Impact of ectoenzymes on p2 and p1 receptor signaling

Adv Pharmacol. 2011:61:263-99. doi: 10.1016/B978-0-12-385526-8.00009-6.


P2 receptors that are activated by extracellular nucleotides (e.g., ATP, ADP, UTP, UDP, Ap(n)A) and P1 receptors activated by adenosine control a diversity of biological processes. The activation of these receptors is tightly regulated by ectoenzymes that metabolize their ligands. This review presents these enzymes as well as their roles in the regulation of P2 and P1 receptor activation. We focus specifically on the role of ectoenzymes in processes of our interest, that is, inflammation, vascular tone, and neurotransmission. An update on the development of ectonucleotidase inhibitors is also presented.

Publication types

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

MeSH terms

  • Animals
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Nucleotidases / antagonists & inhibitors
  • Nucleotidases / metabolism*
  • Receptors, Purinergic P1 / metabolism*
  • Receptors, Purinergic P2 / metabolism*
  • Signal Transduction* / drug effects


  • Enzyme Inhibitors
  • Receptors, Purinergic P1
  • Receptors, Purinergic P2
  • Nucleotidases