P2X7 is a purinergic receptor activated by high concentrations of extracellular ATP, which is released as a danger signal in response to tissue damage, inflammation, and infection. Since its cloning in the 1990s, studies on P2X7 physiological functions have greatly advanced, revealing that it is intimately involved in the formation of inflammatory mediators, such as cytokines, reactive oxygen species, and prostaglandins, as well as cell death. These biological activities were confirmed through in vivo tests, which demonstrated their role in pain, inflammation, and neurodegeneration. Therefore, blocking the P2X7 receptor could be a promising strategy for treating these diseases and the use of P2X7 antagonists has shown beneficial effects, including the reduction of pain, inflammation, neuronal damage, and cognitive impairment.
The development of novel P2X7 antagonists has been driven by both traditional high-throughput screening and structure-based design approaches. Several P2X7 antagonists have been identified and characterized, with different chemical structures, binding modes, and
selectivity profiles. Some of the most promising P2X7 antagonists are negative allosteric modulators, which bind to a site distinct from the ATP-binding pocket and inhibit the receptor function. Selective P2X7 antagonists have progressed to clinical trials for treating rheumatoid
arthritis and depression. Despite many efforts, no drug has been approved for therapy yet.
Many challenges and limitations hinder the development of novel P2X7 antagonists, but they provide valuable lessons for improving the ones under development. Considering the state-of-the-art of artificial intelligence technology, the use of these algorithms can speed up this process.
This Research Topic aims to present the latest advances in research on the development and applications of P2X7 antagonists in inflammatory conditions, cancer, pain, and neurological diseases from the pre-clinical to clinical trials, pointing to the future directions for this emerging research field. High-quality original research articles, and full-length, mini, or systematic reviews are welcome in this collection.
Keywords:
P2X7 antagonists, purinergic receptor, drug development, inflammatory conditions, pain, cancer, neurological disorders
Important Note:
All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.
P2X7 is a purinergic receptor activated by high concentrations of extracellular ATP, which is released as a danger signal in response to tissue damage, inflammation, and infection. Since its cloning in the 1990s, studies on P2X7 physiological functions have greatly advanced, revealing that it is intimately involved in the formation of inflammatory mediators, such as cytokines, reactive oxygen species, and prostaglandins, as well as cell death. These biological activities were confirmed through in vivo tests, which demonstrated their role in pain, inflammation, and neurodegeneration. Therefore, blocking the P2X7 receptor could be a promising strategy for treating these diseases and the use of P2X7 antagonists has shown beneficial effects, including the reduction of pain, inflammation, neuronal damage, and cognitive impairment.
The development of novel P2X7 antagonists has been driven by both traditional high-throughput screening and structure-based design approaches. Several P2X7 antagonists have been identified and characterized, with different chemical structures, binding modes, and
selectivity profiles. Some of the most promising P2X7 antagonists are negative allosteric modulators, which bind to a site distinct from the ATP-binding pocket and inhibit the receptor function. Selective P2X7 antagonists have progressed to clinical trials for treating rheumatoid
arthritis and depression. Despite many efforts, no drug has been approved for therapy yet.
Many challenges and limitations hinder the development of novel P2X7 antagonists, but they provide valuable lessons for improving the ones under development. Considering the state-of-the-art of artificial intelligence technology, the use of these algorithms can speed up this process.
This Research Topic aims to present the latest advances in research on the development and applications of P2X7 antagonists in inflammatory conditions, cancer, pain, and neurological diseases from the pre-clinical to clinical trials, pointing to the future directions for this emerging research field. High-quality original research articles, and full-length, mini, or systematic reviews are welcome in this collection.
Keywords:
P2X7 antagonists, purinergic receptor, drug development, inflammatory conditions, pain, cancer, neurological disorders
Important Note:
All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.