2hlb
From Proteopedia
(New page: 200px<br /> <applet load="2hlb" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hlb, resolution 2.2Å" /> '''A Structural Basis f...) |
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| - | [[Image:2hlb.gif|left|200px]]<br /> | + | [[Image:2hlb.gif|left|200px]]<br /><applet load="2hlb" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2hlb" size=" | + | |
caption="2hlb, resolution 2.2Å" /> | caption="2hlb, resolution 2.2Å" /> | ||
'''A Structural Basis for Nucleotide Exchange on G-alpha-i Subunits and Receptor Coupling Specificity'''<br /> | '''A Structural Basis for Nucleotide Exchange on G-alpha-i Subunits and Receptor Coupling Specificity'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Heterotrimeric G proteins are molecular switches that relay information | + | Heterotrimeric G proteins are molecular switches that relay information intracellularly in response to various extracellular signals. How ligand-activated G protein-coupled receptors act at a distance to exert exchange activity on the Galpha nucleotide binding pocket is poorly understood. Here we describe the synergistic action of two peptides: one from the third intracellular loop of the D2 dopamine receptor (D2N), and a second, Galpha.GDP-binding peptide (KB-752) that mimics the proposed role of Gbetagamma in receptor-promoted nucleotide exchange. The structure of both peptides in complex with Galpha(i1) suggests that conformational changes in the beta3/alpha2 loop and beta6 strand act in concert for efficient nucleotide exchange. Two key residues in the alpha4 helix were found to define a receptor/Galpha(i) coupling specificity determinant. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2HLB is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and GDP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 2HLB is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=GDP:'>GDP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HLB OCA]. |
==Reference== | ==Reference== | ||
| - | Structural basis for nucleotide exchange on | + | Structural basis for nucleotide exchange on G alpha i subunits and receptor coupling specificity., Johnston CA, Siderovski DP, Proc Natl Acad Sci U S A. 2007 Feb 6;104(6):2001-6. Epub 2007 Jan 30. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17264214 17264214] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Johnston, C | + | [[Category: Johnston, C A.]] |
| - | [[Category: Siderovski, D | + | [[Category: Siderovski, D P.]] |
| - | [[Category: Watts, V | + | [[Category: Watts, V J.]] |
[[Category: GDP]] | [[Category: GDP]] | ||
[[Category: SO4]] | [[Category: SO4]] | ||
[[Category: protein:peptide complex]] | [[Category: protein:peptide complex]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:43:08 2008'' |
Revision as of 15:43, 21 February 2008
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A Structural Basis for Nucleotide Exchange on G-alpha-i Subunits and Receptor Coupling Specificity
Contents |
Overview
Heterotrimeric G proteins are molecular switches that relay information intracellularly in response to various extracellular signals. How ligand-activated G protein-coupled receptors act at a distance to exert exchange activity on the Galpha nucleotide binding pocket is poorly understood. Here we describe the synergistic action of two peptides: one from the third intracellular loop of the D2 dopamine receptor (D2N), and a second, Galpha.GDP-binding peptide (KB-752) that mimics the proposed role of Gbetagamma in receptor-promoted nucleotide exchange. The structure of both peptides in complex with Galpha(i1) suggests that conformational changes in the beta3/alpha2 loop and beta6 strand act in concert for efficient nucleotide exchange. Two key residues in the alpha4 helix were found to define a receptor/Galpha(i) coupling specificity determinant.
Disease
Known disease associated with this structure: Dystonia, myoclonic OMIM:[126450]
About this Structure
2HLB is a Protein complex structure of sequences from Homo sapiens with and as ligands. Full crystallographic information is available from OCA.
Reference
Structural basis for nucleotide exchange on G alpha i subunits and receptor coupling specificity., Johnston CA, Siderovski DP, Proc Natl Acad Sci U S A. 2007 Feb 6;104(6):2001-6. Epub 2007 Jan 30. PMID:17264214
Page seeded by OCA on Thu Feb 21 17:43:08 2008
