rethinkPeptides Search
Menu
Study breakdown

Strategies for Locking Peptides Into Alpha-Helix Shape: A Drug Design Review

ReviewModerate evidence
The takeaway

This review covers chemical strategies for stabilizing peptide alpha-helices — stapling, hydrogen bond surrogates, side-chain crosslinks — that make helical peptide drugs stable and functional for clinical development.

Key finding

Contemporary helix stabilization strategies include hydrocarbon stapling, hydrogen bond surrogates, salt bridges, disulfide crosslinks, and unnatural

What the researchers found

Contemporary helix stabilization strategies include hydrocarbon stapling, hydrogen bond surrogates, salt bridges, disulfide crosslinks, and unnatural amino acids — chemical approaches that lock therapeutic peptides into bioactive helical conformations for clinical development.

Why it matters

Relevant for cyclic-peptides, peptide-design.

How the study worked

review study.

What this study cannot tell us

See abstract.

How to read the evidence

moderate evidence.

When this study was published

Published in 2008.

The bigger picture

Advances peptide research.

Questions still open

  • Further research needed.
  • Clinical translation to evaluate.

Common questions

What was studied?
Strategies for Locking Peptides Into Alpha-Helix Shape: A Drug Design Review
What was found?
This review covers chemical strategies for stabilizing peptide alpha-helices — stapling, hydrogen bond surrogates, side-chain crosslinks — that make helical peptide drugs stable and functional for clinical development.

Read the original research

Contemporary strategies for the stabilization of peptides in the alpha-helical conformation.

Current opinion in chemical biology, 12(6), 692-7

Citation

Henchey, Laura K; Jochim, Andrea L; Arora, Paramjit S. (2008). Contemporary strategies for the stabilization of peptides in the alpha-helical conformation.. Current opinion in chemical biology, 12(6), 692-7. https://doi.org/10.1016/j.cbpa.2008.08.019