Project highlights: the assay was developed and screened, and a lead series was identified. Medicinal chemistry was implemented to further improve activity of the compound, and secondary assays were undertaken to demonstrate activity in cells. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.
| Pacold, Michael E; Brimacombe, Kyle R; Chan, Sze Ham et al. (2016) A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol 12:452-8 |
| Pacold, Michael E; Brimacombe, Kyle R; Chan, Sze Ham et al. (2016) Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol 12:656 |
