Inhibitors of NF-κB and P2X7/NLRP3/Caspase 1 pathway in microglia: Novel therapeutic opportunities in neuroinflammation induced early-stage Alzheimer's disease

BS Thawkar, G Kaur - Journal of neuroimmunology, 2019 - Elsevier
Microglial activation is a distinguished attribute in many neurodegenerative diseases of
aging. Compelling evidence suggests that neuroinflammation stimulated by microglia, the …

The P2X7 receptor channel: recent developments and the use of P2X7 antagonists in models of disease

R Bartlett, L Stokes, R Sluyter, DR Sibley - Pharmacological reviews, 2014 - Elsevier
The P2X7 receptor is a trimeric ATP-gated cation channel found predominantly, but not
exclusively, on immune cells. P2X7 activation results in a number of downstream events …

Medicinal chemistry of adenosine, P2Y and P2X receptors

KA Jacobson, CE Müller - Neuropharmacology, 2016 - Elsevier
Pharmacological tool compounds are now available to define action at the adenosine (ARs),
P2Y and P2X receptors. We present a selection of the most commonly used agents to study …

P2X7 in cancer: from molecular mechanisms to therapeutics

R Lara, E Adinolfi, CA Harwood, M Philpott… - Frontiers in …, 2020 - frontiersin.org
P2X7 is a transmembrane receptor expressed in multiple cell types including neurons,
dendritic cells, macrophages, monocytes, B and T cells where it can drive a wide range of …

Ion channels as therapeutic targets: a drug discovery perspective

SK Bagal, AD Brown, PJ Cox, K Omoto… - Journal of medicinal …, 2013 - ACS Publications
Ion channels are membrane proteins expressed in almost all living cells. The sequencing of
the human genome has identified more than 400 putative ion channels, but only a fraction of …

The microglial ATP‐gated ion channel P2X7 as a CNS drug target

A Bhattacharya, K Biber - Glia, 2016 - Wiley Online Library
Based on promising preclinical evidence, microglial P2X7 has increasingly being
recognized as a target for therapeutic intervention in neurological and psychiatric diseases …

Molecular and functional properties of P2X receptors—recent progress and persisting challenges

K Kaczmarek-Hájek, É Lörinczi, R Hausmann… - Purinergic …, 2012 - Springer
Abstract ATP-gated P2X receptors are trimeric ion channels that assemble as homo-or
heteromers from seven cloned subunits. Transcripts and/or proteins of P2X subunits have …

Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ‐47965567

A Bhattacharya, Q Wang, H Ao… - British journal of …, 2013 - Wiley Online Library
Background and Purpose An increasing body of evidence suggests that the purinergic
receptor P2X, ligand‐gated ion channel, 7 (P2X7) in the CNS may play a key role in …

Purinergic mechanisms and pain—an update

G Burnstock - European journal of pharmacology, 2013 - Elsevier
There is a brief summary of the background literature about purinergic signalling. The review
then considers purinergic mechanosensory transduction involved in visceral, cutaneous and …

The purinergic P2X7 receptor as a potential drug target to combat neuroinflammation in neurodegenerative diseases

F Calzaferri, C Ruiz‐Ruiz… - Medicinal research …, 2020 - Wiley Online Library
Neurodegenerative diseases (NDDs) represent a huge social burden, particularly in
Alzheimer's disease (AD) in which all proposed treatments investigated in murine models …