Highly Selective Artificial K Transporters Reverse Liver Fibrosis In Vivo.

JACS Au

State Key Laboratory of Cellular Stress Biology and Fujian Provincial Key Laboratory of Innovative Drug Target Research, School of Pharmaceutical Sciences, Xiamen University, Xiamen, Fujian 361102, China.

Published: October 2024

Liver fibrosis is a life-threatening disease that currently lacks clinically effective therapeutic agents. Given the close correlation between dysregulated intracellular K homeostasis and the progression of liver fibrosis, developing artificial K transporters mimicking the essential function of their natural counterparts in regulating intracellular K levels might offer an appealing yet unexplored treatment strategy. Here, we present an unconventional class of artificial K transporters involving the "motional" collaboration between two K transporter molecules. In particular, exhibits an impressive EC value of 0.28 μM (i.e., 0.28 mol % relative to lipid) toward K and an exceptionally high K/Na selectivity of 15.5, representing one of the most selective artificial K transporters reported to date. Most importantly, our study demonstrates, for the first time, the potential therapeutic effect of K-selective artificial ion transporters in reversing liver fibrosis both and .

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11522913PMC
http://dx.doi.org/10.1021/jacsau.4c00521DOI Listing

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