This collaborative team - composed of groups from NCI, CBC/NExT, U Penn, Vanderbilt, UAB, UNM and NCATS - aims to build on previous research by uncovering novel inhibitors of LDHA for anticancer indications. During this period, the NCATS group, as part of the LDHA collaborative team, has worked to characterize the mechanism of action of the novel LDH inhibitors, guide in vivo efficacy model development, assess in vitro activity of novel LDH degraders, and assess in vitro activity of novel tumor concentrating LDH inhibitors. Multiple publications are under preparation and technology is under negotiation for out-licensing with a small biotech.
| Rai, Ganesha; Brimacombe, Kyle R; Mott, Bryan T et al. (2017) Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem 60:9184-9204 |
