2by4
From Proteopedia
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[[Image:2by4.gif|left|200px]] | [[Image:2by4.gif|left|200px]] | ||
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'''SR CA(2+)-ATPASE IN THE HNE2 STATE COMPLEXED WITH THE THAPSIGARGIN DERIVATIVE BOC-12ADT.''' | '''SR CA(2+)-ATPASE IN THE HNE2 STATE COMPLEXED WITH THE THAPSIGARGIN DERIVATIVE BOC-12ADT.''' | ||
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[[Category: Olsen, C E.]] | [[Category: Olsen, C E.]] | ||
[[Category: Soehoel, H.]] | [[Category: Soehoel, H.]] | ||
- | [[Category: | + | [[Category: Atp-binding]] |
- | [[Category: | + | [[Category: Ca2+-atpase]] |
- | [[Category: | + | [[Category: Calcium]] |
- | [[Category: | + | [[Category: Calcium transport]] |
- | [[Category: | + | [[Category: Endoplasmic reticulum]] |
- | [[Category: | + | [[Category: Hydrolase]] |
- | [[Category: | + | [[Category: Ion transport]] |
- | [[Category: | + | [[Category: Magnesium]] |
- | [[Category: | + | [[Category: Metal-binding]] |
- | [[Category: | + | [[Category: Multigene family]] |
- | [[Category: | + | [[Category: Nucleotide-binding]] |
- | [[Category: | + | [[Category: P-type atpase]] |
- | [[Category: | + | [[Category: Phosphorylation]] |
- | [[Category: | + | [[Category: Prostate cancer]] |
- | [[Category: | + | [[Category: Sarcoplasmic reticulum,transmembrane]] |
- | [[Category: | + | [[Category: Serca]] |
- | [[Category: | + | [[Category: Thapsigargin]] |
- | [[Category: | + | [[Category: Transport]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:57:30 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 17:57, 3 May 2008
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. 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 Sat May 3 20:57:30 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. | 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,transmembrane | Serca | Thapsigargin | Transport