Update of P2X receptor properties and their pharmacology: IUPHAR Review 30

P Illes, CE Müller, KA Jacobson… - British Journal of …, 2021 - Wiley Online Library
The known seven mammalian receptor subunits (P2X1–7) form cationic channels gated by
ATP. Three subunits compose a receptor channel. Each subunit is a polypeptide consisting …

[HTML][HTML] Structural and functional features of the P2X4 receptor: an immunological perspective

JM Kanellopoulos, CLC Almeida-da-Silva… - Frontiers in …, 2021 - frontiersin.org
Extracellular nucleotides are important mediators of activation, triggering various responses
through plasma membrane P2 and P1 receptors. P2 receptors are further subdivided into …

[HTML][HTML] The P2X4 receptor: cellular and molecular characteristics of a promising neuroinflammatory target

RA Sophocleous, L Ooi, R Sluyter - International Journal of Molecular …, 2022 - mdpi.com
The adenosine 5′-triphosphate-gated P2X4 receptor channel is a promising target in
neuroinflammatory disorders, but the ability to effectively target these receptors in models of …

[HTML][HTML] Macrophage Cx43 is necessary for fibroblast cytosolic calcium and lung fibrosis after injury

A Bhattacharyya, P Torre, P Yadav… - Frontiers in …, 2022 - frontiersin.org
Macrophages are paracrine signalers that regulate tissular responses to injury through
interactions with parenchymal cells. Connexin hemichannels have recently been shown to …

Structural basis of the negative allosteric modulation of 5-BDBD at human P2X4 receptors

S Bidula, IB Nadzirin, M Cominetti, H Hickey… - Molecular …, 2022 - ASPET
The P2X4 receptor is a ligand-gated ion channel activated by extracellular ATP. P2X4
activity is associated with neuropathic pain, vasodilation, and pulmonary secretion and is …

P2X receptors: Insights from the study of the domestic dog

R Sluyter, RA Sophocleous, L Stokes - Neuropharmacology, 2023 - Elsevier
Fifty years ago, the late Geoffrey Burnstock described the concept of purinergic nerves and
transmission bringing into existence the broader concepts of purinergic signaling including …

Pharmacological interaction and immune response of purinergic receptors in therapeutic modulation

SH Kiaie, Z Hatami, MS Nasr, P Pazooki, S Hemmati… - Purinergic …, 2023 - Springer
Nucleosides and purine nucleotides serve as transmitter and modulator agents that extend
their functions beyond the cell. In this context, purinergic signaling plays a crucial role in …

Structure–Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists

KS Toti, R Verma, MJ McGonnigle… - Journal of medicinal …, 2022 - ACS Publications
We analyzed the P2X4 receptor structure–activity relationship of a known antagonist 5, a 1,
5-dihydro-2 H-naphtho [1, 2-b][1, 4] diazepine-2, 4 (3 H)-dione. Following extensive …

[HTML][HTML] 6-furopyridine hexamethylene amiloride is a non-selective P2X7 receptor antagonist

P Cuthbertson, A Elhage, D Al-Rifai, RA Sophocleous… - Biomolecules, 2022 - mdpi.com
P2X7 is an extracellular adenosine 5′-triphopshate (ATP)-gated cation channel present on
leukocytes, where its activation induces pro-inflammatory cytokine release and ectodomain …

[HTML][HTML] RNA-seq reveals that anti-obesity irisin and triiodothyronine (T3) hormones differentially affect the purinergic signaling transcriptomics in differentiated human …

LS Mathias, C Herman-de-Sousa, SS Cury… - … et Biophysica Acta (BBA …, 2023 - Elsevier
The anti-obesity thyroid hormone, triiodothyronine (T3), and irisin, an exercise-and/or cold-
induced myokine, stimulate thermogenesis and energy consumption while decreasing lipid …