In March, Vanderbilt University and the global pharmaceutical company Boehringer Ingelheim announced the expansion of their successful existing collaboration to develop novel anti-cancer compounds.

The expanded research partnership will focus on the discovery and development of new chemical therapeutics targeting the pro-survival protein MCL1 as a potential therapy against MCL1 dependent cancers. This is the third collaboration between Boehringer Ingelheim and Vanderbilt to pursue discoveries made in the laboratory of Stephen Fesik, PhD, the Orrin H. Ingram II Professor of Cancer Research and professor of Biochemistry, Pharmacology and Chemistry at Vanderbilt University School of Medicine.

MCL1, when overexpressed, can prevent cancer cells from undergoing programmed cell death (also known as apoptosis). This necessitates the discovery of a molecule that binds extremely tightly and selectively to MCL1 in order to sufficiently induce on-target, mechanism-based cancer cell death. Using fragment-based drug discovery methods they developed, Fesik and his colleagues have discovered potent small molecules that bind to and inhibit MCL1 and which in laboratory studies can stop tumor growth.

The previous agreements involve development of small molecule inhibitors of KRAS, a molecular switch that plays a central role in the onset of some of the deadliest cancers, as well as SOS, the protein that activates the KRAS switch.