3q4t

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (11:33, 14 March 2024) (edit) (undo)
 
Line 3: Line 3:
<StructureSection load='3q4t' size='340' side='right'caption='[[3q4t]], [[Resolution|resolution]] 1.96&Aring;' scene=''>
<StructureSection load='3q4t' size='340' side='right'caption='[[3q4t]], [[Resolution|resolution]] 1.96&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
-
<table><tr><td colspan='2'>[[3q4t]] is a 2 chain structure with sequence from [https://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 [https://proteopedia.org/fgij/fg.htm?mol=3Q4T FirstGlance]. <br>
+
<table><tr><td colspan='2'>[[3q4t]] is a 2 chain structure with sequence from [https://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]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3Q4T FirstGlance]. <br>
-
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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>
+
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.96&#8491;</td></tr>
-
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">ACVR2, ACVR2A ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
+
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Receptor_protein_serine/threonine_kinase Receptor protein serine/threonine kinase], with EC number [https://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'>[https://proteopedia.org/fgij/fg.htm?mol=3q4t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3q4t OCA], [https://pdbe.org/3q4t PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3q4t RCSB], [https://www.ebi.ac.uk/pdbsum/3q4t PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3q4t ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3q4t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3q4t OCA], [https://pdbe.org/3q4t PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3q4t RCSB], [https://www.ebi.ac.uk/pdbsum/3q4t PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3q4t ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
-
[[https://www.uniprot.org/uniprot/AVR2A_HUMAN AVR2A_HUMAN]] On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin A, activin B and inhibin A.
+
[https://www.uniprot.org/uniprot/AVR2A_HUMAN AVR2A_HUMAN] On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin A, activin B and inhibin A.
-
<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.
+
-
 
+
-
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>
+
-
 
+
-
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+
-
</div>
+
-
<div class="pdbe-citations 3q4t" style="background-color:#fffaf0;"></div>
+
-
== References ==
+
-
<references/>
+
__TOC__
__TOC__
</StructureSection>
</StructureSection>
-
[[Category: Human]]
+
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
-
[[Category: Receptor protein serine/threonine kinase]]
+
[[Category: Alfano I]]
-
[[Category: Alfano, I]]
+
[[Category: Arrowsmith CH]]
-
[[Category: Arrowsmith, C H]]
+
[[Category: Bountra C]]
-
[[Category: Bountra, C]]
+
[[Category: Bullock A]]
-
[[Category: Bullock, A]]
+
[[Category: Chaikuad A]]
-
[[Category: Chaikuad, A]]
+
[[Category: Cooper CDO]]
-
[[Category: Cooper, C D.O]]
+
[[Category: Edwards AM]]
-
[[Category: Delft, F von]]
+
[[Category: Krojer T]]
-
[[Category: Edwards, A M]]
+
[[Category: Mahajan P]]
-
[[Category: Krojer, T]]
+
[[Category: Muniz JRC]]
-
[[Category: Mahajan, P]]
+
[[Category: Raynor J]]
-
[[Category: Muniz, J R.C]]
+
[[Category: Sanvitale C]]
-
[[Category: Raynor, J]]
+
[[Category: Vollmar M]]
-
[[Category: Structural genomic]]
+
[[Category: Weigelt J]]
-
[[Category: Sanvitale, C]]
+
[[Category: Von Delft F]]
-
[[Category: Vollmar, M]]
+
-
[[Category: Weigelt, J]]
+
-
[[Category: Protein kinase]]
+
-
[[Category: Sgc]]
+
-
[[Category: Transferase]]
+

Current revision

Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with dorsomorphin

PDB ID 3q4t

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/3q4t"
Personal tools