[PDF][PDF] Membranes Matter: Predicting Drug Toxicity

RL Sanford, J Chiaravalli-Giganti, W Chao… - Biophysical …, 2018 - cell.com
It remains a challenge to predict whether a new drug candidate will have undesirable side
effects. Many biologically active molecules, including drugs and drug-leads, are amphiphiles …

[PDF][PDF] Membranes Matter: Predicting Drug Toxicity

RL Sanford, W Chao, J Chiaravalli-Giganti, A Luz… - Biophysical …, 2017 - cell.com
It remains a challenge to predict whether a new drug candidate will have undesirable side
effects. Many biologically active molecules, including drugs and drug-leads, are amphiphiles …

[PDF][PDF] Predicting Drug Toxicity: Early Detection of Likely Failures in Drug Development

RL Sanford, W Chao, J Chiaravalli-Giganti, A Luz… - Biophysical …, 2015 - cell.com
It remains a challenge to predict whether or not a new drug candidate will have undesirable
side-effects in the clinic. Many biologically active molecules, including drugs and drug-leads …

Membranes Matter: Exploring Lipid-Bilayer Perturbation from Small Bioactive Molecules and Implications for Cytotoxicity

RL Sanford - 2021 - search.proquest.com
Cell membranes are mosaics comprised of lipid bilayers and a multitude of embedded
transmembrane proteins. Because membrane proteins undergo conformational changes …

Screening for bilayer-active and likely cytotoxic molecules reveals bilayer-mediated regulation of cell function

TA Peyear, OS Andersen - Journal of General Physiology, 2023 - rupress.org
A perennial problem encountered when using small molecules (drugs) to manipulate cell or
protein function is to assess whether observed changes in function result from specific …

Assessing the Perturbing Effects of Drugs on Lipid Bilayers Using Gramicidin Channel-Based In Silico and In Vitro Assays

D Sun, TA Peyear, WFD Bennett… - Journal of Medicinal …, 2020 - ACS Publications
Partitioning of bioactive molecules, including drugs, into cell membranes may produce
indiscriminate changes in membrane protein function. As a guide to safe drug development …

Screening for small molecules' bilayer-modifying potential using a gramicidin-based fluorescence assay

HI Ingólfsson, OS Andersen - Assay and drug development …, 2010 - liebertpub.com
Many drugs and other small molecules used to modulate biological function are amphiphiles
that adsorb at the bilayer/solution interface and thereby alter lipid bilayer properties. This is …

Interactions of drugs and amphiphiles with membranes: modulation of lipid bilayer elastic properties by changes in acyl chain unsaturation and protonation

MJ Bruno, R Rusinova, NJ Gleason, RE Koeppe II… - Faraday …, 2013 - pubs.rsc.org
Poly-unsaturated fatty acids (PUFAs) alter the function of many membrane proteins, whereas
monounsatured fatty acids generally are inert. We previously showed that docosahexaenoic …

Membranes–from Barriers to Magic Bullets

OG Mouritsen - Pharmacokinetic Profiling in Drug Research …, 2006 - Wiley Online Library
It is important to realize that a lipid bilayer membrane is not just a homogeneous thin slap of
a dielectric medium immersed in water but that the bilayer is a highly stratified structure with …

Gramicidin-based fluorescence assay; for determining small molecules potential for modifying lipid bilayer properties

HI Ingólfsson, RL Sanford, R Kapoor… - JoVE (Journal of …, 2010 - jove.com
Many drugs and other small molecules used to modulate biological function are amphiphiles
that adsorb at the bilayer/solution interface and thereby alter lipid bilayer properties. This is …