Anticancer agents interacting with membrane glucose transporters
The altered metabolism observed in cancer cells generally consists of increased glucose uptake and glycolytic activity.
Insights into solute carriers: physiological functions and implications in disease and pharmacokinetics
SLCs transport many endogenous and exogenous compounds including drugs; SLCs dysfunction has implications in pharmacokinetics, drug toxicity or lack of efficacy.
The role of transporter ectodomains in drug recognition and binding: phlorizin and the sodium–glucose cotransporter
This article reviews the role of segments of SLCs located outside the plasma membrane bilayer (ectodomains) using the inhibition of SGLTs (SLC5 family) by the aromatic glucoside phlorizin as a model system.
SLC transporters: structure, function, and drug discovery
The human solute carrier (SLC) transporters are important targets for drug development.
Fatty acid transport proteins: targeting FATP2 as a gatekeeper involved in the transport of exogenous fatty acids
FATP2 as the gatekeeper (A), dysregulation of fatty acid metabolism from FA overload (B), and Lipofermata or Grassofermata treatment (C).
Ibuprofen transport in renal cell cultures: characterization of an ibuprofen transporter upregulated by hyperosmolarity
An ibuprofen transporter localizes to the apical and basolateral membrane of MDCK I cells is upregulated by hyperosmotic exposure. Ibuprofen uptake is inhibited by other NSAIDs and ibuprofen metabolites.
From linked open data to molecular interaction: studying selectivity trends for ligands of the human serotonin and dopamine transporter
Retrieval of consistent SAR data sets is a challenging task. Combining integrated open data sources with workflow tools allows studying selectivity trends of compound series.
Molecular localization and characterization of multiple binding sites of organic anion transporting polypeptide 2B1 (OATP2B1) as the mechanism for substrate and modulator dependent drug–drug interaction
Schematic model of the relationship and locations of putative binding sites of substrates and modulators in OATP2B1. Drug–drug interaction and drug–food interaction on OATP2B1 can be predicted by clarification of multiple binding sites.
The biogenic amine transporter activity of vinylogous amphetamine analogs
Vinylogous amphetamine analog S-6 is a potent dual dopamine/serotonin (DA/5-HT) releaser with no activity at 5-HT2 receptors.
The discovery and evaluation of diaryl ether heterocyclic sulfonamides as URAT1 inhibitors for the treatment of gout
A series of acidic heterocyclic sulfonamides that are potent and selective URAT1 inhibitors is described.
The design, synthesis and evaluation of low molecular weight acidic sulfonamides as URAT1 inhibitors for the treatment of gout
A series of low molecular weight and synthetically facile acidic sulfonamides that are potent and selective URAT1 inhibitors is described.
Identification of a novel BODIPY minihepcidin tool for the high content analysis of ferroportin (SLC40A1) pharmacology
Herein, we describe the design and synthesis of a novel BODIPY-labelled minihepcidin peptide to enable the high content analysis of ferroportin (SLC40A1) pharmacology.
A cyclosporine derivative is a substrate of the oligopeptide transporter PepT1
Cyclosporine was attached to a thiodipeptide carrier, yielding conjugate 7; this is a substrate for PepT1 with oral bioavailability potential.
Design and synthesis of thiamine analogues to study their binding to the ECF transporter for thiamine in bacteria
This work presents new small molecules that bind to the protein ThiT, which confers substrate specificity to the Energy-Coupling Factor (ECF) transporter for thiamine. Further development of the molecules may lead to compounds with antimicrobial activity.
Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors
Gln and Tyr conjugates of MCT inhibitors were designed and shown to be highly cytotoxic to a human cancer cell line expressing the transporters Asct2, LAT1, and MCT1/2.
About this collection
Metabolic homeostasis within cells requires strict control over the import and export of metabolites, nutrients and ions across membranes. Polar chemical species such as these have negligible ability to cross phospholipid membranes by simple diffusion and instead require highly regulated transport proteins to control their movement. The largest class of transport proteins is the solute carrier (SLC) series (www.bioparadigms.org) and it is on this superfamily that this themed collection focuses.
These proteins are of great interest for basic academic research, but beyond that they are of central importance in a number of areas of applied science: as drug targets, as controllers of drug disposition and pharmacokinetics, and as the cause of drug toxicity.
This collection of articles, guest edited by Prof Matthias A. Hediger (University of Bern, Switzerland ) and & Dr David Hepworth (Pfizer) is a celebration of all areas of research where the chemical sciences have impacted the study of the SLC superfamily.
New articles will be added to this collection as they are published.
Please return to this page frequently to see the collection grow.