Lubiprostone is a Non-Selective Activator of cAMP-Gated Ion Channels and Chloride Channel Protein 2 (Clc-2) Has a Minor Role in its Prosecretory Effect in Intestinal …

AA Oak, T Chu, P Yottasan, PD Chhetri, J Zhu… - Molecular …, 2022 - ASPET
Loss of prosecretory Cl-channel cystic fibrosis transmembrane conductance regulator
(CFTR) activity is considered the key cause of gastrointestinal disorders in cystic fibrosis,
including constipation and meconium ileus. Chloride channel protein 2 (Clc-2) is proposed
as an alternative Cl-channel in intestinal epithelia that can compensate for CFTR loss-of-
function. Lubiprostone is a Food and Drug Administration-approved drug with Clc-2
activation as its presumed mechanism of action. However, relative contribution of Clc-2 in …

Lubiprostone is non-selective activator of cAMP-gated ion channels and Clc-2 has a minor role in its prosecretory effect in intestinal epithelial cells.

A Oak, T Chu, P Yottasan, P Chhetri, J Zhu… - Molecular …, 2022 - escholarship.org
Loss of prosecretory Cl-channel CFTR activity is considered as the key cause of
gastrointestinal disorders in cystic fibrosis including constipation and meconium ileus. Clc-2
is proposed as an alternative Cl-channel in intestinal epithelia that can compensate for
CFTR loss-of-function. Lubiprostone is an FDA-approved drug with Clc-2 activation as its
presumed mechanism of action. However, relative contribution of Clc-2 in intestinal Cl-
secretion and the mechanism of action of lubiprostone remain controversial due to lack of …