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EnglishMany 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.
| Titolo: | A 2a adenosine receptor: Structures, modeling, and medicinal chemistry | |
| Autori: | BARALDI, Stefania (Primo) BARALDI, Pier Giovanni (Secondo) CIANCETTA, Antonella (Penultimo) | |
| Data di pubblicazione: | 2018 | |
| Serie: | ||
| Handle: | http://hdl.handle.net/11392/2420280 | |
| ISBN: | 978-3-319-90807-6 978-3-319-90808-3 | |
| Appare nelle tipologie: | 02.1 Contributo in volume (Capitolo, articolo) |
File in questo prodotto:
| File | Descrizione | Tipologia | Licenza | |
|---|---|---|---|---|
| BaraldiStefania2018_Chapter_A2AAdenosineReceptorStructures.pdf | Full text editoriale | Full text (versione editoriale) | NON PUBBLICO - Accesso privato/ristretto | Administrator Richiedi una copia |
| 2018_Bookmatter_TheAdenosineReceptors.pdf | Frontespizio, indice del volume | Altro materiale allegato | PUBBLICO - Pubblico con Copyright | Open Access Visualizza/Apri |
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