We are engaged with the University of Minnesota’s community of scholars, and we can leverage our synthetic expertise to enable and accelerate research focused on addressing grand challenges. We initiated a collaboration on bromodomain inhibitors. Bromodomains function at a key point in DNA replication. Inhibiting bromodomain binding can be used to prevent cell proliferation and thereby treat cancer. Several bromodomain inhibitors are being evaluated in clinical trials; however, most of these inhibitors are not selective for one of the 61 human bromodomains. Developing selective inhibitors is vital to maximizing therapeutic potential, minimizing side effects, and understanding the divergent functions of different bromodomains. Presently, we are working with the Pomerantz and Harki labs to develop potent and selective bromodomain inhibitors.
Carlson, A.S.; Cui, H.; Divakaran, A.; Johnson, J.A.; Brunner, R.M.; Pomerantz, W.C.K.*; Topczewski, J.J.* ACS Med. Chem. Lett., 2019, 10, 1296-1301. (doi.org/10.1021/acsmedchemlett.9b00227)
Divakaran, A.; Talluri, S. K.; Ayoub, A. M.; Mishra, N.; Cui, H.; Widen, J. C.; Berndt, N.; Zhu, J.; Carlson, A. S.; Topczewski, J. J.; Schönbrunn, E.; Harki, D. A.; Pomerantz, W. C. K. J. Med. Chem., 2018, 61, 9316–9334.