2pzx
From Proteopedia
(New page: 200px<br /><applet load="2pzx" size="450" color="white" frame="true" align="right" spinBox="true" caption="2pzx, resolution 3.50Å" /> '''Structure of the met...) |
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| - | [[Image:2pzx.jpg|left|200px]]<br /><applet load="2pzx" size=" | + | [[Image:2pzx.jpg|left|200px]]<br /><applet load="2pzx" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2pzx, resolution 3.50Å" /> | caption="2pzx, resolution 3.50Å" /> | ||
'''Structure of the methuselah ectodomain with peptide inhibitor'''<br /> | '''Structure of the methuselah ectodomain with peptide inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2PZX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Drosophila_melanogaster Drosophila melanogaster]. Full crystallographic information is available from [http:// | + | 2PZX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Drosophila_melanogaster Drosophila melanogaster]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2PZX OCA]. |
==Reference== | ==Reference== | ||
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[[Category: signaling protein]] | [[Category: signaling protein]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:52:31 2008'' |
Revision as of 11:52, 23 January 2008
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Structure of the methuselah ectodomain with peptide inhibitor
Overview
G protein-coupled receptors (GPCRs) mediate signaling from extracellular, ligands to intracellular signal transduction proteins. Methuselah (Mth) is, a class B (secretin-like) GPCR, a family typified by their large, ligand-binding, N-terminal extracellular domains. Downregulation of mth, increases the life span of Drosophila melanogaster; inhibitors of Mth, signaling should therefore enhance longevity. We used mRNA display, selection to identify high-affinity (K(d) = 15 to 30 nM) peptide ligands, that bind to the N-terminal ectodomain of Mth. The selected peptides are, potent antagonists of Mth signaling, and structural studies suggest that, they perturb the interface between the Mth ecto- and transmembrane, domains. Flies constitutively expressing a Mth antagonist peptide have a, robust life span extension, which suggests that the peptides inhibit Mth, signaling in vivo. Our work thus provides new life span-extending ligands, for a metazoan and a general approach for the design of modulators of this, important class of GPCRs.
About this Structure
2PZX is a Single protein structure of sequence from Drosophila melanogaster. Full crystallographic information is available from OCA.
Reference
Extension of Drosophila melanogaster life span with a GPCR peptide inhibitor., Ja WW, West AP Jr, Delker SL, Bjorkman PJ, Benzer S, Roberts RW, Nat Chem Biol. 2007 Jul;3(7):415-9. Epub 2007 Jun 3. PMID:17546039
Page seeded by OCA on Wed Jan 23 13:52:31 2008
