Adenosine receptors and the central nervous system

AM Sebastiao, JA Ribeiro - Adenosine receptors in health and disease, 2009 - Springer
The adenosine receptors (ARs) in the nervous system act as a kind of “go-between” to
regulate the release of neurotransmitters (this includes all known neurotransmitters) and the …

Structure-Based Discovery of A2A Adenosine Receptor Ligands

J Carlsson, L Yoo, ZG Gao, JJ Irwin… - Journal of medicinal …, 2010 - ACS Publications
The recent determination of X-ray structures of pharmacologically relevant GPCRs has
made these targets accessible to structure-based ligand discovery. Here we explore …

[HTML][HTML] Structure of the adenosine A1 receptor reveals the basis for subtype selectivity

A Glukhova, DM Thal, AT Nguyen, EA Vecchio, M Jörg… - Cell, 2017 - cell.com
The adenosine A 1 receptor (A 1-AR) is a G-protein-coupled receptor that plays a vital role in
cardiac, renal, and neuronal processes but remains poorly targeted by current drugs. We …

The adenosine metabolite inosine is a functional agonist of the adenosine A2A receptor with a unique signaling bias

AA Welihinda, M Kaur, K Greene, Y Zhai, EP Amento - Cellular signalling, 2016 - Elsevier
Inosine is an endogenous purine nucleoside that is produced by catabolism of adenosine.
Adenosine has a short half-life (approximately 10 s) and is rapidly deaminated to inosine, a …

Adenosine and inflammation: what's new on the horizon?

L Antonioli, B Csóka, M Fornai, R Colucci, E Kokai… - Drug Discovery …, 2014 - Elsevier
Highlights•Adenosine contributes to tissue integrity by modulating the immune
system.•Adenosine receptor ligands emerged for the management of inflammation.•These …

Adenosine receptors and inflammation

MR Blackburn, CO Vance, E Morschl… - Adenosine receptors in …, 2009 - Springer
Extracellular adenosine is produced in a coordinated manner from cells following cellular
challenge or tissue injury. Once produced, it serves as an autocrine-and paracrine-signaling …

Adenosine receptors in the nervous system: pathophysiological implications

JA Ribeiro, AM Sebastiao, A De Mendonça - Progress in neurobiology, 2002 - Elsevier
Adenosine is a ubiquitous homeostatic substance released from most cells, including
neurones and glia. Once in the extracellular space, adenosine modifies cell functioning by …

New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A2B Receptor with an Improved Selectivity Profile Compared to the Reference Agonist N …

MW Beukers, LCW Chang… - Journal of medicinal …, 2004 - ACS Publications
The adenosine A2B receptor is the least well characterized of the four known adenosine
receptor subtypes because of the absence of potent, selective agonists. Here, we present …

[HTML][HTML] Adenosine A2A receptor ligand recognition and signaling is blocked by A2B receptors

S Hinz, G Navarro, D Borroto-Escuela, BF Seibt… - Oncotarget, 2018 - ncbi.nlm.nih.gov
The adenosine receptor (AR) subtypes A 2A and A 2B are rhodopsin-like G s protein-
coupled receptors whose expression is highly regulated under pathological, eg hypoxic …

Targeting adenosine A2A receptor antagonism for treatment of cancer

M Congreve, GA Brown, A Borodovsky… - Expert opinion on drug …, 2018 - Taylor & Francis
ABSTRACT Introduction: Adenosine A2A Receptor (A2AR) antagonists are an emerging
class of agents that treat cancers, both as a monotherapy and in combination with other …