Our Approach
We focus on induced proximity technology such as Targeted Protein Degradation (TPD), which leverages heterobifunctional chemical molecules. TPD promotes ubiquitination of target proteins by inducing the proximity between target proteins and E3 ubiquitin ligases, leading to protein degradation by the proteasome.
Conventional small molecule drugs require a functional deep pocket in the target protein. TPD molecules, however, only weakly bind to a shallow pocket on the target protein, catalytically inducing the proximity of the target protein to the E3 ligase, and selectively degrading the target protein. TPD can be applied to a wider range of proteins, including historically undruggable proteins, because it can use shallow pockets normally present in most proteins.
*Learn more about Astellas’ Primary Focus TPD here.
ASP3082
Applying the concept of TPD we have discovered ASP3082, a first-in-class and selective KRAS G12D degrader. Phase I clinical trials are underway in the U.S. to study the efficacy and safety of the drug for pancreatic cancer, colorectal cancer, and lung cancer with KRAS G12D mutation.