Uppsala University Researchers Report Research in Proinsulin [Benzylhydroxamic acids as inhibitors of insulin regulated aminopeptidase (IRAP)].

Researchers at Uppsala University in Sweden have conducted a study on proinsulin, focusing on the design and synthesis of small molecule inhibitors of insulin-regulated aminopeptidase (IRAP) for potential cognitive enhancement in neurodegenerative disorders like Alzheimer's disease. The study identified promising compounds with good solubility but limited blood-brain barrier permeability, leading to further structural optimization of benzylhydroxamic acid derivatives. The research concluded that one compound showed a ten-fold improvement in IRAP inhibition and selectivity over Aminopeptidase N (APN), suggesting potential for targeted therapeutic applications. The study was published in the European Journal of Medicinal Chemistry Reports. [Extracted from the article]