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Zinc-Binding Group Peptides

Peptides containing zinc-binding pharmacophores for metalloprotease inhibition including hydroxamates, carboxylates, and thiols.

By Encyclopeptide Editorial | 1 min read
zinc-binding metalloprotease hydroxamate pharmacophore enzyme-inhibitor

Overview

Zinc-binding groups (ZBGs) are pharmacophoric moieties that coordinate with catalytic zinc ions in metalloproteases. They are essential components of many enzyme inhibitor drugs.

Common Zinc-Binding Groups

ZBGZinc CoordinationSelectivityStability
HydroxamateBidentateModerateModerate
CarboxylateBidentateHighHigh
ThiolBidentateHighLow (redox)
PhosphinateBidentateHighHigh
N-hydroxyamideBidentateModerateModerate

Therapeutic Applications

  • Matrix metalloproteinase inhibitors: Marimastat, batimastat
  • ACE inhibitors: Enalapril, lisinopril (carboxylate)
  • Histone deacetylase inhibitors: Vorinostat (hydroxamate)
  • Proteasome inhibitors: Bortezomib (boronic acid, analogous)

Chemical Identity

PropertyValue
NameZinc-Binding Group Peptides
CategoryTherapeutic Peptides

References

  1. Encyclopeptide Database. “Zinc-Binding Group Peptides” monograph. encyclopeptide.com.

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