An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs

G protein-coupled receptors (GPCRs) represent 50–60% of the current drug targets. There is no doubt that this family of membrane proteins plays a crucial role in drug discovery today. Classically, a number of drugs based on GPCRs have been developed for such different indications as cardiovascular,...

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Autor principal: Lundstrom, Kenneth
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2009
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7122359/
https://www.ncbi.nlm.nih.gov/pubmed/19513641
http://dx.doi.org/10.1007/978-1-60327-317-6_4
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author Lundstrom, Kenneth
author_facet Lundstrom, Kenneth
author_sort Lundstrom, Kenneth
collection PubMed
description G protein-coupled receptors (GPCRs) represent 50–60% of the current drug targets. There is no doubt that this family of membrane proteins plays a crucial role in drug discovery today. Classically, a number of drugs based on GPCRs have been developed for such different indications as cardiovascular, metabolic, neurodegenerative, psychiatric, and oncologic diseases. Owing to the restricted structural information on GPCRs, only limited exploration of structure-based drug design has been possible. Much effort has been dedicated to structural biology on GPCRs and very recently an X-ray structure of the β2-adrenergic receptor was obtained. This breakthrough will certainly increase the efforts in structural biology on GPCRs and furthermore speed up and facilitate the drug discovery process.
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spelling pubmed-71223592020-04-06 An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs Lundstrom, Kenneth G Protein-Coupled Receptors in Drug Discovery Article G protein-coupled receptors (GPCRs) represent 50–60% of the current drug targets. There is no doubt that this family of membrane proteins plays a crucial role in drug discovery today. Classically, a number of drugs based on GPCRs have been developed for such different indications as cardiovascular, metabolic, neurodegenerative, psychiatric, and oncologic diseases. Owing to the restricted structural information on GPCRs, only limited exploration of structure-based drug design has been possible. Much effort has been dedicated to structural biology on GPCRs and very recently an X-ray structure of the β2-adrenergic receptor was obtained. This breakthrough will certainly increase the efforts in structural biology on GPCRs and furthermore speed up and facilitate the drug discovery process. 2009-04-14 /pmc/articles/PMC7122359/ /pubmed/19513641 http://dx.doi.org/10.1007/978-1-60327-317-6_4 Text en © Humana Press, a part of Springer Science+Business Media, LLC 2009 This article is made available via the PMC Open Access Subset for unrestricted research re-use and secondary analysis in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic.
spellingShingle Article
Lundstrom, Kenneth
An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
title An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
title_full An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
title_fullStr An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
title_full_unstemmed An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
title_short An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs
title_sort overview on gpcrs and drug discovery: structure-based drug design and structural biology on gpcrs
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7122359/
https://www.ncbi.nlm.nih.gov/pubmed/19513641
http://dx.doi.org/10.1007/978-1-60327-317-6_4
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