Abstract# 3721: A novel small molecule exhibits potent growth suppressive activity through the inhibition of constitutive JAK2/STAT3 signaling in breast cancer, pancreatic cancer, and glioblastoma cells.

摘要: The constitutive activation of Signal Transducer and Activator of Transcription 3 (STAT3) is frequently detected in most types of human cancer where it plays important roles in growth, survival, drug-resistance, angiogenesis, and other functions. Targeting constitutive STAT3 signaling is thus an attractive therapeutic approach for these cancers. We have recently developed a novel small molecule STAT3 inhibitor known as FLLL32, which is derived from curcumin (the primary bioactive compound of turmeric). FLLL32 binds to both JAK2 (an upsteam kinase that phosphorylates STAT3) and STAT3, opening a new door for the targeted therapy of cancer. Our results demonstrate that FLLL32 is a potent agent that inhibits JAK2 kinase activity and STAT3 phosphorylation in human breast cancer, pancreatic cancer, and glioblastoma cells with constitutive STAT3 signaling, but has little effect on ERK1/2, PKC-\#948;, mTOR …