Transcription factors drug development

Finally, development of drugs targeted toward modification of kinases and phosphatases required for activation or inhibition of particular transcription factors is a promising therapeutic approach. The problem with this paradigm is the specificity of the kinases and phosphatases, since they will often act enzymatically on multiple proteins (see Chs 24 and 25). Furthermore, such drugs often lack specificity and may interact with multiple kinases or phosphatases. 

Nuclear factor kappa B (NF-kB) serves as a central regulator of the human immune and inflammatory response, and is a family of inducible transcription factors found virtually ubiquitously in all cells and functions in a variety of human diseases including those related to inflammation, cancer, asthma, atherosclerosis, AIDS, septic shock, and arthritis. Due to its role in a wide variety of diseases, NF-kB has become one of the major targets for drug development. Inhibition of NF-kB activity potentially contributes to cancer chemoprevention [27,28]. 

NF-AT3 also cooperates with GATA-4, a heart-specific transcription factor. When Ca2+ levels rise in a stressed heart, NF-AT3 moves to the nucleus and binds to GATA-4 and both turn on genes responsible for cardiac hypertrophy. The clinical importance of cardiac hypertrophy, which eventually causes heart failure, makes the development of drugs that act like immunosuppressives, preventing nuclear import of NF-AT3, an active area of research into control of cardiac hypertrophy. ... 

---