1, 2, 3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

K Bozorov, J Zhao, HA Aisa - Bioorganic & medicinal chemistry, 2019 - Elsevier
Abstract The 1, 2, 3-triazole ring is a major pharmacophore system among nitrogen-
containing heterocycles. These five-membered heterocyclic motifs with three nitrogen …

The P2X7 receptor: central hub of brain diseases

R Andrejew, Á Oliveira-Giacomelli… - Frontiers in Molecular …, 2020 - frontiersin.org
The P2X7 receptor is a cation channel activated by high concentrations of adenosine
triphosphate (ATP). Upon long-term activation, it complexes with membrane proteins forming …

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 …

Characterization of the central nervous system penetrant and selective purine P2X7 receptor antagonist JNJ-54175446 in patients with major depressive disorder

K Recourt, P de Boer, P van der Ark, H Benes… - Translational …, 2023 - nature.com
JNJ-54175446 is a selective purine P2X7 receptor (P2X7R) antagonist that attenuates
microglial IL-1β/IL-18 release. In healthy volunteers, JNJ-54175446 suppressed peripheral …

Where do recent small molecule clinical development candidates come from?

DG Brown, J Boström - Journal of medicinal chemistry, 2018 - ACS Publications
An analysis of 66 published clinical candidates from Journal of Medicinal Chemistry has
been conducted to shed light on which lead generation strategies are most frequently …

Emerging role of the P2X7-NLRP3-IL1β pathway in mood disorders

A Bhattacharya, DNC Jones - Psychoneuroendocrinology, 2018 - Elsevier
The science of neuroimmunopsychiatry has evolved rapidly in the last few years with the
hope of tackling the unmet need in mood disorders. This article focuses on an inflammatory …

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 …

Recent advances in CNS P2X7 physiology and pharmacology: focus on neuropsychiatric disorders

A Bhattacharya - Frontiers in Pharmacology, 2018 - frontiersin.org
The ATP-gated P2X7 ion channel is an abundant microglial protein in the CNS that plays an
important pathological role in executing ATP-driven danger signal transduction. Emerging …

P2X7 receptor: an emerging target in Alzheimer's disease

Q Huang, J Ying, W Yu, Y Dong, H Xiong… - Molecular …, 2024 - Springer
Alzheimer's disease (AD) is a major cause of age-related dementia, which is becoming a
global health crisis. However, the pathogenesis and etiology of AD are still not fully …

Antagonism of the ATP-gated P2X7 receptor: a potential therapeutic strategy for cancer

M Drill, NC Jones, M Hunn, TJ O'Brien, M Monif - Purinergic signalling, 2021 - Springer
Abstract The P2X receptor 7 (P2X7R) is a plasma membrane receptor sensing extracellular
ATP associated with a wide variety of cellular functions. It is most commonly expressed on …