2by4
From Proteopedia
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==Overview== | ==Overview== | ||
| - | An analysis of the binding of the | + | 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== | ==About this Structure== | ||
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[[Category: Oryctolagus cuniculus]] | [[Category: Oryctolagus cuniculus]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Christensen, S | + | [[Category: Christensen, S B.]] |
| - | [[Category: Denmeade, S | + | [[Category: Denmeade, S R.]] |
| - | [[Category: Isaacs, J | + | [[Category: Isaacs, J T.]] |
| - | [[Category: Jensen, A | + | [[Category: Jensen, A L.]] |
| - | [[Category: Moller, J | + | [[Category: Moller, J V.]] |
[[Category: Nissen, P.]] | [[Category: Nissen, P.]] | ||
| - | [[Category: Olsen, C | + | [[Category: Olsen, C E.]] |
[[Category: Soehoel, H.]] | [[Category: Soehoel, H.]] | ||
[[Category: ACP]] | [[Category: ACP]] | ||
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[[Category: transport]] | [[Category: transport]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:42:51 2008'' |
Revision as of 14:42, 21 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
Page seeded by OCA on Thu Feb 21 16:42:51 2008
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
