2by4
From Proteopedia
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| - | [[Image:2by4.gif|left|200px]]<br /><applet load="2by4" size=" | + | [[Image:2by4.gif|left|200px]]<br /><applet load="2by4" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2by4, resolution 3.30Å" /> | caption="2by4, resolution 3.30Å" /> | ||
'''SR CA(2+)-ATPASE IN THE HNE2 STATE COMPLEXED WITH THE THAPSIGARGIN DERIVATIVE BOC-12ADT.'''<br /> | '''SR CA(2+)-ATPASE IN THE HNE2 STATE COMPLEXED WITH THE THAPSIGARGIN DERIVATIVE BOC-12ADT.'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2BY4 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus] with MG, NA, AD4 and ACP as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Calcium-transporting_ATPase Calcium-transporting ATPase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.6.3.8 3.6.3.8] Known structural/functional Site: <scene name='pdbsite=AC1:Na Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 2BY4 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=NA:'>NA</scene>, <scene name='pdbligand=AD4:'>AD4</scene> and <scene name='pdbligand=ACP:'>ACP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Calcium-transporting_ATPase Calcium-transporting ATPase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.6.3.8 3.6.3.8] Known structural/functional Site: <scene name='pdbsite=AC1:Na+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BY4 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transport]] | [[Category: transport]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:29:12 2008'' |
Revision as of 08:29, 3 February 2008
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SR CA(2+)-ATPASE IN THE HNE2 STATE COMPLEXED WITH THE THAPSIGARGIN DERIVATIVE BOC-12ADT.
Overview
An analysis of the binding of the, 8-O-N-tert-butoxycarbonyl-12-aminododecanoyl derivative of, 8-O-debutanoylthapsigargin to the target molecule, the SERCA pump, has, revealed the importance of the length and flexibility of the side chain, attached to O-8. Based on the analysis a series of analogues to the, 2-unsubstituted analogue trilobolide has been constructed and shown to be, equipotent with thapsigargin as SERCA inhibitors. Only the, 12-Boc-aminododecaonoyl derivative, however, was found to be apoptotic.
About this Structure
2BY4 is a Single protein structure of sequence from Oryctolagus cuniculus with , , and as ligands. Active as Calcium-transporting ATPase, with EC number 3.6.3.8 Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Natural products as starting materials for development of second-generation SERCA inhibitors targeted towards prostate cancer cells., Sohoel H, Jensen AM, Moller JV, Nissen P, Denmeade SR, Isaacs JT, Olsen CE, Christensen SB, Bioorg Med Chem. 2006 Apr 15;14(8):2810-5. Epub 2006 Jan 10. PMID:16412648
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Categories: Calcium-transporting ATPase | Oryctolagus cuniculus | Single protein | Christensen, S.B. | Denmeade, S.R. | Isaacs, J.T. | Jensen, A.L. | Moller, J.V. | Nissen, P. | Olsen, C.E. | Soehoel, H. | ACP | AD4 | MG | NA | Atp-binding | Ca2+-atpase | Calcium | Calcium transport | Endoplasmic reticulum | Hydrolase | Ion transport | Magnesium | Metal-binding | Multigene family | Nucleotide-binding | P-type atpase | Phosphorylation | Prostate cancer | Sarcoplasmic reticulum | Serca | Thapsigargin | Transmembrane | Transport
