Discovery of novel elongator protein 2 inhibitors by compound library screening using surface plasmon resonance

摘要: Tumour necrosis factor-α (TNF-α) is a pleiotropic cytokine that becomes elevated in chronic inflammatory states, including slowing down osteogenic differentiation, which leads to bone dysplasia long-term microenvironments. The elongator complex plays role gene regulation and association with various cellular activities, the downstream signal transduction of TNF-α cells. To find an inhibitor Elongator Protein 2 (Elp2), we performed compound library screen verified pharmaceutical effects candidate compounds on mouse myoblast cell (C2C12) osteoblastic cells (MC3T3-E1). commercial FDA-approved drug (FD) bioactive (BC) were used as libraries. After label-free, high-throughput affinity measurement surface plasmon resonance (SPRi), seven kinds showed binding Elp2 protein. candidates then perform inhibition test TNF-α-induced C2C12 MC3T3-E1 lines. One reduced differentiation suppression caused by resuscitated alkaline phosphatase (ALP) activity, mineralization intensity expression marker genes. results our study provide competitive mitigate differentia.