Plasma protein binding: from discovery to development

T Bohnert, LS Gan - Journal of pharmaceutical sciences, 2013 - Elsevier
The importance of plasma protein binding (PPB) in modulating the effective drug
concentration at pharmacological target sites has been the topic of significant discussion …

Dietary polyphenols as modulators of brain functions: biological actions and molecular mechanisms underpinning their beneficial effects

D Vauzour - Oxidative medicine and cellular longevity, 2012 - Wiley Online Library
Accumulating evidence suggests that diet and lifestyle can play an important role in delaying
the onset or halting the progression of age‐related health disorders and to improve cognitive …

Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain—a Game Changing Parameter for CNS Drug Discovery and Development

I Loryan, A Reichel, B Feng, C Bundgaard… - Pharmaceutical …, 2022 - Springer
Purpose More than 15 years have passed since the first description of the unbound brain-to-
plasma partition coefficient (Kp, uu, brain) by Prof. Margareta Hammarlund-Udenaes, which …

Comparison of brain capillary endothelial cell-based and epithelial (MDCK-MDR1, Caco-2, and VB-Caco-2) cell-based surrogate blood–brain barrier penetration …

É Hellinger, S Veszelka, AE Tóth, F Walter… - European journal of …, 2012 - Elsevier
An accurate means of predicting blood–brain barrier (BBB) penetration and blood–brain
partitioning of NCEs (new chemical entities) would fulfill a major need in pharmaceutical …

Fate of microbial metabolites of dietary polyphenols in rats: is the brain their target destination?

M Gasperotti, S Passamonti, F Tramer… - ACS chemical …, 2015 - ACS Publications
Different polyphenol compounds are ingested when consuming a serving of fruits rich in
polyphenols, spanning from one-phenol hydroxybenzoic acid to more complex polymeric …

Do polyphenols enter the brain and does it matter? Some theoretical and practical considerations

S Schaffer, B Halliwell - Genes & nutrition, 2012 - Springer
Although several epidemiological and intervention studies suggest that polyphenols (PPs)
and PP-rich foods may improve memory and cognition in animals and humans, PPs' mode …

Structure− brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids

M Fridén, S Winiwarter, G Jerndal… - Journal of medicinal …, 2009 - ACS Publications
New experimental methodologies were applied to measure the unbound brain-to-plasma
concentration ratio (K p, uu, brain) and the unbound CSF-to-plasma concentration ratio (K p …

Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas

M Verreault, C Schmitt, L Goldwirt, K Pelton… - Clinical Cancer …, 2016 - AACR
Purpose: p53 pathway alterations are key molecular events in glioblastoma (GBM). MDM2
inhibitors increase expression and stability of p53 and are presumed to be most efficacious …

Mechanisms of dietary flavonoid action in neuronal function and neuroinflammation

BN Jaeger, SL Parylak, FH Gage - Molecular aspects of medicine, 2018 - Elsevier
Flavonoids are a class of plant-derived dietary polyphenols that have attracted attention for
their pro-cognitive and anti-inflammatory effects. The diversity of flavonoids and their …

Understanding the brain uptake and permeability of small molecules through the BBB: A technical overview

EA Chowdhury, B Noorani, F Alqahtani… - Journal of Cerebral …, 2021 - journals.sagepub.com
The brain is the most important organ in our body requiring its unique microenvironment. By
the virtue of its function, the blood-brain barrier poses a significant hurdle in drug delivery for …