Ligand identification for G-protein-coupled receptors: a lead generation perspective
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作者:
Bleicher, KH
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F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, SwitzerlandF Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, Switzerland
Bleicher, KH
[1
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Green, LG
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F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, SwitzerlandF Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, Switzerland
Green, LG
[1
]
Martin, RE
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F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, SwitzerlandF Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, Switzerland
Martin, RE
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Rogers-Evans, M
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F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, SwitzerlandF Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, Switzerland
Rogers-Evans, M
[1
]
机构:
[1] F Hoffmann La Roche & Co Ltd, Div Pharmaceut, Lead Generat, PRBDCI, CH-4070 Basel, Switzerland
This review addresses strategies for the generation of ligands for G-protein-coupled receptors outside classical high-throughput screening and literature based approaches. These range from the chemical intuition-based strategies of endogenous ligand elaboration and privileged structure decoration to the in silico approaches of virtual screening and de novo design. Examples are cited where supporting pharmacological data has been presented.