Our laboratory has identified several E3 ligases as key players in oncogenic signaling and cancer regulation (Science, 2009; Cell, 2012). The next goal is to develop small molecule inhibitors to target those E3 ligases.
To achieve this goal, we have formulated a multi-disciplinary research team with diverge expertise ranging from cancer biology, computer-based in slical screening, medicinal chemistry and X-ray crystallography study.
Using such an approach, we have identified a Skp2 small molecule inhibitor displaying potent anti-tumor activity in vivo (Cell, 2013). With such an initiative, we hope to develop small molecule inhibitors targeting diverse E3 ligases and others for cancer therapy.