3q4t: Difference between revisions

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{{STRUCTURE_3q4t|  PDB=3q4t  |  SCENE=  }}
==Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with dorsomorphin==
===Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with dorsomorphin===
<StructureSection load='3q4t' size='340' side='right' caption='[[3q4t]], [[Resolution|resolution]] 1.96&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[3q4t]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3Q4T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3Q4T FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=TAK:6-[4-(2-PIPERIDIN-1-YLETHOXY)PHENYL]-3-PYRIDIN-4-YLPYRAZOLO[1,5-A]PYRIMIDINE'>TAK</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">ACVR2, ACVR2A ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein_serine/threonine_kinase Receptor protein serine/threonine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.30 2.7.11.30] </span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3q4t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3q4t OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3q4t RCSB], [http://www.ebi.ac.uk/pdbsum/3q4t PDBsum]</span></td></tr>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
GDF8, or myostatin, is a member of the TGF-beta superfamily of secreted polypeptide growth factors. GDF8 is a potent negative regulator of myogenesis both in vivo and in vitro. We found that GDF8 signaling was inhibited by the small molecule ATP competitive inhibitors Dorsomorphin and LDN-193189. These compounds were previously shown to be potent inhibitors of BMP signaling by binding to the type BMP type I receptors ALK1/2/3/6. We present the crystal structure of the type II receptor ActRIIA with dorsomorphin, and demonstrate that dorsomorphin or LDN-193189 target GDF8 induced Smad2/3 signaling and repression of myogenic transcription factors. As a result, both inhibitors rescue myogenesis in myoblasts treated with GDF8. As revealed by quantitative live cell microscopy, treatment with dorsomorphin or LDN-193189 promoted the contractile activity of myotubular networks in vitro. We therefore suggest these inhibitors as suitable tools to promote functional myogenesis.


==About this Structure==
Small Molecules Dorsomorphin and LDN-193189 Inhibit Myostatin/GDF8 Signaling and Promote Functional Myoblast Differentiation.,Horbelt D, Boergermann JH, Chaikuad A, Alfano I, Williams E, Lukonin I, Timmel T, Bullock AN, Knaus P J Biol Chem. 2014 Nov 3. pii: jbc.M114.604397. PMID:25368322<ref>PMID:25368322</ref>
[[3q4t]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3Q4T OCA].
 
[[Category: Homo sapiens]]
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Human]]
[[Category: Receptor protein serine/threonine kinase]]
[[Category: Receptor protein serine/threonine kinase]]
[[Category: Alfano, I.]]
[[Category: Alfano, I]]
[[Category: Arrowsmith, C H.]]
[[Category: Arrowsmith, C H]]
[[Category: Bountra, C.]]
[[Category: Bountra, C]]
[[Category: Bullock, A.]]
[[Category: Bullock, A]]
[[Category: Chaikuad, A.]]
[[Category: Chaikuad, A]]
[[Category: Cooper, C D.O.]]
[[Category: Cooper, C D.O]]
[[Category: Delft, F von.]]
[[Category: Delft, F von]]
[[Category: Edwards, A M.]]
[[Category: Edwards, A M]]
[[Category: Krojer, T.]]
[[Category: Krojer, T]]
[[Category: Mahajan, P.]]
[[Category: Mahajan, P]]
[[Category: Muniz, J R.C.]]
[[Category: Muniz, J R.C]]
[[Category: Raynor, J.]]
[[Category: Raynor, J]]
[[Category: SGC, Structural Genomics Consortium.]]
[[Category: Structural genomic]]
[[Category: Sanvitale, C.]]
[[Category: Sanvitale, C]]
[[Category: Vollmar, M.]]
[[Category: Vollmar, M]]
[[Category: Weigelt, J.]]
[[Category: Weigelt, J]]
[[Category: Protein kinase]]
[[Category: Protein kinase]]
[[Category: Sgc]]
[[Category: Sgc]]
[[Category: Structural genomics consortium]]
[[Category: Transferase]]
[[Category: Transferase]]
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