Organotypic and microphysiological models of liver, gut, and kidney for studies of drug metabolism, pharmacokinetics, and toxicity

JX Shen, S Youhanna, R Zandi Shafagh… - Chemical research in …, 2019 - ACS Publications
Despite extensive breakthroughs in chemistry, molecular biology, and genetics in the last
decades, the success rates of drug development projects remain low. To improve …

NMR Characterization of the Interactions between Glycosaminoglycans and Proteins

C Bu, L Jin - Frontiers in Molecular Biosciences, 2021 - frontiersin.org
Glycosaminoglycans (GAGs) constitute a considerable fraction of the glycoconjugates found
on cellular membranes and in the extracellular matrix of virtually all mammalian tissues. The …

Advantages and potential limitations of applying AFM kymograph analysis to pharmaceutically relevant membrane proteins in lipid bilayers

KG Schaefer, AG Roberts, GM King - Scientific Reports, 2023 - nature.com
Membrane proteins play critical roles in disease and in the disposition of many
pharmaceuticals. A prime example is P-glycoprotein (Pgp) which moves a diverse range of …

Drug absorption related nephrotoxicity assessment on an intestine-kidney chip

Z Li, W Su, Y Zhu, T Tao, D Li, X Peng, J Qin - Biomicrofluidics, 2017 - pubs.aip.org
Drug absorption in the intestine is tightly related to drug-induced nephrotoxicity, which is a
relatively common side effect in clinical practice. It highlights a great need to develop …

Cooperativity between verapamil and ATP bound to the efflux transporter P-glycoprotein

KV Ledwitch, ME Gibbs, RW Barnes… - Biochemical …, 2016 - Elsevier
The P-glycoprotein (Pgp) transporter plays a central role in drug disposition by effluxing a
chemically diverse range of drugs from cells through conformational changes and ATP …

Colchicine and macrolides: a cohort study of the risk of adverse outcomes associated with concomitant exposure

MS Tan, A Gomez-Lumbreras, L Villa-Zapata… - Rheumatology …, 2022 - Springer
Colchicine is increasingly used as the number of potential indications expands. However, it
also has a narrow therapeutic index that is associated with bothersome to severe side …

Four decades of Cytochrome P450 2B research: from protein adducts to protein structures and beyond

AG Roberts, JC Stevens, GD Szklarz, EE Scott… - Drug Metabolism and …, 2023 - ASPET
This article features selected findings from the senior author and colleagues dating back to
1978 and covering approximately three-fourths of the 60 years since the discovery of …

Drug-induced conformational dynamics of P-glycoprotein underlies the transport of camptothecin analogs

GAK Mensah, KG Schaefer, MG Bartlett… - International Journal of …, 2023 - mdpi.com
P-glycoprotein (Pgp) plays a pivotal role in drug bioavailability and multi-drug resistance
development. Understanding the protein's activity and designing effective drugs require …

The conformation and dynamics of P-glycoprotein in a lipid bilayer investigated by atomic force microscopy

KP Sigdel, LA Wilt, BP Marsh, AG Roberts… - Biochemical …, 2018 - Elsevier
The membrane-bound P-glycoprotein (Pgp) transporter plays a major role in human disease
and drug disposition because of its ability to efflux a chemically diverse range of drugs …

Cardiovascular ion channel inhibitor drug-drug interactions with P-glycoprotein

KV Ledwitch, AG Roberts - The AAPS journal, 2017 - Springer
P-glycoprotein (Pgp) is an ATP-binding cassette (ABC) transporter that plays a major role in
cardiovascular drug disposition by effluxing a chemically and structurally diverse range of …