2by4: Difference between revisions
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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 MG, NA, AD4 and ACP as ligands. Active as Calcium-transporting ATPase, with EC number 3.6.3.8 Known structural/functional Site: AC1. 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
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.
- 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
