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. Author manuscript; available in PMC: 2021 Sep 10.
Published in final edited form as: J Med Chem. 2020 Mar 26;63(17):8880–8900. doi: 10.1021/acs.jmedchem.9b01927

Figure 8.

Figure 8.

Properties of bioactive therapeutic modalities. Current and emerging strategies to affect downstream biology include antibodies (rituximab, PDB code 4KAQ), ASOs (Nusinersen), small molecules (TGP-210), and targeted degradation approaches (TGP-210 RIBOTAC). Each targets a unique space, but RIBOTACs can affect bioactivity of RNA without binding to a functional site. RIBOTACs also degrade their targets in a catalytic and substoichiometric fashion, thus allowing greater potency. Small-molecule-based modalities are advantageous as their physicochemical properties can be potentially medicinally optimized. ASO, small molecule, and targeted degradation models were made using the Online SMILES Generator (National Cancer Institute).