title: Purinergic receptor P2X₇: a novel target for anti-inflammatory therapy.
abstract: 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 P2X₇ receptor expressing gene (P2RX₇) knockout (KO) phenotypes. Therefore, newly developed potent antagonists of P2X₇ 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.
authors: Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, Punjab, India.
authors: Nisha
authors: N
authors: Mehta
authors: Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, Punjab, India.
authors: Maninder
authors: M
authors: Kaur
authors: Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, Punjab, India.
authors: Manjinder
authors: M
authors: Singh
authors: Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, Punjab, India.
authors: Sukhvir
authors: S
authors: Chand
authors: Department of Chemistry, Punjabi University, Patiala, 147002, Punjab, India.
authors: Bhawna
authors: B
authors: Vyas
authors: Adina Institute of Pharmaceutical Sciences, Sagar, 470002, Madhya Pradesh, India.
authors: Pragati
authors: P
authors: Silakari
authors: Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, Punjab, India.
authors: Malkeet Singh
authors: MS
authors: Bahia
authors: Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147002, Punjab, India. Electronic address: omsilakari@rediffmail.com.
authors: Om
authors: O
authors: Silakari
mesh_terms: D000893:Anti-Inflammatory Agents / Q000276:immunology* / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D058847:Inflammasomes / Q000276:immunology / Q000378:metabolism*; D053583:Interleukin-1beta / Q000276:immunology / Q000378:metabolism*; D011983:Receptors, Purinergic / Q000276:immunology* / Q000378:metabolism; D015398:Signal Transduction; D051193:Toll-Like Receptors / Q000276:immunology / Q000378:metabolism*
chemical_list: D000893:Anti-Inflammatory Agents; D058847:Inflammasomes; D053583:Interleukin-1beta; D011983:Receptors, Purinergic; D051193:Toll-Like Receptors
keywords: Caspase-1; Inflammasome; Interleukin-1β; P2X(7) receptor antagonists; Pro-inflammatory cytokines; Purinergic receptor; Toll like receptor (TLR)