Many selective agonists and antagonists of the A 2A adenosine receptor (AR) have been reported, while allosteric modulators specific for this receptor are still needed. Many heterocyclic chemotypes have been discovered as A 2A AR antagonists, while most of the known AR agonists are nucleosides or 3,5-dicyanopyridine derivatives. A few A 2A AR ligands have been in clinical trials as antihypertensives, anti-inflammatory or diagnostic compounds (agonists), and as drugs for treating Parkinson’s disease and cancer (antagonists). The A 2A AR has become one of the most widely investigated G protein-coupled receptor (GPCR) structures using X-ray crystallography and also biophysical techniques such as NMR. Thus, the design of agonists, antagonists, and allosteric modulators has become structure-based, with numerous examples of in silico approaches, including virtual ligand screening (VLS), leading to the discovery of both novel agonists and antagonists.

A 2a adenosine receptor: Structures, modeling, and medicinal chemistry

Baraldi S.
Primo
;
Baraldi P. G.
Secondo
;
Oliva P.;Ciancetta A.
Penultimo
;
2018

Abstract

Many selective agonists and antagonists of the A 2A adenosine receptor (AR) have been reported, while allosteric modulators specific for this receptor are still needed. Many heterocyclic chemotypes have been discovered as A 2A AR antagonists, while most of the known AR agonists are nucleosides or 3,5-dicyanopyridine derivatives. A few A 2A AR ligands have been in clinical trials as antihypertensives, anti-inflammatory or diagnostic compounds (agonists), and as drugs for treating Parkinson’s disease and cancer (antagonists). The A 2A AR has become one of the most widely investigated G protein-coupled receptor (GPCR) structures using X-ray crystallography and also biophysical techniques such as NMR. Thus, the design of agonists, antagonists, and allosteric modulators has become structure-based, with numerous examples of in silico approaches, including virtual ligand screening (VLS), leading to the discovery of both novel agonists and antagonists.
978-3-319-90807-6
978-3-319-90808-3
A 2a adenosine receptors ; A 2a agonists ; A 2a allosteric modulators ; A 2a antagonists ; X-ray structures
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2420280
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