Related Experiment Video
Updated: Mar 31, 2026

A Proteoliposome-Based Efflux Assay to Determine Single-molecule Properties of Cl- Channels and Transporters
Published on: April 20, 2015
Does lipophilicity affect the effectiveness of a transmembrane anion transporter? Insight from
Zhi Li1, Li-Qun Deng, Jin-Xiang Chen
1School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, P. R. China. whchen@smu.edu.cn.
Abstract:
Six squaramido-functionalized bis(choloyl) conjugates were synthesized and fully characterized on the basis of NMR ((1)H and (13)C) and ESI MS (LR and HR) data. Their transmembrane anionophoric activity was investigated in detail by means of chloride ion selective electrode technique and pyranine assay. The data indicate that this set of compounds is capable of promoting the transmembrane transport of anions presumably via proton/anion symport and anion exchange processes, and that lipophilicity in terms of clog P from 3.90 to 8.32 affects the apparent ion transport rate in a concentration-dependent fashion. Detailed kinetic analysis on the data obtained from both the chloride efflux and pH discharge experiments reveals that there may exist an optimum clog P range for the intrinsic ion transport rate. However, lipophilicity exhibits little effect on the effectiveness of this set of compounds in terms of either k2/Kdiss or EC50 values.
More Related Videos
09:59Functional Reconstitution and Channel Activity Measurements of Purified Wildtype and Mutant CFTR Protein
Published on: March 9, 2015
07:38Functional Characterization of Na+/H+ Exchangers of Intracellular Compartments Using Proton-killing Selection to Express Them at the Plasma Membrane
Published on: March 30, 2015
Related Concept Videos
Drug Absorption Mechanism: Passive Membrane Transport
Pore Transport and Ion-Pair Transport
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Hepatic Drug Clearance: Role of Transporters
Facilitated Diffusion
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
Bioavailability Enhancement: Drug Permeability Enhancement