Gene expression/regulation ligand binding

Dervan PB, Poulin-Kerstien AT, Fechter EJ, Edelson BS (2005) Regulation of Gene Expression by Synthetic DNA-Binding Ligands. 253 1-31 Dias N, Vezin H, Lansiaux A, Badly C (2005) Topoisomerase Inhibitors of Marine Origin and Their Potential Use as Anticancer Agents. 253 89-108 DiMauro E, see Saladino R (2005) 259 29-68... 

In most instances, ligand binding appears to promote receptor dimerization, bringing their associated JAKs into close proximity (Figure 4.2). The JAKs then phosphorylate — and hence activate — each other (transphosphorylation). The activated kinases subsequently phosphorylate specific tyrosine residues on the receptor itself. This promotes direct association between one or more members of a family of cytoplasmic proteins (STATs) and the receptor. Once docked at the receptor surface, the STATs are in turn phosphorylated (and hence activated) by the JAKs (Figure 4.2). As described below, activated STATs then translocate to the nucleus and directly regulate expression of IFN and other cytokine-sensitive genes. 

Collins, S., M. G. Caron, and R. J. Lefkowitz, From ligand binding to gene expression New insights into the regulation of G-protein-coupled receptors. Trends Biochem. Sci. 17 37-39, 1992. 

---