Back to School

The summer holidays are mainly over in Finland and the school, as well as the semester at the Universities, have already started. I had a relaxing summer break, however, the scientists never have a real break, which is sometimes difficult fo non-scientists (like my husband) to understand. But this summer was not that bad, only a few manuscript readings, galley proof checkings and "some emails and phone calls" :). 

We luckily get one of the very challenging and long-lasting projects published in Molecular Neurobiology. The studied under the title

"Targeting of Perforin Inhibitor into the Brain Parenchyma Via a Prodrug Approach Can Decrease Oxidative Stress and Neuroinflammation and Improve Cell Survival" (link to the publication)

describes how a prodrug that utilizes LAT1 transporter and is delivered more effectively into the brain (across the blood-brain barrier) and into the brain parenchymal cells (e.g., neurons, microglia, and astrocytes) can improve its pharmacological effects. The parent drug of this prodrug is a perforin inhibitor (molecules that I worked with at the Auckland Cancer Society Research Centre in New Zealand 2009-2011) and it is supposed to inhibit endogenous perforin protein that is released e.g., in neurodegenerative diseases and which aids in destroying brain cells. Moreover, with LAT1-utilizing prodrug we were able to affect several different factors related to inflammation and oxidative stress in the brain (which is also associated with several neurodegenerative diseases) and to our surprise, the compound also inhibited an enzyme function, very special hallmark to Alzheimer's disease (BACE1; β-site amyloid precursor protein (APP) cleaving enzyme 1) and thus, our prodrug was functioning as a multitargeted drug within the brain. Most importantly, this publication is one of the first ones to show that rationally developed LAT1-utilizing prodrugs of a selected parent drug can really result in improved brain drug delivery and subsequently improved pharmacological effects! 

Thanks for the team for the great effort! :)