Crystallization and preliminary diffraction studies of porcine pancreatic elastase in complex with a novel inhibitor

Protein Pept Lett. 2007;14(1):93-5. doi: 10.2174/092986607779117173.

Abstract

Porcine pancreatic elastase (PPE) was crystallized in complex with a novel inhibitor at pH 5 and X-ray diffraction data were collected at a synchrotron source to 1.66 A. Crystals belong to the orthorhombic space group P2(1)2(1)2(1), with unit cell parameters a = 50.25 A, b = 57.94 A and c = 74.69 A. PPE is often used as model for drug target, due to its structural homology with the important therapeutic target human leukocyte elastase (HLE). Elastase is a serine protease that belongs to the chymotrypsin family, which has the ability to degrade elastin, an important component in connective tissues. Excessive elastin proteolysis leads to a number of pathological diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Crystallization
  • Crystallography, X-Ray
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Models, Molecular
  • Molecular Structure
  • Pancreas / enzymology*
  • Pancreatic Elastase / antagonists & inhibitors*
  • Pancreatic Elastase / chemistry*
  • Pancreatic Elastase / isolation & purification
  • Swine*

Substances

  • Enzyme Inhibitors
  • Pancreatic Elastase