Global ETD Search
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Showing 1 to 5 of 5 for “"GPCR pharmacology"”.
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Computational and experimental investigation of G protein-coupled receptor signalling mechanisms
G Protein-Coupled Receptors (GPCRs) are 7-transmembrane domain proteins. These receptors translate extracellular stimuli into cellular responses through heterotrimeric G proteins and β-arrestin proteins. These receptors are of considerable therapeutic interest, targeted by over 500 drugs approved …
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Influence of Peptide Allosteric Modulators on Agonist Bias at Class B1 G Protein-Coupled Receptors
Class B1 G Protein-Coupled Receptors (GPCRs) are a small family within the GPCR superfamily. However, they are implicated in the pathologies of some of the most prevalent diseases, such as type 2 diabetes and heart disease. Despite being such a small family, their signalling is very diverse; each …
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Multiplexed Mapping of the Interactome of G Protein-Coupled Receptors and Receptor Activity-Modifying Proteins
… of many aspects of G protein-coupled receptor (GPCR) biology and pharmacology. The RAMP family was discovered more than two decades ago and GPCR-RAMP interactions and their functional consequences on receptor trafficking and ligand selectivity have been documented for several GPCRs, mostly …
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Drug discovery at class A and class B GPCRs
G protein-coupled receptors (GPCRs) are a big family of membrane receptors encoded by more than 800 genes in humans. The vast number and diversity of GPCRs enables them to interact with an equally great number of ligands enabling them to regulate many physiological functions such as senses, …
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Investigating small-molecule inhibitors of platelet aggregation
… is mediated by the Gi-protein-coupled receptor (GPCR), P2Y12. Therefore, P2Y12 antagonists are clinically used to prevent thrombotic events. However, current antiplatelet drugs have several drawbacks such as the increased risk of bleeding, difficulty in fine-tuning the antiplatelet effects of …