A small synthetic molecule forms selective potassium channels to regulate cell membrane potential and blood vessel tone

• Published in: Organic & biomolecular chemistry Vol. 12; no. 41; p. 8174
• Main Authors: Zha, Hui-Yan, Shen, Bing, Yau, Kwok-Hei, Li, Shing-To, Yao, Xiao-Qiang, Yang, Dan
• Format: Journal Article
• Language: English
• Published: England 07-11-2014
• Subjects: Blood Vessels - drug effects; Blood Vessels - metabolism; Cell Membrane - drug effects; Cell Membrane - metabolism; HEK293 Cells; Humans; Molecular Conformation; Permeability - drug effects; Potassium Channels - metabolism; Small Molecule Libraries - chemical synthesis; Small Molecule Libraries - chemistry; Small Molecule Libraries - pharmacology
• ISSN: 1477-0539
• DOI: 10.1039/c4ob01420k

In living cell membranes, K(+) permeability is higher than that of other ions such as Na(+) and Cl(-) owing to abundantly expressed K(+) channels. Polarized membrane potential is mainly established by K(+) outward flow because the K(+) concentration in the intracellular side is much higher than that in the extracellular side. We have found that the small synthetic molecule 1 is capable of self-assembling into selective K(+) channels, enhancing K(+) permeability and hyperpolarizing liposome membrane potential. Interestingly, molecule 1 also functions as K(+) channel hyperpolarizing living cell membrane potential and relaxing agonist-induced blood vessel contraction. Therefore, it may have the potential to become a lead compound for the treatment of human diseases associated with K(+) channel dysfunction.