Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site

Ross V. Weatherman; David C. Carroll; Thomas S. Scanlan

doi:10.1016/S0960-894X(01)00646-1

Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site

Ross V. Weatherman, David C. Carroll, Thomas S. Scanlan

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

To test the effect of ligand flexibility on the selective transcriptional activities of ERα and ERβ from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERα than with ERβ, mimicking 4-hydroxytamoxifen more than raloxifene.

Original language	English (US)
Pages (from-to)	3129-3131
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	24
DOIs	https://doi.org/10.1016/S0960-894X(01)00646-1
State	Published - Dec 17 2001
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/S0960-894X(01)00646-1

Cite this

@article{30d697534d9647059ad67c7992d8a5cb,

title = "Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site",

abstract = "To test the effect of ligand flexibility on the selective transcriptional activities of ERα and ERβ from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERα than with ERβ, mimicking 4-hydroxytamoxifen more than raloxifene.",

author = "Weatherman, {Ross V.} and Carroll, {David C.} and Scanlan, {Thomas S.}",

note = "Funding Information: The work was supported by a grant from the National Institutes of Health (DK-57574). R.V.W. was supported by a postdoctoral fellowship from the American Cancer Society, California Division.",

year = "2001",

month = dec,

day = "17",

doi = "10.1016/S0960-894X(01)00646-1",

language = "English (US)",

volume = "11",

pages = "3129--3131",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "24",

}

TY - JOUR

T1 - Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site

AU - Weatherman, Ross V.

AU - Carroll, David C.

AU - Scanlan, Thomas S.

N1 - Funding Information: The work was supported by a grant from the National Institutes of Health (DK-57574). R.V.W. was supported by a postdoctoral fellowship from the American Cancer Society, California Division.

PY - 2001/12/17

Y1 - 2001/12/17

N2 - To test the effect of ligand flexibility on the selective transcriptional activities of ERα and ERβ from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERα than with ERβ, mimicking 4-hydroxytamoxifen more than raloxifene.

AB - To test the effect of ligand flexibility on the selective transcriptional activities of ERα and ERβ from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERα than with ERβ, mimicking 4-hydroxytamoxifen more than raloxifene.

UR - http://www.scopus.com/inward/record.url?scp=0035904877&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0035904877&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(01)00646-1

DO - 10.1016/S0960-894X(01)00646-1

M3 - Article

C2 - 11720858

AN - SCOPUS:0035904877

SN - 0960-894X

VL - 11

SP - 3129

EP - 3131

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this