2by4 | pdb_00002by4
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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 Structure known Active 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 Mon Nov 5 17:52:36 2007
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- 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
