Purinergic receptor P2X7: A novel target for anti-inflammatory therapy

Nisha Mehta, Maninder Kaur, Manjinder Singh, Sukhvir Chand, Bhawna Vyas, Pragati Silakari, Malkeet Singh Bahia, Om Silakari

Research output: Contribution to journalReview articlepeer-review

88 Scopus citations


Purinergic receptors, also known as purinoceptors, are ligand gated membrane ion channels involved in many cellular functions. Among all identified purinergic receptors, P2X7 subform is unique since it induces the caspase activity, cytokine secretion, and apoptosis. The distribution of P2X7 receptors, and the need of high concentration of ATP required to activate this receptor exhibited its ability to function as 'danger' sensor associated with tissue inflammation and damage. Further, the modulation of other signalling pathways associated with P2X7 has also been proposed to play an important role in the control of macrophage functions and inflammatory responses, especially towards lipopolysaccharides. Experimentally, researchers have also observed the decreased severity of inflammatory responses in P2X 7 receptor expressing gene (P2RX7) knockout (KO) phenotypes. Therefore, newly developed potent antagonists of P2X 7 receptor would serve as novel therapeutic agents to combat various inflammatory conditions. In this review article, we tried to explore various aspects of P2X7 receptors including therapeutic potential, and recent discoveries and developments of P2X7 receptor antagonists.

Original languageEnglish
Pages (from-to)54-88
Number of pages35
JournalBioorganic and Medicinal Chemistry
Issue number1
StatePublished - 1 Jan 2014
Externally publishedYes


  • Caspase-1
  • Inflammasome
  • Interleukin-1β
  • P2X receptor antagonists
  • Pro-inflammatory cytokines
  • Purinergic receptor
  • Toll like receptor (TLR)


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