Table 1.
Main Approaches To Suppress Target Of Interest | ||||
---|---|---|---|---|
PROTAC | Monoclonal Antibody | Small Molecule Inhibitor | Gene-Editing Via Nucleic Acids |
|
Selectivity | +++ | ++ | + | ++ |
Route Of Administration | PO/IV/SC | IV/SC | PO/IV/SC | IV/SC |
Target Of Interest | Protein on cell surface and inside a cell | Protein on cell surface | Protein on cell surface and inside a cell | DNA or RNA |
Metabolic Stability | ++ | -/+ | ++ | -/+ |
Tissue/Cell Penetration | + | -/+ | ++ | -/+ |
Concentrations Required | Substoichiometric | N/A | Stoichiometric | N/A |
Active Binding Site | - (Can target undruggable and mutated proteins) |
+++ (Can target undruggable proteins) |
+++ (Cannot target mutated proteins) |
- (Can target undruggable proteins) |
Inhibitory Outcome | Blockade of both enzymatic and scaffolding functions | N/A | Impaired enzymatic function | N/A |
Elimination Of POI | +++ | - | - | +++ |
Catalytic Mechanism Of Action | +++ | - | - | +++ |
Systemic Delivery | +++ | +++ | +++ | - |