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To Inhibit or Enhance? Is There a Benefit to Positive Allosteric Modulation of P2X Receptors? [PDF]

open access: yesFrontiers in Pharmacology, 2020
The family of ligand-gated ion channels known as P2X receptors were discovered several decades ago. Since the cloning of the seven P2X receptors (P2X1-P2X7), a huge research effort has elucidated their roles in regulating a range of physiological and ...
Leanne Stokes   +3 more
doaj   +2 more sources

P2X receptors. [PDF]

open access: yesPhilos Trans R Soc Lond B Biol Sci, 2016
Extracellular adenosine 5′-triphosphate (ATP) activates cell surface P2X and P2Y receptors. P2X receptors are membrane ion channels preferably permeable to sodium, potassium and calcium that open within milliseconds of the binding of ATP. In molecular architecture, they form a unique structural family.
North RA.
europepmc   +4 more sources

P2X Receptors: Potential Therapeutic Targets for Symptoms Associated With Lung Cancer — A Mini Review [PDF]

open access: yesFrontiers in Oncology, 2021
Symptoms associated with lung cancer mainly consist of cancer-associated pain, cough, fatigue, and dyspnea. However, underlying mechanisms of lung cancer symptom clusters remain unclear.
Yonglin Mai   +5 more
doaj   +2 more sources

Activity of Peptides Modulating the Action of p2x Receptors: Focus on the p2x7 Receptor [PDF]

open access: yesPharmaceuticals
P2X receptors are a family of ATP-gated ion channels widely distributed in various tissues, especially in neuronal cells and hematopoietic cells. ATP activates P2X receptors, causing the opening of an ionic channel with preferential permeability to the ...
Jonathas Albertino De Souza Oliveira Carneiro   +3 more
doaj   +2 more sources

Pharmacology of P2X Receptors and Their Possible Therapeutic Potential in Obesity and Diabetes [PDF]

open access: yesPharmaceuticals
The role of P2X ionotropic receptors in the behavior of purinergic signaling on pathophysiological processes has been widely studied. In recent years, the important participation of P2X receptors in physiological and pathological processes, such as ...
Guillermo A. Cabral-García   +5 more
doaj   +2 more sources

Activated P2X receptors can up-regulate the expressions of inflammation-related genes via NF-κB pathway in spotted sea bass (Lateolabrax maculatus) [PDF]

open access: yesFrontiers in Immunology, 2023
P2X receptors, including seven subtypes, i.e., P2X1-7, are the ligand-gated ion channels activated by the extracellular ATP playing the critical roles in inflammation and immune response.
Zhaosheng Sun   +13 more
doaj   +2 more sources

Subtype-Specific Ligand Binding and Activation Gating in Homomeric and Heteromeric P2X Receptors [PDF]

open access: yesBiomolecules
P2X receptors are ATP-activated, non-specific cation channels involved in sensory signalling, inflammation, and certain forms of pain. Investigations of agonist binding and activation are essential for comprehending the fundamental mechanisms of receptor
Xenia Brünings   +4 more
doaj   +2 more sources

The Molecular Determinants of Small-Molecule Ligand Binding at P2X Receptors [PDF]

open access: yesFrontiers in Pharmacology, 2018
P2X receptors are trimeric eukaryotic ATP-gated cation channels. Extracellular ATP—their physiological ligand—is released as a neurotransmitter and in conditions of cell damage such as inflammation, and substantial evidence implicates P2X receptors in ...
Gaia Pasqualetto   +2 more
doaj   +2 more sources

Structural insights into the orthosteric inhibition of P2X receptors by non-ATP analog antagonists [PDF]

open access: yeseLife
P2X receptors are extracellular ATP-gated ion channels that form homo- or heterotrimers and consist of seven subtypes. They are expressed in various tissues, including neuronal and nonneuronal cells, and play critical roles in physiological processes ...
Danqi Sheng   +7 more
doaj   +2 more sources

Radioligands Targeting the Purinergic P2X Receptors [PDF]

open access: yesCells
Purinergic P2X receptors have a wide distribution within the body and modulate a number of physiological processes, being also involved in the development and progression of inflammation-, neuroinflammation-, neurodegeneration-, and cancer-related ...
Diego Dal Ben   +7 more
doaj   +2 more sources

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