Search: id:"swepub:oai:gup.ub.gu.se/289450" >
A Selective Ligand ...
A Selective Ligand for Estrogen Receptor Proteins Discriminates Rapid and Genomic Signaling
- Article/chapterEnglish2019
Publisher, publication year, extent ...
Numbers
-
LIBRIS-ID:oai:gup.ub.gu.se/289450
-
https://gup.ub.gu.se/publication/289450URI
-
https://doi.org/10.1016/j.chembiol.2019.10.009DOI
Supplementary language notes
Part of subdatabase
Classification
-
Subject category:ref swepub-contenttype
-
Subject category:art swepub-publicationtype
Notes
-
Estrogen exerts extensive and diverse effects throughout the body of women. In addition to the classical nuclear estrogen receptors (ER alpha and ER beta), the G protein-coupled estrogen receptor GPER is an important mediator of estrogen action. Existing ER-targeted therapeutic agents act as GPER agonists. Here, we report the identification of a small molecule, named AB-1, with the previously unidentified activity of high selectivity for binding classical ERs over GPER. AB-1 also possesses a unique functional activity profile as an agonist of transcriptional activity but an antagonist of rapid signaling through ER alpha. Our results define a class of small molecules that discriminate between the classical ERs and GPER, as well as between modes of signaling within the classical ERs. Such an activity profile, if developed into an ER antagonist, could represent an opportunity for the development of first-in-class nuclear hormone receptor-targeted therapeutics for breast cancer exhibiting reduced acquired and de novo resistance.
Subject headings and genre
Added entries (persons, corporate bodies, meetings, titles ...)
-
Bologa, C. G.
(author)
-
Pepermans, R. A.
(author)
-
Sharma, G.
(author)
-
Petrie, W. K.
(author)
-
Alcon, S. N.
(author)
-
Field, A. S.
(author)
-
Ramesh, C.
(author)
-
Parker, M. A.
(author)
-
Savchuk, N. P.
(author)
-
Sklar, L. A.
(author)
-
Hathaway, H. J.
(author)
-
Arterburn, J. B.
(author)
-
Oprea, Tudor IGothenburg University,Göteborgs universitet,Institutionen för medicin, avdelningen för reumatologi och inflammationsforskning,Institute of Medicine, Department of Rheumatology and Inflammation Research
(author)
-
Prossnitz, E. R.
(author)
-
Göteborgs universitetInstitutionen för medicin, avdelningen för reumatologi och inflammationsforskning
(creator_code:org_t)
Related titles
-
In:Cell Chemical Biology: Elsevier BV26:122451-94482451-9456
Internet link
Find in a library
To the university's database
- By the author/editor
-
Revankar, C. M.
-
Bologa, C. G.
-
Pepermans, R. A.
-
Sharma, G.
-
Petrie, W. K.
-
Alcon, S. N.
-
show more...
-
Field, A. S.
-
Ramesh, C.
-
Parker, M. A.
-
Savchuk, N. P.
-
Sklar, L. A.
-
Hathaway, H. J.
-
Arterburn, J. B.
-
Oprea, Tudor I
-
Prossnitz, E. R.
-
show less...
- About the subject
-
- NATURAL SCIENCES
-
NATURAL SCIENCES
-
and Biological Scien ...
-
and Biochemistry and ...
- Articles in the publication
-
Cell Chemical Bi ...
- By the university
-
University of Gothenburg