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PDBsum entry 3pvu

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protein ligands Protein-protein interface(s) links
Transferase/signaling protein/inhibitor PDB id
3pvu

 

 

 

 

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Contents
Protein chains
609 a.a.
339 a.a.
61 a.a.
Ligands
QRW
Waters ×12
PDB id:
3pvu
Name: Transferase/signaling protein/inhibitor
Title: Bovine grk2 in complex with gbetagamma subunits and a selective kinase inhibitor (cmpd101)
Structure: Beta-adrenergic receptor kinase 1. Chain: a. Synonym: grk2, beta-ark-1, g-protein-coupled receptor kinase 2. Engineered: yes. Mutation: yes. Guanine nucleotide-binding protein g(i)/g(s)/g(t) subunit beta-1. Chain: b. Synonym: transducin beta chain 1.
Source: Bos taurus. Bovine. Organism_taxid: 9913. Gene: adrbk1, grk2. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Gene: gnb1. Gene: gng2. Expression_system_taxid: 7108
Resolution:
2.48Å     R-factor:   0.229     R-free:   0.274
Authors: D.M.Thal,J.J.Tesmer
Key ref: D.M.Thal et al. (2011). Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol Pharmacol, 80, 294-303. PubMed id: 21596927
Date:
07-Dec-10     Release date:   01-Jun-11    
PROCHECK
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 Headers
 References

Protein chain
Pfam   ArchSchema ?
P21146  (ARBK1_BOVIN) -  Beta-adrenergic receptor kinase 1 from Bos taurus
Seq:
Struc:
 
Seq:
Struc:
689 a.a.
609 a.a.
Protein chain
Pfam   ArchSchema ?
P62871  (GBB1_BOVIN) -  Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 from Bos taurus
Seq:
Struc:
340 a.a.
339 a.a.
Protein chain
Pfam   ArchSchema ?
P63212  (GBG2_BOVIN) -  Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 from Bos taurus
Seq:
Struc:
71 a.a.
61 a.a.*
Key:    PfamA domain  Secondary structure  CATH domain
* PDB and UniProt seqs differ at 1 residue position (black cross)

 Enzyme reactions 
   Enzyme class: Chain A: E.C.2.7.11.15  - [beta-adrenergic-receptor] kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: [beta-adrenergic receptor] + ATP = [beta-adrenergic receptor]-phosphate + ADP + H+
[beta-adrenergic receptor]
+ ATP
= [beta-adrenergic receptor]-phosphate
+ ADP
+ H(+)
Molecule diagrams generated from .mol files obtained from the KEGG ftp site

 

 
    reference    
 
 
Mol Pharmacol 80:294-303 (2011)
PubMed id: 21596927  
 
 
Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.
D.M.Thal, R.Y.Yeow, C.Schoenau, J.Huber, J.J.Tesmer.
 
  ABSTRACT  
 
No abstract given.

 

 

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