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Literature summary for 3.6.5.1 extracted from

  • Sprang, S.R.
    G Protein mechanism: insights from structural analysis (1997), Annu. Rev. Biochem., 66, 639-678.
    View publication on PubMed
Search for more literature for 3.6.5.1

Activating Compound

Activating Compound Comment Organism Structure
cell-surface receptors of the seven-transmembrane-helix class, activated by catalyzing the exchange of GDP for GTP in the guanine nucleotide-binding site of the alpha-subunit Mammalia

Inhibitors

Inhibitors Comment Organism Structure
betagamma subunit of the hetreotrimeric G protein inhibits by selectively binding to and stabilization of the GDP-bound state Mammalia
pertussis toxin pertussis toxin-catalysed ADP-ribosylation prevents functional contacts between G-protein-coupled receptors and the Gi-like G-proteins Mammalia

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GTP + H2O Mammalia Galpha subunits can regulate intracellular effectors, such as adenylyl cyclase, phospholipase Cbeta, K+ and Ca+ channels, and cyclic GMP phosphodiesterase GDP + phosphate
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Organism

Organism UniProt Comment Textmining
Mammalia
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Posttranslational Modification

Posttranslational Modification Comment Organism
lipoprotein most Galpha subunits, excluding alphat, are S-palmitoylated at one or more Cys near the amino terminus, others, alphao, alphaz, alphai and alphat are N-myristoylated at Gly2 as well. Lipid modifications help bind alpha subunits to the plasma membrane, juxtaposing them to their cognate receptors and effector targets Mammalia

Reaction

Reaction Comment Organism Reaction ID
GTP + H2O = GDP + phosphate binding and hydrolysis of GTP triggers reciprocal conformational changes within a switch region within the catalytic domain Mammalia
a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + H2O
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 Mammalia GDP + phosphate
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 ?
GTP + H2O Galpha subunits can regulate intracellular effectors, such as adenylyl cyclase, phospholipase Cbeta, K+ and Ca+ channels, and cyclic GMP phosphodiesterase Mammalia GDP + phosphate
-
 ?