Enantioselectivity in drug pharmacokinetics and toxicity: Pharmacological relevance and analytical methods

MM Coelho, C Fernandes, F Remião, ME Tiritan - Molecules, 2021 - mdpi.com
Enzymes, receptors, and other binding molecules in biological processes can recognize
enantiomers as different molecular entities, due to their different dissociation constants …

Hepatic solute carrier transporters and drug therapy: Regulation of expression and impact of genetic variation

AT Nies, E Schaeffeler, M Schwab - Pharmacology & Therapeutics, 2022 - Elsevier
Organic cation transporters (OCT), organic anion transporting polypeptides (OATP) and
organic anion transporters (OAT) from the solute carrier (SLC) family play an essential role …

Structural basis of promiscuous substrate transport by Organic Cation Transporter 1

YC Zeng, M Sobti, A Quinn, NJ Smith… - Nature …, 2023 - nature.com
Abstract Organic Cation Transporter 1 (OCT1) plays a crucial role in hepatic metabolism by
mediating the uptake of a range of metabolites and drugs. Genetic variations can alter the …

Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2

L Gebauer, O Jensen, J Brockmöller… - Journal of medicinal …, 2022 - ACS Publications
Organic cation transporters (OCTs) 1, 2, and 3 facilitate cellular uptake of structurally diverse
endogenous and exogenous substances. However, their substrate and inhibitor specificity …

Identification of novel high-affinity substrates of OCT1 using machine learning-guided virtual screening and experimental validation

O Jensen, J Brockmöller… - Journal of medicinal …, 2021 - ACS Publications
OCT1 is the most highly expressed cation transporter in the liver and affects
pharmacokinetics and pharmacodynamics. Newly marketed drugs have previously been …

Caffeic acid O-methyltransferase from Ligusticum chuanxiong alleviates drought stress, and improves lignin and melatonin biosynthesis

E Huang, J Tang, S Song, H Yan, X Yu, C Luo… - Frontiers in Plant …, 2024 - frontiersin.org
Drought stress is a major constraint on plant growth and agricultural productivity. Caffeic
acid O-methyltransferase (COMT), an enzyme involved in the methylation of various …

Relationships between inhibition, transport and enhanced transport via the organic cation transporter 1

O Jensen, L Gebauer, J Brockmöller… - International Journal of …, 2022 - mdpi.com
The organic cation transporter 1 (OCT1, SLC22A1) transports a large number of structurally
diverse endogenous and exogenous substrates. There are numerous known competitive …

Molecular basis for stereoselective transport of fenoterol by the organic cation transporters 1 and 2

L Gebauer, NA Murugan, O Jensen… - Biochemical …, 2022 - Elsevier
Stereoselectivity is important in many pharmacological processes but its impact on drug
membrane transport is scarcely understood. Recent studies showed strong stereoselective …

Stereoselectivity of interaction of nonsteroidal anti-inflammatory drug S-ketoprofen with L/D-tryptophan in phospholipid membranes

AV Mastova, OY Selyutina, NE Polyakov - Membranes, 2022 - mdpi.com
The mechanisms of stereoselectivity of the interaction of chiral drugs with active sites of
enzymes and cell receptors attract significant attention. The first reason is the difference in …

Cellular uptake of psychostimulants–are high-and low-affinity organic cation transporters drug traffickers?

O Jensen, M Rafehi, L Gebauer… - Frontiers in …, 2021 - frontiersin.org
Psychostimulants are used therapeutically and for illegal recreational purposes. Many of
these are inhibitors of the presynaptic noradrenaline, dopamine, and serotonin transporters …