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