Stat Inhibitors
STAT proteins also known as Signal Transducer and Activator of Transcription are transcription factors involved in a huge repertoire of biological signal transduction cascades leading to embryonic development, programmed cell death, organogenesis, innate immunity, adaptive immunity and cell growth regulation in organisms ranging from insects to man. There are seven mammalian STAT family members that have been identified: STAT1, 2, 3, 4, 5 and 6. They are responsible for conveying information from extracellular sources (e.g. receptor-ligand interaction at the cell surface) to the nucleus so that gene expression can be coordinated to external stimuli. Many growth factors, cytokines, hormones like insulin and their receptors relay intracellular signals through STAT proteins. Tyrosine kinases (for example: Janus Kinase/JAK) associated to the growth factor/cytokine receptors phosphorylate STAT proteins which results in their dimerization and transport into the nucleus followed by binding to target gene regulatory elements thus controlling gene expression. The STAT proteins can be dephosphorylated by nuclear phosphatases, which lead to their inactivation and they are transported out of the nucleus into the cytosol awaiting the next round of activation signal. Under normal physiological conditions, the activation of STATs is tightly regulated. In malignant cells however, STAT proteins become activated constitutively. Due to the versatility of the functional consequences of STAT-mediated signaling, they represent a potentially important target for drug development for a variety of human diseases. BioVision proudly offers an array of STAT inhibitors either directly acting on STAT proteins or other proteins playing critical roles in the STAT signaling pathway.
