Adenosine as a multi-signalling guardian angel in human diseases: when, where and how does it exert its protective effects?

PA Borea, S Gessi, S Merighi, K Varani - Trends in pharmacological …, 2016 - cell.com
The importance of adenosine for human health cannot be overstated. Indeed, this ubiquitous
nucleoside is an integral component of ATP, and regulates the function of every tissue and …

Historical and current adenosine receptor agonists in preclinical and clinical development

KA Jacobson, DK Tosh, S Jain, ZG Gao - Frontiers in cellular …, 2019 - frontiersin.org
Adenosine receptors (ARs) function in the body's response to conditions of pathology and
stress associated with a functional imbalance, such as in the supply and demand of …

Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia

CJ Draper-Joyce, R Bhola, J Wang, A Bhattarai… - Nature, 2021 - nature.com
The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …

Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief

DD Jensen, TM Lieu, ML Halls, NA Veldhuis… - Science Translational …, 2017 - science.org
Typically considered to be cell surface sensors of extracellular signals, heterotrimeric GTP-
binding protein (G protein)–coupled receptors (GPCRs) control many pathophysiological …

A pH-responsive nanoparticle targets the neurokinin 1 receptor in endosomes to prevent chronic pain

PD Ramírez-García, JS Retamal, P Shenoy… - Nature …, 2019 - nature.com
Nanoparticle-mediated drug delivery is especially useful for targets within endosomes
because of the endosomal transport mechanisms of many nanomedicines within cells. Here …

Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission

RE Yarwood, WL Imlach, TM Lieu… - Proceedings of the …, 2017 - National Acad Sciences
G protein-coupled receptors (GPCRs) are considered to function primarily at the plasma
membrane, where they interact with extracellular ligands and couple to G proteins that …

Pharmacological characterisation of the highly NaV1.7 selective spider venom peptide Pn3a

JR Deuis, Z Dekan, JS Wingerd, JJ Smith… - Scientific reports, 2017 - nature.com
Human genetic studies have implicated the voltage-gated sodium channel NaV1. 7 as a
therapeutic target for the treatment of pain. A novel peptide, μ-theraphotoxin-Pn3a, isolated …

Treatment of chronic neuropathic pain: purine receptor modulation

KA Jacobson, LA Giancotti, F Lauro, F Mufti… - Pain, 2020 - journals.lww.com
Extracellular nucleosides and nucleotides have widespread functions in responding to
physiological stress. The “purinome” encompasses 4 G-protein-coupled receptors (GPCRs) …

[HTML][HTML] Adenosine receptors: Emerging non-opioids targets for pain medications

SM Jung, L Peyton, H Essa, DS Choi - Neurobiology of Pain, 2022 - Elsevier
Physical and emotional pain deteriorates the quality of well-being. Also, numerous non-
invasive and invasive treatments for diagnosed diseases such as cancer medications and …

Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor

Y Miao, A Bhattarai, ATN Nguyen, A Christopoulos… - Scientific reports, 2018 - nature.com
Despite intense interest in designing positive allosteric modulators (PAMs) as selective
drugs of the adenosine A1 receptor (A1AR), structural binding modes of the receptor PAMs …