ArticleMolecular pharmaceutics2012
Potent inhibitors of human organic anion transporters 1 and 3 from clinical drug libraries: discovery and molecular characterization.
Article in Molecular pharmaceutics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed.
- Ginger and Its Purified Major Components Inhibit Clinically Relevant Uptake and Efflux Transporters In Vitro.Pharmaceutics · 2026Article
- Redefining AT1 Receptor PET Imaging: Introducing the Radiotracer [Hypertension (Dallas, Tex. : 1979) · 2025Article
- Computational Approaches for Predicting Drug Interactions with Human Organic Anion Transporter 4 (OAT4).Molecular pharmaceutics · 2025Article
- The Competitive Counterflow Assay for Identifying Drugs Transported by Solute Carriers: Principle, Applications, Challenges/Limits, and Perspectives.European journal of drug metabolism and pharmacokinetics · 2024Review
- Obstacles to Early Diagnosis of Acute Hepatic Porphyria: Current Perspectives on Improving Early Diagnosis and Clinical Management.Clinical and experimental gastroenterology · 2024Review
- A robust fluorescence-based assay for human erythrocyte CaEuropean biophysics journal : EBJ · 2023Article
- Maternal and Fetal Expression of ATP-Binding Cassette and Solute Carrier Transporters Involved in the Brain Disposition of Drugs.Advances in experimental medicine and biology · 2023Article
- Deuterated Indocyanine Green (ICG) with Extended Aqueous Storage Shelf-Life: Chemical and Clinical Implications.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Drug Metabolites Potently Inhibit Renal Organic Anion Transporters, OAT1 and OAT3.Journal of pharmaceutical sciences · 2021Article
- Insulin-like growth factor 1 modulates the phosphorylation, expression, and activity of organic anion transporter 3 through protein kinase A signaling pathway.Acta pharmaceutica Sinica. B · 2020Article
- Renal secretion of hydrochlorothiazide involves organic anion transporter 1/3, organic cation transporter 2, and multidrug and toxin extrusion protein 2-K.American journal of physiology. Renal physiology · 2019Article
- A simple model to solve a complex drug toxicity problem.Toxicology research · 2019Article
- AG490, a JAK2-specific inhibitor, downregulates the expression and activity of organic anion transporter-3.Journal of pharmacological sciences · 2018Article
- Position-related renal perfusion disturbances as a possible underestimated mechanism in patients with resistant hypertension: a case vignette.International urology and nephrology · 2017Article
- Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profilesMedChemComm · 2017Article
- Article
- Inhibition of Human Drug Transporter Activities by the Pyrethroid Pesticides Allethrin and Tetramethrin.PloS one · 2017Article
- Molecular Properties of Drugs Interacting with SLC22 Transporters OAT1, OAT3, OCT1, and OCT2: A Machine-Learning Approach.The Journal of pharmacology and experimental therapeutics · 2016Article
- An Organic Anion Transporter 1 (OAT1)-centered Metabolic Network.The Journal of biological chemistry · 2016Article
- Posttranslational Regulation of Organic Anion Transporters by Ubiquitination: Known and Novel.Medicinal research reviews · 2016Review
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Authors and funding
6 authors.
Funding
Abstract
Transporter-mediated drug-drug interactions in the kidney dramatically influence the pharmacokinetics and other clinical effects of drugs. Human organic anion transporters 1 (hOAT1) and 3 (hOAT3) are the major transporters in the basolateral membrane of kidney proximal tubules, mediating the rate-limiting step in the elimination of a broad spectrum of drugs. In the present study, we screened two clinical drug libraries against hOAT1 and hOAT3. Of the 727 compounds screened, 92 compounds inhibited hOAT1 and 262 compounds inhibited hOAT3. When prioritized based on the peak unbound plasma concentrations of these compounds, three inhibitors for hOAT1 and seven inhibitors for hOAT3 were subsequently identified with high inhibitory potency (>95%). Computational analyses revealed that inhibitors and noninhibitors can be differentiated from each other on the basis of several physicochemical features, including number of hydrogen-bond donors, number of rotatable bonds, and topological polar surface area (TPSA) for hOAT1; and molecular weight, number of hydrogen-bond donors and acceptors, TPSA, partition coefficient (log P(7.4)), and polarizability for hOAT3. Pharmacophore modeling identified two common structural features associated with inhibitors for hOAT1 and hOAT3, viz., an anionic hydrogen-bond acceptor atom, and an aromatic center separated by ∼5.7 Å. Such model provides mechanistic insights for predicting new OAT inhibitors.
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