Peptide Therapeutics Near the Sweetest Spots

by Richard Stein, M.D., Ph.D.
April 01, 2018

Advantages May Place Peptides Ahead of Small-Molecule Drugs

Peptide therapeutics would seem to occupy a sweet spot between small molecules and biologics. Small molecules, which represent the majority of clinical drugs, preferentially bind hydrophobic pockets or cavities, but targeting them to protein interfaces that are large or shallow, or contain combinations of polar and apolar residues, is challenging.

Biologics, or larger molecules, use more extensive contact areas and can modulate protein–protein interactions extracellularly, but are difficult to deliver into cells.

The difficulties posed by small molecules and biologics could be avoided by peptide therapeutics, which present drug developers with distinct advantages. These include simpler production, lower costs, and superior safety and tolerability. Consequently, some drug developers see peptide therapeutics as an attractive means of reaching targets that are known to be therapeutically relevant but are, as yet, “undruggable.” Peptide therapeutics, however, need to manifest sweet spots of their own.

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