Collaborative Effort Leads to Potential New Class of Drugs for Crohn’s Disease and Other Autoimmune Disorders

Collaborative Effort Leads to Potential New Class of Drugs for Crohn’s Disease and Other Autoimmune Disorders
A joint effort between researchers at Merck Research Laboratories (named MSD outside the U.S. and Canada), Eindhoven University of Technology (TU/e) and Leiden University, both in The Netherlands, has led to the discovery of a completely new way to block a human nuclear receptor, with possible implications for Crohn's disease. The study, entitled Identification of an allosteric binding site for RORγt inhibition – published in the journal Nature Communications on December 7 – is a breakthrough in drug development research. Nuclear receptors are crucial for a large number of physiological processes, and they are also involved in numerous pathological states. They are, therefore, attractive targets for drug development. Drugs targeting nuclear receptors constitute 13 percent of the medications available on the market today. Currently available drugs all use the same mechanism when interacting with the receptor ­– targeting the receptor’s natural ligand binding site. However, this approach is surrounded by a number of serious disadvantages, such as selectivity problems. Also, developing resistance may render drugs useless, and searching for substances targeting orphan receptors – where the identity of the natural ligand isn't known – is a difficult task when tailoring substances to fit a receptor's main binding site. Researchers, while studying a nuclear receptor called RORγt, discovered that the receptor had another binding site. When a specific class of substances was applied to the receptor, this b
Subscribe or to access all post and page content.