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Registro Completo |
Biblioteca(s): |
Ebooks. |
Data corrente: |
01/02/2013 |
Data da última atualização: |
01/02/2013 |
Autoria: |
NEVE, K. A. |
Afiliação: |
Kim A. Neve. |
Título: |
Functional Selectivity of G Protein-Coupled Receptor Ligands: New Opportunities for Drug Discovery. |
Ano de publicação: |
2009 |
Fonte/Imprenta: |
Springer eBooks. |
Descrição Física: |
digital. |
Série: |
The Receptors |
ISBN: |
9781603273350 |
DOI: |
10.1007/978-1-60327-335-0 |
Idioma: |
Inglês |
Conteúdo: |
Historical Overview of the Concept of Functional Selectivity -- Functional Selectivity: Theoretical Considerations and Future Directions -- Agonist Selective Coupling of G Protein-Coupled Receptors -- Ligand-Selective Receptor Desensitization and Endocytosis -- Selectivity for G protein or Arrestin-Mediated Signaling -- In Vivo Evidence for and Consequences of Functional Selectivity -- Functional Selectivity at Adrenergic Receptors -- Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity -- Functional Selectivity at Serotonin Receptors -- Functional Selectivity at Dopamine Receptors -- Functional Selectivity at Receptors for Cannabinoids and other Lipids -- Functional Selectivity at Opioid Receptors -- Functional Selectivity at non-Opioid Peptide Receptors .Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function. MenosHistorical Overview of the Concept of Functional Selectivity -- Functional Selectivity: Theoretical Considerations and Future Directions -- Agonist Selective Coupling of G Protein-Coupled Receptors -- Ligand-Selective Receptor Desensitization and Endocytosis -- Selectivity for G protein or Arrestin-Mediated Signaling -- In Vivo Evidence for and Consequences of Functional Selectivity -- Functional Selectivity at Adrenergic Receptors -- Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity -- Functional Selectivity at Serotonin Receptors -- Functional Selectivity at Dopamine Receptors -- Functional Selectivity at Receptors for Cannabinoids and other Lipids -- Functional Selectivity at Opioid Receptors -- Functional Selectivity at non-Opioid Peptide Receptors .Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within... Mostrar Tudo |
Palavras-Chave: |
Biomedicine; Neurobiology; Neurology; Neurosciences; Pharmacology/Toxicology. |
Thesaurus Nal: |
human physiology; medicine; toxicology. |
Categoria do assunto: |
-- |
URL: |
https://dx.doi.org/10.1007/978-1-60327-335-0
|
Marc: |
LEADER 02889nam a2200253 a 4500 001 1947408 005 2013-02-01 008 2009 bl uuuu 00u1 u #d 020 $a9781603273350 024 7 $a10.1007/978-1-60327-335-0$2DOI 100 1 $aNEVE, K. A. 245 $aFunctional Selectivity of G Protein-Coupled Receptor Ligands$bNew Opportunities for Drug Discovery.$h[electronic resource] 260 $aSpringer eBooks.$c2009 300 $cdigital. 490 $aThe Receptors 520 $a<P>Historical Overview of the Concept of Functional Selectivity -- Functional Selectivity: Theoretical Considerations and Future Directions -- Agonist Selective Coupling of G Protein-Coupled Receptors -- Ligand-Selective Receptor Desensitization and Endocytosis -- Selectivity for G protein or Arrestin-Mediated Signaling -- In Vivo Evidence for and Consequences of Functional Selectivity -- Functional Selectivity at Adrenergic Receptors -- Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity -- Functional Selectivity at Serotonin Receptors -- Functional Selectivity at Dopamine Receptors -- Functional Selectivity at Receptors for Cannabinoids and other Lipids -- Functional Selectivity at Opioid Receptors -- Functional Selectivity at non-Opioid Peptide Receptors</P>.<P>Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function. </P> 650 $ahuman physiology 650 $amedicine 650 $atoxicology 653 $aBiomedicine 653 $aNeurobiology 653 $aNeurology 653 $aNeurosciences 653 $aPharmacology/Toxicology
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