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• W2085381168 endingPage "259" @default.
• W2085381168 startingPage "249" @default.
• W2085381168 abstract "The past couple of years have seen several novel X-ray structures of 7 transmembrane (7TM) receptors in complex with antagonists and even with a peptide fragment of a G protein. These structures demonstrate that the main ligand-binding pocket in 7TM receptors is like a funnel with a partial ‘lid’ in which extracellular loop 2b, in particular, functions as a gating element. Small-molecule antagonists and inverse agonists bind in very different modes: some very deeply and others more superficially, even reaching out above the transmembranes. Several highly conserved residues seem to function as micro-switches of which ArgIII:26 (Arg3.50) in its active conformation interacts directly with the G protein. These micro-switches together with a hydrogen-bond network between conserved polar residues and structural water molecules are proposed to constitute an extended allosteric interface between the domains (i.e. especially TM-VI), which performs the large, global toggle switch movements connecting ligand binding with intracellular signaling. The past couple of years have seen several novel X-ray structures of 7 transmembrane (7TM) receptors in complex with antagonists and even with a peptide fragment of a G protein. These structures demonstrate that the main ligand-binding pocket in 7TM receptors is like a funnel with a partial ‘lid’ in which extracellular loop 2b, in particular, functions as a gating element. Small-molecule antagonists and inverse agonists bind in very different modes: some very deeply and others more superficially, even reaching out above the transmembranes. Several highly conserved residues seem to function as micro-switches of which ArgIII:26 (Arg3.50) in its active conformation interacts directly with the G protein. These micro-switches together with a hydrogen-bond network between conserved polar residues and structural water molecules are proposed to constitute an extended allosteric interface between the domains (i.e. especially TM-VI), which performs the large, global toggle switch movements connecting ligand binding with intracellular signaling." @default.
• W2085381168 created "2016-06-24" @default.
• W2085381168 creator A5005007970 @default.
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• W2085381168 creator A5083291362 @default.
• W2085381168 date "2009-05-01" @default.
• W2085381168 modified "2023-10-16" @default.
• W2085381168 title "Ligand binding and micro-switches in 7TM receptor structures" @default.
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• W2085381168 doi "https://doi.org/10.1016/j.tips.2009.02.006" @default.
• W2085381168 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19375807" @default.
• W2085381168 hasPublicationYear "2009" @default.
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