Kinetic scaffolding mediated by a phospholipase C-beta and Gq signaling complex

TitleKinetic scaffolding mediated by a phospholipase C-beta and Gq signaling complex
Publication TypeJournal Article
Year of Publication2010
AuthorsWaldo GL, Ricks TK, Hicks SN, Cheever ML, Kawano T, Tsuboi K, Wang X, Montell C, Kozasa T, Sondek J, T Harden K
JournalScience
Volume330
Pagination974-80
Date Published11/2010
ISSN1095-9203
KeywordsAmino Acid Sequence, Animals, Catalytic Domain, Crystallography, X-Ray, Enzyme Activation, GTP-Binding Protein alpha Subunits, Gq-G11, Guanosine Triphosphate, Humans, Hydrogen Bonding, Hydrolysis, Isoenzymes, Kinetics, Mice, Models, Molecular, Molecular Sequence Data, Mutagenesis, Phospholipase C beta, Protein Binding, Protein Structure, Tertiary, Recombinant Fusion Proteins, Signal Transduction
Abstract

Transmembrane signals initiated by a broad range of extracellular stimuli converge on nodes that regulate phospholipase C (PLC)-dependent inositol lipid hydrolysis for signal propagation. We describe how heterotrimeric guanine nucleotide-binding proteins (G proteins) activate PLC-βs and in turn are deactivated by these downstream effectors. The 2.7-angstrom structure of PLC-β3 bound to activated Gα(q) reveals a conserved module found within PLC-βs and other effectors optimized for rapid engagement of activated G proteins. The active site of PLC-β3 in the complex is occluded by an intramolecular plug that is likely removed upon G protein-dependent anchoring and orientation of the lipase at membrane surfaces. A second domain of PLC-β3 subsequently accelerates guanosine triphosphate hydrolysis by Gα(q), causing the complex to dissociate and terminate signal propagation. Mutations within this domain dramatically delay signal termination in vitro and in vivo. Consequently, this work suggests a dynamic catch-and-release mechanism used to sharpen spatiotemporal signals mediated by diverse sensory inputs.

DOI10.1126/science.1193438
Alternate JournalScience
PubMed ID20966218
PubMed Central IDPMC3046049
Grant ListEY010852 / EY / NEI NIH HHS / United States
GM074001 / GM / NIGMS NIH HHS / United States
GM38213 / GM / NIGMS NIH HHS / United States
GM57391 / GM / NIGMS NIH HHS / United States
GM61454 / GM / NIGMS NIH HHS / United States
R01 GM057391-13 / GM / NIGMS NIH HHS / United States
R01 GM062299 / GM / NIGMS NIH HHS / United States
R01 GM062299-08 / GM / NIGMS NIH HHS / United States