Recent progress in the discovery of antagonists acting at P2X7receptor
- 1 March 2005
- journal article
- Published by Taylor & Francis in Expert Opinion on Therapeutic Patents
- Vol. 15 (3) , 271-287
- https://doi.org/10.1517/13543776.15.3.271
Abstract
The P2X7 receptor is involved in several processes relevant to inflammation (cytokine release, nitric oxide (NO) generation, killing of intracellular pathogens, cytotoxicity), thus, it may be an appealing target for pharmacological intervention. These findings prompted a number of drug companies, including AstraZeneca, King and Pfizer to initiate small-molecule programmes taking a number of different approaches, which are reviewed in this review article. The extensive use of high-throughput screening approaches, utilising diverse compound library sources, has lead to the identification of two important lead series (adamantane and benzenamide derivatives) acting on P2X7.Keywords
This publication has 38 references indexed in Scilit:
- P2X7 polymorphism and chronic lymphocytic leukaemia: lack of correlation with incidence, survival and abnormalities of chromosome 12Leukemia, 2003
- Synthesis and Biological Activity of N-Arylpiperazine-Modified Analogues of KN-62, a Potent Antagonist of the Purinergic P2X7 ReceptorJournal of Medicinal Chemistry, 2003
- P2X7 Receptor Cell Surface Expression and Cytolytic Pore Formation Are Regulated by a Distal C-terminal RegionJournal of Biological Chemistry, 2003
- Expression of the P2X7 Receptor Subunit of the Adenosine 5’-Triphosphate-Gated Ion Channel in the Developing and Adult Rat CochleaAudiology and Neurotology, 2003
- P2X7 receptors activate protein kinase D and p42/p44 mitogen-activated protein kinase (MAPK) downstream of protein kinase CBiochemical Journal, 2002
- Differential Assembly of Rat Purinergic P2X7 Receptor in Immune Cells of the Brain and PeripheryJournal of Biological Chemistry, 2001
- Extracellular ATP Activates Transcription Factor NF-κB through the P2Z Purinoreceptor by Selectively Targeting NF-κB p65 (RelA)The Journal of cell biology, 1997
- The isoquinoline derivative KN‐62 a potent antagonist of the P2Z‐receptor of human lymphocytesBritish Journal of Pharmacology, 1997
- The Cytolytic P 2Z Receptor for Extracellular ATP Identified as a P 2X Receptor (P2X 7 )Science, 1996
- Pharmacology of Protein Kinase InhibitorsAnnual Review of Pharmacology and Toxicology, 1992