Sandbox Reserved 1646

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Current revision (10:50, 19 January 2022) (edit) (undo)
(CHANGED A SOURCE FOR A BETTER ONE (more relevant))
 
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Following structural highlights are different to receptors of this family: The well-known conserved D-R-Y motif is in fact the <scene name='86/868179/D-r-s_motif/2'>D138-R139-S140</scene> motif in GnRH1R. An intrahelical [https://en.wikipedia.org/wiki/Salt_bridge_(protein_and_supramolecular salt bridge] is observed between D138 and R139, as well as a polar interaction between R139 and T265 (This interaction restricts the outward movement of those TMs associated with GPCR activation). The <scene name='86/868179/N-terminus/6'>N-terminal region</scene> (aa 18–33) before TM1 is well folded and appears inserted into the orthostatic binding cavity.
Following structural highlights are different to receptors of this family: The well-known conserved D-R-Y motif is in fact the <scene name='86/868179/D-r-s_motif/2'>D138-R139-S140</scene> motif in GnRH1R. An intrahelical [https://en.wikipedia.org/wiki/Salt_bridge_(protein_and_supramolecular salt bridge] is observed between D138 and R139, as well as a polar interaction between R139 and T265 (This interaction restricts the outward movement of those TMs associated with GPCR activation). The <scene name='86/868179/N-terminus/6'>N-terminal region</scene> (aa 18–33) before TM1 is well folded and appears inserted into the orthostatic binding cavity.
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This structure belongs to the numerous structures of GPCR currently published. The G-protein-coupled receptor (GPCR) superfamily comprises an estimated 600–1,000 members and is the largest known class of molecular targets with proven therapeutic value. They play an incredible role in a range of functions in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third and one-half of the marketed drugs act by binding to GPCRs.<ref>DOI: 10.1146/annurev-pharmtox-032112-135923</ref>
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This structure belongs to the numerous structures of GPCR currently published. The G-protein-coupled receptor (GPCR) superfamily comprises an estimated 600–1,000 members and is the largest known class of molecular targets with proven therapeutic value. They play an incredible role in a range of functions in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third and one-half of the marketed drugs act by binding to GPCRs.<ref>DOI:10.1186/1471-2105-9-363</ref>

Current revision

This Sandbox is Reserved from 26/11/2020, through 26/11/2021 for use in the course "Structural Biology" taught by Bruno Kieffer at the University of Strasbourg, ESBS. This reservation includes Sandbox Reserved 1643 through Sandbox Reserved 1664.
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Gonadotropin releasing hormone 1 receptor (GnRHR)

PDB ID 7BR3

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