4d0n
From Proteopedia
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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=4d0n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d0n OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4d0n RCSB], [http://www.ebi.ac.uk/pdbsum/4d0n PDBsum]</span></td></tr> | <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=4d0n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d0n OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4d0n RCSB], [http://www.ebi.ac.uk/pdbsum/4d0n PDBsum]</span></td></tr> | ||
<table> | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Revision as of 06:45, 24 September 2014
AKAP13 (AKAP-Lbc) RhoGEF domain in complex with RhoA
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Categories: Small monomeric GTPase | Allerston, C. | Arrowsmith, C. | Azeez, K R.Abdul. | Bountra, C. | Delft, F von. | Edwards, A M. | Elkins, J M. | Klussmann, E. | Knapp, S. | Krojer, T. | Shrestha, L. | Akap-lbc | Akap13 | Cell cycle | Dh domain | Gef | Lbc | Ph domain | Rhogef
