Novel small molecule inhibitor has immunosuppression properties

Immunosuppression is one approach to care some autoimmune diseases, such as rheumatoid arthritis. Etarnercept and cortisone are currently used to care these disorders. In Nature Medicine has been recently published a work that describes a novel possible therapy for this kind of disease. Scientists focussed their attention on small molecule inhibitors of immunoproteasome. This cellular compartment has been identified in monocytes and lymphocytes and is specialized in generating MCH I peptides.

The selective inhibitor of LMP7, a specific protein belonged to immunoproteasome, down-regulated the expression of MCH I complex and reduced the level of some cytokines, for instance IL23, IL6 and TNF. All these molecules are implicated in the autoimmune response in rheumatoid arthritis. The expression of other cytokines were tuned in following inhibitor exposure. The small molecule inhibitor could have pleiotropic effects of various cell types, by ameliorating drug efficacy. In animal models, indeed, this molecules gained better results than Etanercept in TNF blockade and consequently showed faster resolution of symptoms of immune disorders. This study represents a great hope for all people that are affected by rheumatoid arthritis, but a lot of work still to be done before entering in clinical phase.