TY - JOUR
T1 - Purinergic receptor P2X7
T2 - A novel target for anti-inflammatory therapy
AU - Mehta, Nisha
AU - Kaur, Maninder
AU - Singh, Manjinder
AU - Chand, Sukhvir
AU - Vyas, Bhawna
AU - Silakari, Pragati
AU - Bahia, Malkeet Singh
AU - Silakari, Om
PY - 2014/1/1
Y1 - 2014/1/1
N2 - 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.
AB - 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.
KW - Caspase-1
KW - Inflammasome
KW - Interleukin-1β
KW - P2X receptor antagonists
KW - Pro-inflammatory cytokines
KW - Purinergic receptor
KW - Toll like receptor (TLR)
UR - http://www.scopus.com/inward/record.url?scp=84891483656&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2013.10.054
DO - 10.1016/j.bmc.2013.10.054
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C2 - 24314880
AN - SCOPUS:84891483656
SN - 0968-0896
VL - 22
SP - 54
EP - 88
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 1
ER -