Please use this identifier to cite or link to this item:
https://scholarbank.nus.edu.sg/handle/10635/107470
DC Field | Value | |
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dc.title | Interactions of sterols with antiestrogen-binding sites: structural requirements for high-affinity binding | |
dc.contributor.author | Hwang, P.L.H. | |
dc.contributor.author | Matin, A. | |
dc.date.accessioned | 2014-11-06T08:24:52Z | |
dc.date.available | 2014-11-06T08:24:52Z | |
dc.date.issued | 1989 | |
dc.identifier.citation | Hwang, P.L.H.,Matin, A. (1989). Interactions of sterols with antiestrogen-binding sites: structural requirements for high-affinity binding. Journal of Lipid Research 30 (2) : 239-245. ScholarBank@NUS Repository. | |
dc.identifier.issn | 00222275 | |
dc.identifier.uri | http://scholarbank.nus.edu.sg/handle/10635/107470 | |
dc.description.abstract | Animal and human tissues contain a microsomal protein that binds nonsteroidal antiestrogens with high affinity and specificity. The functions of these binding sites and the identity of their natural ligands are unknown. Following a report that certain sterols inhibit [3H]tamoxifen binding to this site, we attempted to define the structural requirements for maximal inhibition of [3H]tamoxifen binding to rat liver antiestrogen-binding sites. Our studies identified 5α-cholestan-3β-ol-7-one (7-ketocholestanol) as the most potent sterol, having an inhibitory activity that was 12% that of unlabeled tamoxifen and an equilibrium dissociation constant of 6.3 nM. Structural features that appeared important for the inhibitory activity of this sterol include the presence of i) a hydrocarbon side chain at C17; ii) an oxygen function at C7; iii) a hydroxyl group at C3; and iv) the absence of a double-bond between C5 and C6. Saturation analysis and kinetic studies of [3H]tamoxifen binding in the presence of varying concentrations of 7-ketocholestanol clearly indicated that this sterol competed directly with tamoxifen for the antiestrogen-binding site. Unlike tamoxifen, this sterol did not bind to the estrogen receptor. These features make 7-ketocholestanol a potentially valuable tool for studying the properties and functions of this site. | |
dc.source | Scopus | |
dc.type | Article | |
dc.contributor.department | PHYSIOLOGY | |
dc.description.sourcetitle | Journal of Lipid Research | |
dc.description.volume | 30 | |
dc.description.issue | 2 | |
dc.description.page | 239-245 | |
dc.description.coden | JLPRA | |
dc.identifier.isiut | NOT_IN_WOS | |
Appears in Collections: | Staff Publications |
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