Discovery of Lomitapide as a Novel Mast Cell Regulatory Agent Through Chemical Library Screening.

ABSTRACT: Allergic diseases are a global health concern, and new molecular insights and therapeutic agents are necessary to support future research and interventions. Mast cells (MCs) play a crucial role in allergic reactions, in which antigen (Ag) cross-linking of high-affinity receptors (FcεRI) activates signaling pathways, leading to the release of various types of inflammatory mediators. We developed a chemical library screening system using RBL-2H3 cells, a widely used MC model, to identify anti-allergic agents. This method revealed that lomitapide, a microsomal triglyceride transfer protein (MTTP) inhibitor, is a novel MC regulatory agent. Furthermore, lomitapide was found to inhibit MC degranulation by altering MC plasma membrane dynamics, specifically by preventing endocytosis of plasma memb

SUBMITTER: Mamorita S 

PROVIDER: S-EPMC12925385 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature