3pvu Summary

pdbe.org/3pvu
spacer

Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101)

The structure was published by Thal, D.M., Yeow, R.Y., Schoenau, C., Huber, J., and Tesmer, J.J., in 2011 in a paper entitled "Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors." (abstract).

This crystal structure was determined using X-ray diffraction at a resolution of 2.48 Å and deposited in 2010.

The experimental data on which the structure is based was also deposited.

This PDB entry contains a complex of 3 biomacromolecules, namely Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, and Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2.

It also contains one or more heterogenic compounds (e.g., ligands, co-factors, ions, modified amino acids, etc.); see here for a complete list.

The molecule most likely forms heterotrimers.

The following tables show cross-reference information to other databases (to obtain a list of all PDB entries sharing the same property or classification, click on the magnifying glass icon):


Chain Name UniProt Name of source organism % of UniProt sequence present in the sample Residues in the sample molecules % of residues observed
A Beta-adrenergic receptor kinase 1 P21146 (1-689) (ARBK1_BOVIN)search Bos taurussearch 97% 695 87%
B Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 P62871 (1-340) (GBB1_BOVIN)search Bos taurussearch 100% 340 99%
G Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 P63212 (1-68) (GBG2_BOVIN)search Bos taurussearch 94% 74 82%


This entry contains 3 unique UniProt proteins:

UniProt accession Name Organism PDB
P21146 (1 - 689) Beta-adrenergic receptor kinase 1 Bos taurus
P62871 (1 - 340) Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 Bos taurus
P63212 (1 - 68) Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 Bos taurus

Chain Structural classification (CATH) Sequence family (Pfam)
A (P21146) Regulator of G-protein Signalling 4, domain 2search, Phosphorylase Kinase; domain 1search, Transferase(Phosphotransferase) domain 1search, Pleckstrin-homology domain (PH domain)/Phosphotyrosine-binding domain (PTB)search PF00069: Protein kinase domainsearch, PF00169: PH domainsearch, PF00615: Regulator of G protein signaling domainsearch
B (P62871) YVTN repeat-like/Quinoprotein amine dehydrogenasesearch PF00400: WD domain, G-beta repeatsearch
G (P63212) PF00631: GGL domainsearch

Chain ID Biological process (GO) Molecular function (GO) Cellular component (GO)
A (P21146) protein phosphorylationsearch heart developmentsearch G-protein coupled receptor signaling pathwaysearch intracellular protein transportsearch regulation of the force of heart contractionsearch phosphorylationsearch peptidyl-serine phosphorylationsearch negative regulation of the force of heart contraction by chemical signalsearch termination of G-protein coupled receptor signaling pathwaysearch signal transductionsearch desensitization of G-protein coupled receptor protein signaling pathwaysearch negative regulation of striated muscle contractionsearch regulation of signal transductionsearch tachykinin receptor signaling pathwaysearch G-protein coupled receptor internalizationsearch cardiac muscle contractionsearch receptor internalizationsearch peptidyl-threonine phosphorylationsearch G-protein coupled acetylcholine receptor signaling pathwaysearch protein serine/threonine kinase activitysearch ATP bindingsearch protein kinase activitysearch G-protein coupled receptor kinase activitysearch nucleotide bindingsearch transferase activity, transferring phosphorus-containing groupssearch protein bindingsearch alpha-2A adrenergic receptor bindingsearch transferase activitysearch beta-adrenergic receptor kinase activitysearch Edg-2 lysophosphatidic acid receptor bindingsearch kinase activitysearch cytoplasmsearch membranesearch cytosolsearch
B (P62871) retina development in camera-type eyesearch adenylate cyclase-activating dopamine receptor signaling pathwaysearch cellular response to catecholamine stimulussearch signal transductionsearch cell proliferationsearch GTP catabolic processsearch phospholipase C-activating G-protein coupled receptor signaling pathwaysearch cellular response to prostaglandin E stimulussearch G-protein coupled receptor signaling pathwaysearch sensory perception of tastesearch protein complex bindingsearch GTPase bindingsearch protein bindingsearch signal transducer activitysearch GTPase activitysearch photoreceptor disc membranesearch photoreceptor outer segmentsearch heterotrimeric G-protein complexsearch extracellular vesicular exosomesearch membranesearch lysosomal membranesearch intracellularsearch
G (P63212) G-protein coupled receptor signaling pathwaysearch cellular response to prostaglandin E stimulussearch GTP catabolic processsearch signal transductionsearch cell proliferationsearch adenylate cyclase-activating dopamine receptor signaling pathwaysearch cellular response to catecholamine stimulussearch G-protein beta-subunit bindingsearch signal transducer activitysearch GTPase activitysearch heterotrimeric G-protein complexsearch membranesearch extracellular vesicular exosomesearch plasma membranesearch

Chain InterPro annotation
A GPCR kinasesearch Regulator of G protein signalling domainsearch Protein kinase domainsearch AGC-kinase, C-terminalsearch Pleckstrin homology domainsearch Serine/threonine/dual specificity protein kinase, catalytic domainsearch Serine/threonine-protein kinase, active sitesearch Protein kinase-like domainsearch Pleckstrin homology-like domainsearch Regulator of G protein signalling superfamilysearch Protein kinase, ATP binding sitesearch
B G-protein, beta subunitsearch WD40 repeatsearch WD40/YVTN repeat-like-containing domainsearch Guanine nucleotide-binding protein, beta subunitsearch WD40-repeat-containing domainsearch WD40 repeat, conserved sitesearch G-protein beta WD-40 repeatsearch
G G-protein, gamma subunitsearch G-protein gamma-like domainsearch