Crystal structure of human cystatin D, a cysteine peptidase inhibitor with restricted inhibition profile

J Biol Chem. 2005 May 6;280(18):18221-8. doi: 10.1074/jbc.M411914200. Epub 2005 Feb 23.

Abstract

Cystatins are natural inhibitors of papain-like (family C1) and legumain-related (family C13) cysteine peptidases. Cystatin D is a type 2 cystatin, a secreted inhibitor found in human saliva and tear fluid. Compared with its homologues, cystatin D presents an unusual inhibition profile with a preferential inhibition cathepsin S > cathepsin H > cathepsin L and no inhibition of cathepsin B or pig legumain. To elucidate the structural reasons for this specificity, we have crystallized recombinant human Arg(26)-cystatin D and solved its structures at room temperature and at cryo conditions to 2.5- and 1.8-A resolution, respectively. Human cystatin D presents the typical cystatin fold, with a five-stranded anti-parallel beta-sheet wrapped around a five-turn alpha-helix. The structures reveal differences in the peptidase-interacting regions when compared with other cystatins, providing plausible explanations for the restricted inhibitory specificity of cystatin D for some papain-like peptidases and its lack of reactivity toward legumain-related enzymes.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cathepsin B / metabolism
  • Cathepsin H
  • Cathepsin L
  • Cathepsins / antagonists & inhibitors
  • Crystallization
  • Crystallography, X-Ray
  • Cystatins / chemistry*
  • Cystatins / physiology*
  • Cysteine Endopeptidases / metabolism
  • Cysteine Proteinase Inhibitors / chemistry*
  • Cysteine Proteinase Inhibitors / pharmacology
  • Humans
  • Molecular Sequence Data
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / pharmacology
  • Swine

Substances

  • Cystatins
  • Cysteine Proteinase Inhibitors
  • Recombinant Proteins
  • CST5 protein, human
  • Cathepsins
  • Cysteine Endopeptidases
  • Cathepsin B
  • CTSL protein, human
  • Cathepsin L
  • CTSH protein, human
  • Cathepsin H
  • cathepsin S
  • asparaginylendopeptidase

Associated data

  • PDB/1RN7
  • PDB/1ROA