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 …

Structural and functional basis for understanding the biological significance of P2X7 receptor

MÁ Martínez-Cuesta, MA Blanch-Ruiz… - International journal of …, 2020 - mdpi.com
The P2X7 receptor (P2X7R) possesses a unique structure associated to an as yet not fully
understood mechanism of action that facilitates cell permeability to large ionic molecules …

A small-molecule P2RX7 activator promotes anti-tumor immune responses and sensitizes lung tumor to immunotherapy

L Douguet, S Janho dit Hreich, J Benzaquen… - Nature …, 2021 - nature.com
Only a subpopulation of non-small cell lung cancer (NSCLC) patients responds to
immunotherapies, highlighting the urgent need to develop therapeutic strategies to improve …

Piperine promotes autophagy flux by P2RX4 activation in SNCA/α-synuclein-induced Parkinson disease model

R Li, Y Lu, Q Zhang, W Liu, R Yang, J Jiao, J Liu… - Autophagy, 2022 - Taylor & Francis
Olfactory dysfunction, one of the earliest non-motor symptoms of Parkinson disease (PD), is
accompanied by abnormal deposition of SNCA/α-synuclein in the olfactory bulb (OB). The …

Microglia specific drug targeting using natural products for the regulation of redox imbalance in neurodegeneration

SK Maurya, N Bhattacharya, S Mishra… - Frontiers in …, 2021 - frontiersin.org
Microglia, a type of innate immune cell of the brain, regulates neurogenesis, immunological
surveillance, redox imbalance, cognitive and behavioral changes under normal and …

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 …

Neurosteroids as positive and negative allosteric modulators of ligand-gated ion channels: P2X receptor perspective

S Sivcev, E Kudova, H Zemkova - Neuropharmacology, 2023 - Elsevier
Neurosteroids are steroids synthesized de novo in the brain from cholesterol in an
independent manner from peripheral steroid sources. The term “neuroactive steroid …

To inhibit or enhance? Is there a benefit to positive allosteric modulation of P2X receptors?

L Stokes, S Bidula, L Bibič, E Allum - Frontiers in pharmacology, 2020 - frontiersin.org
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 …

Drug development in channelopathies: Allosteric modulation of ligand-gated and voltage-gated ion channels

Y Zhang, K Wang, Z Yu - Journal of medicinal chemistry, 2020 - ACS Publications
Ion channels have been characterized as promising drug targets for treatment of numerous
human diseases. Functions of ion channels can be fine-tuned by allosteric modulators …

Inhibiting the P2X4 receptor suppresses prostate cancer growth in vitro and in vivo, suggesting a potential clinical target

J He, Y Zhou, HM Arredondo Carrera, A Sprules… - Cells, 2020 - mdpi.com
Prostate cancer (PCa) is the most frequently diagnosed cancer in men, causing
considerable morbidity and mortality. The P2X4 receptor (P2X4R) is the most ubiquitously …