Related Experiment Video
Updated: Sep 3, 2025

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Sodium phosphate cotransporter 2a inhibitors: potential therapeutic uses
Jianxiang Xue1, Linto Thomas1, Jessica A Dominguez Rieg1,2
1Department of Molecular Pharmacology and Physiology.
Targeting sodium phosphate cotransporter 2a (Npt2a) offers a novel strategy for treating hyperphosphatemia in chronic kidney disease (CKD). Npt2a inhibition lowers plasma phosphate and parathyroid hormone, with potential cardiovascular benefits.
Area of Science:
- Nephrology
- Pharmacology
Background:
- Hyperphosphatemia is a common complication in chronic kidney disease (CKD).
- Sodium phosphate cotransporter 2a (Npt2a) plays a key role in phosphate reabsorption in the kidneys.
Purpose of the Study:
- To review recent studies on the efficacy of Npt2a inhibition for hyperphosphatemia in CKD.
- To evaluate the plasma phosphate-lowering effects and potential cardiovascular benefits of Npt2a inhibition.
Main Methods:
- Review of recent studies on Npt2a inhibitors (PF-06869206 and BAY-767).
- Analysis of effects on plasma phosphate, parathyroid hormone, and fibroblast growth factor 23.
- Assessment of effects on urinary excretion of ions and vascular calcification in animal models.
Main Results:
- Npt2a inhibition effectively lowers plasma phosphate and parathyroid hormone levels.
- Responses of plasma fibroblast growth factor 23 varied between inhibitors.
- Npt2a inhibition enhanced urinary excretion of Na+, Cl-, and Ca2+.
- BAY-767 treatment attenuated vascular calcification in an animal model.
Conclusions:
- Npt2a inhibition is a promising therapeutic approach for hyperphosphatemia in CKD.
- Npt2a inhibition may offer beneficial "off-target" effects on cardiovascular complications.
More Related Videos
10:08Study of the Functions and Activities of Neuronal K-Cl Co-Transporter KCC2 Using Western Blotting
Published on: December 9, 2022
06:59A Fluorescence-Based Assay of Membrane Potential for High-Throughput Functional Study of Two Endogenous Ion Channels in Two Epithelial Cell Lines
Published on: June 22, 2022
Related Concept Videos
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Secondary Active Transport
Active Transport
Primary active transporters, like Na+, K+ and -ATPase, directly utilize ATP to move ions across the membrane. These transporters play significant roles in various physiological processes. For instance, Na+, K+ and -ATPase maintain...
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Antihypertensive Drugs: Potassium-Sparing Diuretics