PMID: 12483204

 

    Legend: Sugar

Title : Crystal structure of human dipeptidyl peptidase IV / CD26 in complex with a substrate analog

Abstract :
  1. Dipeptidyl peptidase IV ( DPP-IV / CD26 ) is a multifunctional type II transmembrane serine peptidase
  2. This enzyme contributes to the regulation of various physiological processes, including blood sugar homeostasis , by cleaving peptide hormones, chemokines and neuropeptides
  3. We have determined the 2.5 A structure of the extracellular region of DPP-IV in complex with the inhibitor valine-pyrrolidide
  4. The catalytic site is located in a large cavity formed between the alpha/beta-hydrolase domain and an eight-bladed beta-propeller domain
  5. Both domains participate in inhibitor binding
  6. The structure indicates how substrate specificity is achieved and reveals a new and unexpected opening to the active site