ArticleACS medicinal chemistry letters2018
Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1).
Article in ACS medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 31 citations in OpenAlex.
- The effects of elevated phosphate on the kidney - damaging the gatekeeper.Pflugers Archiv : European journal of physiology · 2026Review
- Updates on renal phosphate transport.Current opinion in nephrology and hypertension · 2025Review
- Beyond SGLT2: proximal tubule transporters as potential drug targets for chronic kidney disease.Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association · 2025Review
- Pharmacology of Mammalian NaHandbook of experimental pharmacology · 2024Article
- Ablation of TRPC3 compromises bicarbonate and phosphate transporter activity in mice proximal tubular cells.Clinical and experimental pharmacology & physiology · 2023Article
- RGS14 regulates PTH- and FGF23-sensitive NPT2A-mediated renal phosphate uptake via binding to the NHERF1 scaffolding protein.The Journal of biological chemistry · 2022Article
- Npt2a as a target for treating hyperphosphatemia.Biochemical Society transactions · 2022Review
- Selective pharmacological inhibition of the sodium-dependent phosphate cotransporter NPT2a promotes phosphate excretion.The Journal of clinical investigation · 2020Article
- PF-06869206 is a selective inhibitor of renal PAmerican journal of physiology. Renal physiology · 2020Article
- Nephropathic Cystinosis: A Distinct Form of CKD-Mineral and Bone Disorder that Provides Novel Insights into the Regulation of FGF23.Journal of the American Society of Nephrology : JASN · 2020Article
- Drug-nutrient interactions: discovering prescription drug inhibitors of the thiamine transporter ThTR-2 (SLC19A3).The American journal of clinical nutrition · 2020Article
- Another Tool in the Fight Against Phosphate Toxicity: Where Will It Fit and What Does It Tell Us about Phosphate Homeostasis?Journal of the American Society of Nephrology : JASN · 2019Article
- Pharmacological Npt2a Inhibition Causes Phosphaturia and Reduces Plasma Phosphate in Mice with Normal and Reduced Kidney Function.Journal of the American Society of Nephrology : JASN · 2019Article
- Mechanisms of phosphate transport.Nature reviews. Nephrology · 2019Review
- Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review.European journal of medicinal chemistry · 2019Review
- Substrates and inhibitors of phosphate transporters: from experimental tools to pathophysiological relevance.Pflugers Archiv : European journal of physiology · 2019Review
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
Abstract
Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solute-carrier (SLC) transporter located in the kidney proximal tubule that reabsorbs glomerular-filtered phosphate. Inhibition of NaPi2a may enhance urinary phosphate excretion and correct maladaptive mineral and hormonal derangements associated with increased cardiovascular risk in chronic kidney disease-mineral and bone disorder (CKD-MBD). To date, only nonselective NaPi inhibitors have been described. Herein, we detail the discovery of the first series of selective NaPi2a inhibitors, resulting from optimization of a high-throughput screening hit. The oral PK profile of inhibitor PF-06869206 (
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.