4d0o

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==AKAP13 (AKAP-Lbc) DH domain==
==AKAP13 (AKAP-Lbc) DH domain==
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<StructureSection load='4d0o' size='340' side='right' caption='[[4d0o]], [[Resolution|resolution]] 2.75&Aring;' scene=''>
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<StructureSection load='4d0o' size='340' side='right'caption='[[4d0o]], [[Resolution|resolution]] 2.75&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4d0o]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4D0O OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4D0O FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4d0o]] 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=4D0O OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4D0O FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4d0n|4d0n]]</td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.75&#8491;</td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4d0o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d0o OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4d0o RCSB], [http://www.ebi.ac.uk/pdbsum/4d0o PDBsum]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4d0o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d0o OCA], [https://pdbe.org/4d0o PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4d0o RCSB], [https://www.ebi.ac.uk/pdbsum/4d0o PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4d0o ProSAT]</span></td></tr>
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<table>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/AKP13_HUMAN AKP13_HUMAN] Anchors cAMP-dependent protein kinase (PKA) and acts as an adapter protein to selectively couple G alpha-13 and Rho. Augments gene activation by the estrogen receptor in an element-specific and ligand-dependent manner. Activates estrogen receptor beta by a p38 MAPK-dependent pathway. Stimulates exchange activity on Rho proteins in vitro, but not on CDC42, Ras or Rac and may bind calcium ions.<ref>PMID:11546812</ref> <ref>PMID:9627117</ref> <ref>PMID:9891067</ref> <ref>PMID:11579095</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The RhoGEF domain of AKAP-Lbc (AKAP13) catalyses nucleotide exchange on RhoA and is involved in development of cardiac hypertrophy. The RhoGEF activity of AKAP-Lbc has also been implicated in cancer. We have determined the X-ray crystal structure of the complex between RhoA:GDP and the AKAP-Lbc RhoGEF (DH-PH) domain to 2.1 A resolution. The structure reveals important differences compared to related RhoGEF proteins such as Leukemia-associated RhoGEF. Nucleotide exchange assays comparing the activity of the DH-PH domain to the DH domain alone showed no role for the PH domain in nucleotide exchange, which is explained by the RhoA:AKAP-Lbc structure. Comparison to a structure of the isolated AKAP-Lbc DH domain revealed a change in conformation of the N-terminal 'GEF switch' region upon binding to RhoA. Isothermal titration calorimetry showed that AKAP-Lbc has only micromolar affinity for RhoA which combined with the presence of potential binding pockets for small molecules on AKAP-Lbc raises the possibility of targeting AKAP-Lbc with guanine nucleotide exchange factor inhibitors.
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The Crystal Structure of the RhoA : AKAP-Lbc DH-PH Domain Complex.,Abdul Azeez KR, Knapp S, Fernandes JM, Klussmann E, Elkins JM Biochem J. 2014 Sep 4. PMID:25186459<ref>PMID:25186459</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4d0o" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[A-kinase anchor protein 3D structures|A-kinase anchor protein 3D structures]]
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Allerston, C.]]
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[[Category: Homo sapiens]]
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[[Category: Arrowsmith, C.]]
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[[Category: Large Structures]]
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[[Category: Azeez, K R.Abdul.]]
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[[Category: Abdul Azeez KR]]
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[[Category: Bountra, C.]]
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[[Category: Allerston C]]
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[[Category: Delft, F von.]]
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[[Category: Arrowsmith C]]
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[[Category: Edwards, A M.]]
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[[Category: Bountra C]]
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[[Category: Elkins, J M.]]
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[[Category: Edwards AM]]
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[[Category: Klussmann, E.]]
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[[Category: Elkins JM]]
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[[Category: Knapp, S.]]
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[[Category: Klussmann E]]
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[[Category: Krojer, T.]]
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[[Category: Knapp S]]
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[[Category: Shrestha, L.]]
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[[Category: Krojer T]]
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[[Category: Akap-lbc]]
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[[Category: Shrestha L]]
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[[Category: Cell cycle]]
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[[Category: Von Delft F]]
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[[Category: Gef]]
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[[Category: Ph domain]]
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[[Category: Rhogef]]
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Current revision

AKAP13 (AKAP-Lbc) DH domain

PDB ID 4d0o

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