. Together, these characteristics make buparlisib the ideal candidate for intracranially-targeted therapeutic strategies that involve PI3K inhibition. äBuparlisib is a brain penetrable pan-PI3K inhibitor (epmc).pdf DeepDyve Pubget Overpricing