Cisbio eBook - 18

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Advantages
May Place Peptides
Ahead of SmallMolecule Drugs
Richard A. Stein M.D., Ph.D.

P

eptide 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.

18 | GENengnews.com

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.
For example, peptide therapeutics need to

ADDITIONAL CONTENT

Technical Note
Tips to pharmacological
characterization of
PPI inhibitors

Download Technical Note


http://learn.cisbio.com/lp/tn-how-to-access-true-kd-values-in-ppi-assays http://learn.cisbio.com/lp/tn-how-to-access-true-kd-values-in-ppi-assays http://www.GENengnews.com

Cisbio eBook

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