In collaboration with the Center of Competence for Innovative Diabetes Therapy KomIT, we published our discoveries investigating the effect of a novel positive allosteric modulator (PAM) of the GABAA-receptor for NAFLD. In the present study we were able to demonstrate that HK4 is a selective GABAA receptor PAM, activating both stably transfected and native GABAA receptors. We provided further insights about its protective effect in human hepatocytes against lipotoxicity-induced injury by preventing apoptosis, inflammation, DNA damage and ER stress. These effects appear to be mediated by prominent transcription factors and changes in gene expression. Thus, GABAA receptor PAMs might be considered as a novel first-in-class treatment strategy for this severe liver disease. To check out the full publication please click here. The work is available as open access at Diabetes, Obesity and Metabolism – a journal of pharmacology and therapeutics.
Special thanks to one close partner of the KomIT the German Diabetes Center. Together, CureDiab and the German Diabetes Center will start soon further in vivo studies with PAMS of the GABAA-receptor to continuously exchange and gain information and expertise. Another step in the right direction!