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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
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- 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