Activin receptor

spinqualitylabelsall models Human Acvr1 kinase domain complex with inhibitor, ethylene glycol and citrate (PDB code 4bgg) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Function Activin receptors (Acvr) are integral to the activin and myostatin signalling pathway. Binding of activin to the Acvr on muscle cell membrane leads to enhanced muscle protein breakdown and debilitating loss of muscle mass and functional capacity. See also: Enzyme-linked receptor. Disease A mutation in Acrv1 exists in individuals with the rare developmental disorder fibrodysplasia ossificans progressiva. Relevance Increased activin/Acvr2 signalling links aging and heart failure pathobiology and that targeted inhibition of this catabolic pathway may form a therapeutic strategy for multiple forms of hear failure. Structural highlights 3D structure of the kinase domain of Acvr1 complex with inhibitor shows the inhibitor forming various interactions with the protein including a hydrogen bonds to His residues and a water bridged hydrogen bond to the catalytic lysine. Water molecule is shown as red sphere.

3D structures of activin receptor

Updated on 09-January-2023

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• Activin receptor type 1 or Activin receptor-like type 2 or Serine/threonine-protein kinase receptor R1 or ALK2 or BMP type 1 receptor kinase
  • Enzyme-linked receptor - hAcvr1 kinase domain 172-499 + inhibitor - human
    
  • 6acr, 6gi6, 6gip, 6gin, 4bgg, 3q4u, 3mtf, 6t6d, 6jux, 6tnb, 6tn8, 6t8n, 6szm, 6eix, 6srh, 5oy6, 6z36, 6zgc, 7a21, 7c3g - hAcvr1 kinase domain (mutant) + inhibitor
    
  • 3h9r, 4c02, 6i1s - hAcvr1 kinase domain + FKBP12 + inhibitor
    
  • 7nns - hAcvr1 kinase domain + drug
    
• Activin receptor type 2
  • 1bte - Acvr2 LBD 19-134 - mouse
    
• Activin receptor type 2A
  • 4asx, 3soc, 3q4t - hAcvr2A kinase domain + inhibitor
    
  • 5nh3 - hAcvr2A LBD + antibody
    
  • 7u5p - hAcvr2A LBD + inhibin
    
  • 2goo, 2h64, 2h62 - mAcvr2A LBD + BMP-2 + ALK3
    
  • 1lx5 - mAcvr2A LBD + BMP-7
    
• Activin receptor type 2B
  • 2qlu - hAcvr2B kinase domain
    
  • 5ngv, 5nhr - hAcvr2B LBD + antibody
    
  • 7oly - hAcvr2B LBD + hAcvr1B LBD + antibody + inhibin
    
  • 7mrz - hAcvr2B LBD + hAcvr1B LBD + antibody + GDF11
    
  • 1s4y - mAcvr2B LBD + inhibin
    
  • 1nyu - rAcvr2B LBD + inhibin - rat
    
  • 6mac - rAcvr2B LBD + GDF-11 + ALK5
    
• Activin receptor-like type 1 or Serine/threonine-protein kinase receptor R3 or ALK1
  • 2lcr - hALK1 LBD - NMR
    
  • 6sf2 - hALK1 LBD + GDF-2
    
  • 4fao - hALK1 LBD + GDF-2 + SKR3
    
  • 6sf1, 6sf3 - hALK1 LBD + BMP10
    
  • 3my0 - hALK1 kinase domain + inhibitor
    

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Michal Harel, Alexander Berchansky