Activin receptor
From Proteopedia
(Difference between revisions)
(New page: <StructureSection load='1stp' size='340' side='right' caption='Caption for this structure' scene=''> <ref>PMID:21638687</ref> to the rescue. == Function == == Disease == == Relevance =...) |
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| - | + | <StructureSection load='4bgg' size='340' side='right' caption='Human Acvr1 kinase domain complex with inhibitor, ethylene glycol and citrate (PDB code [[4bgg]])' scene='84/843934/Cv/1'> | |
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== Function == | == Function == | ||
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| + | '''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<ref>PMID:23721881</ref>. | ||
| + | *'''Acvr1''' is involved in bone, heart, cartilage, nervous and reproductive system development and regulation<ref>PMID:31683698</ref>. | ||
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| + | See also: [[Enzyme-linked receptor]]. | ||
== Disease == | == Disease == | ||
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| + | A mutation in Acvr1 exists in individuals with the rare developmental disorder fibrodysplasia ossificans progressiva<ref>PMID:28918311</ref>. | ||
== Relevance == | == Relevance == | ||
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| + | 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<ref>PMID:30842316</ref>. | ||
== Structural highlights == | == Structural highlights == | ||
| - | + | 3D structure of the kinase domain of Acvr1 complex with inhibitor shows <scene name='84/843934/Cv/3'>the inhibitor forming various interactions</scene> with the protein including a <scene name='84/843934/Cv/5'>hydrogen bonds to His residues</scene> and a <scene name='84/843934/Cv/6'>water bridged hydrogen bond to the catalytic lysine</scene><ref>PMID:25101911</ref>. Water molecule is shown as red sphere. | |
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==3D structures of activin receptor== | ==3D structures of activin receptor== | ||
| - | + | [[Activin receptor 3D structures]] | |
| - | **[[5oxg]] - hAcvr1 kinase domain 172-499 + inhibitor - human<br /> | ||
| - | **[[6acr]], [[6gi6]], [[6gip]], [[6gin]], [[4bgg]], [[3q4u]], [[3mtf]] - hAcvr1 kinase domain (mutant) + inhibitor<br /> | ||
| - | **[[3h9r]] - hAcvr1 kinase domain + FKBP12 + inhibitor<br /> | ||
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| - | *Activin receptor type 2 | ||
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| - | **[[1bte]] - Acvr2 LBD 25-121 - mouse<br /> | ||
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| - | *Activin receptor type 2A | ||
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| - | **[[4asx]], [[3soc]], [[3q4t]] - hAcvr2A kinase domain + inhibitor<br /> | ||
| - | **[[5nh3]] - hAcvr2A LBD + antibody<br /> | ||
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| - | *Activin receptor type 2B | ||
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| - | **[[2qlu]] - hAcvr2B kinase domain<br /> | ||
| - | **[[5ngv]], [[5nhr]] - hAcvr2B LBD + antibody<br /> | ||
| - | **[[1s4y]] - mAcvr2B LBD + inhibin<br /> | ||
| - | **[[1nyu]] - rAcvr2B LBD + inhibin - rat<br /> | ||
| - | }} | ||
== References == | == References == | ||
<references/> | <references/> | ||
| + | </StructureSection> | ||
| + | [[Category:Topic Page]] | ||
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