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Table 1 Comparison among PROTACs, small molecule inhibitors (SMIs), monoclonal antibodies, and therapeutic nucleic acids (TNAs)

From: Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

PROTACs SMIs Monoclonal antibodies TNAs
Highly selective Poor selectivity Selective Selective
Oral bioavailability can be achieved Oral bioavailability is easy to achieve Oral bioavailability is not achievable Oral bioavailability is not achievable
Can target proteins on cell surface and inside a cell Can target proteins on cell surface and inside a cell Can only target proteins on cell surface, not inside a cell Target DNA or RNA
Tissue penetration is good Tissue penetration is good Tissue penetration is poor Tissue penetration is poor
Metabolic stability is good Metabolic stability is good Metabolic stability is poor Metabolic stability is poor
Sub-stoichiometric concentrations are required Stoichiometric concentrations are required N/A N/A
Can target proteins without an active binding site i.e. undruggable proteins Difficult to target proteins without an active binding site N/A N/A
Can target mutated proteins Cannot target mutated proteins N/A N/A
Degradation blocks both enzymatic and scaffolding functions Inhibition blocks only enzymatic functions N/A N/A