Science
"UPPTHERA develops innovative drugs employing TPD science"
UPS(Ubiquitin Proteasome System) is an intracellular protein degradation pathway which breaks about 80% of intracellular proteins : TPD(Targeted Protein Degradation) is a novel drug modality degrading disease-causing proteins by harnessing the UPS.
① PROTAC draws POI intro a ternary complex with E3 Ligase
② E3 Ligase then polyubiquitinates lysine residues on the surface of POI
③ Proteasome recognizes the poly-ubiqutin chain and degrades POI
Degraders have competitive edges in solving unmet needs which have not been solved by traditional drug modalities
Small Molecule Inhibitor ![]()
SM inhibitor could be developed only for a protein that possesses binding pocket wity an active site
(15% of total disease-causing protein)
'Inhibition' of disease-causing proteins
Low target selectivity / Off-target issue
1 drug inhibits 1 protein ![]()
(Occupancy-driven MoA)
VS
Degrader (PROTAC) ![]()
PROTAC could degrade a disease-causing protein as long as it binds the protein in any manners to make it ubquitinated, regardless of presence of binding pocket in the protein
'Degradation' of disease-causing proteins
Enhance target selectivity
1 drug degrades multiple proteins ![]()
(Event-driven MoA)
