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1y3a

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1y3a, resolution 2.50Å ()
Ligands:
Gene: GNAI1 (Homo sapiens)
Domains: G-alpha, G-alpha
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Structure of G-Alpha-I1 bound to a GDP-selective peptide provides insight into guanine nucleotide exchange

Publication Abstract from PubMed

Heterotrimeric G proteins are molecular switches that regulate numerous signaling pathways involved in cellular physiology. This characteristic is achieved by the adoption of two principal states: an inactive, GDP bound state and an active, GTP bound state. Under basal conditions, G proteins exist in the inactive, GDP bound state; thus, nucleotide exchange is crucial to the onset of signaling. Despite our understanding of G protein signaling pathways, the mechanism of nucleotide exchange remains elusive. We employed phage display technology to identify nucleotide state-dependent Galpha binding peptides. Herein, we report a GDP-selective Galpha binding peptide, KB-752, that enhances spontaneous nucleotide exchange of Galpha(i) subunits. Structural determination of the Galpha(i1)/peptide complex reveals unique changes in the Galpha switch regions predicted to enhance nucleotide exchange by creating a GDP dissociation route. Our results cast light onto a potential mechanism by which Galpha subunits adopt a conformation suitable for nucleotide exchange.

Structure of Galpha(i1) bound to a GDP-selective peptide provides insight into guanine nucleotide exchange., Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP, Structure. 2005 Jul;13(7):1069-80. PMID:16004878

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

1Y3A is a 8 chains structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP. Structure of Galpha(i1) bound to a GDP-selective peptide provides insight into guanine nucleotide exchange. Structure. 2005 Jul;13(7):1069-80. PMID:16004878 doi:10.1016/j.str.2005.04.007

Page seeded by OCA on Mon Feb 16 13:31:55 2009

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