3cik Summary

pdbe.org/3cik
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Human GRK2 in Complex with Gbetagamma subunits

The structure was published by Tesmer, J.J., Tesmer, V.M., Lodowski, D.T., Steinhagen, H., and Huber, J., in 2010 in a paper entitled "Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol." (abstract).

This crystal structure was determined using X-ray diffraction at a resolution of 2.75 Å and deposited in 2008.

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 P25098 (1-689) (ARBK1_HUMAN)search Homo sapienssearch 93% 689 89%
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
P25098 (1 - 689) Beta-adrenergic receptor kinase 1 Homo sapiens
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 (P25098) 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) Transducin (heterotrimeric G protein), gamma chainsearch PF00631: GGL domainsearch

Chain ID Biological process (GO) Molecular function (GO) Cellular component (GO)
A (P25098) protein phosphorylationsearch positive regulation of catecholamine secretionsearch regulation of the force of heart contractionsearch signal transductionsearch cardiac muscle contractionsearch fibroblast growth factor receptor signaling pathwaysearch desensitization of G-protein coupled receptor protein signaling pathwaysearch negative regulation of striated muscle contractionsearch heart developmentsearch termination of G-protein coupled receptor signaling pathwaysearch activation of phospholipase C activitysearch G-protein coupled receptor signaling pathwaysearch G-protein coupled acetylcholine receptor signaling pathwaysearch peptidyl-threonine phosphorylationsearch neurotrophin TRK receptor signaling pathwaysearch epidermal growth factor receptor signaling pathwaysearch phosphorylationsearch peptidyl-serine phosphorylationsearch tachykinin receptor signaling pathwaysearch receptor internalizationsearch innate immune responsesearch negative regulation of the force of heart contraction by chemical signalsearch protein kinase activitysearch kinase activitysearch protein bindingsearch transferase activity, transferring phosphorus-containing groupssearch ATP bindingsearch G-protein coupled receptor kinase activitysearch protein serine/threonine kinase activitysearch beta-adrenergic receptor kinase activitysearch Edg-2 lysophosphatidic acid receptor bindingsearch nucleotide bindingsearch transferase activitysearch alpha-2A adrenergic receptor bindingsearch primary ciliumsearch membranesearch plasma membranesearch cytoplasmsearch cytosolsearch
B (P62871) G-protein coupled receptor signaling pathwaysearch GTP catabolic processsearch cellular response to prostaglandin E stimulussearch signal transductionsearch retina development in camera-type eyesearch sensory perception of tastesearch adenylate cyclase-activating dopamine receptor signaling pathwaysearch cell proliferationsearch cellular response to catecholamine stimulussearch phospholipase C-activating G-protein coupled receptor signaling pathwaysearch GTPase activitysearch protein bindingsearch GTPase bindingsearch signal transducer activitysearch protein complex bindingsearch membranesearch heterotrimeric G-protein complexsearch intracellularsearch extracellular vesicular exosomesearch photoreceptor disc membranesearch lysosomal membranesearch vesiclesearch photoreceptor outer segmentsearch
G (P63212) cellular response to catecholamine stimulussearch metabolic processsearch G-protein coupled receptor signaling pathwaysearch cellular response to prostaglandin E stimulussearch cell proliferationsearch signal transductionsearch adenylate cyclase-activating dopamine receptor signaling pathwaysearch signal transducer activitysearch GTPase activitysearch G-protein beta-subunit bindingsearch membranesearch heterotrimeric G-protein complexsearch plasma membranesearch extracellular vesicular exosomesearch

Chain InterPro annotation
A GPCR kinasesearch 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 RGS domainsearch 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