Discovery of a potent, orally available, and isoform-selective retinoic acid β2 receptor agonist
Lund, Birgitte W. ; Piu, Fabrice ; Gauthier, Natalie K. ; Eeg, Anne ; Currier, Erika ; Sherbukhin, Vladimir ; Brann, Mark R. ; Hacksell, Uli and Olsson, Roger LU
(2005)
In Journal of Medicinal Chemistry
48(24).
p.7517-7519
- Abstract
4′-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARβ2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorly soluble hit into a more potent and orally available compound (2, AC-261066) with retained β2 selectivity and greatly improved physiochemical properties. Being an isoform-selective RARβ2 receptor agonist that discriminates between nuclear receptor isoforms having identical ligand binding domains, 2 will be useful as a pharmacological research tool but also a valuable starting point for drug development.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/9ab96399-4c6c-4cb1-973e-e7481c33d7be
- author
- Lund, Birgitte W.
; Piu, Fabrice
; Gauthier, Natalie K.
; Eeg, Anne
; Currier, Erika
; Sherbukhin, Vladimir
; Brann, Mark R.
; Hacksell, Uli
and Olsson, Roger
LU
- publishing date
- 2005-11-04
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Journal of Medicinal Chemistry
- volume
- 48
- issue
- 24
- pages
- 7517 - 7519
- publisher
- The American Chemical Society (ACS)
- external identifiers
-
- scopus:28144440125
- pmid:16302793
- ISSN
- 0022-2623
- DOI
- 10.1021/jm050891r
- language
- English
- LU publication?
- no
- id
- 9ab96399-4c6c-4cb1-973e-e7481c33d7be
- date added to LUP
- 2019-10-02 09:53:01
- date last changed
- 2024-04-02 19:06:08
@article{9ab96399-4c6c-4cb1-973e-e7481c33d7be,
abstract = {{<p>4′-Octyl-4-biphenylcarboxylic acid (1g, AC-55649) was identified as a highly isoform-selective agonist at the human RARβ2 receptor in a functional intact cell-based screening assay. The subsequent hit to lead optimization transformed the lipophilic, poorly soluble hit into a more potent and orally available compound (2, AC-261066) with retained β2 selectivity and greatly improved physiochemical properties. Being an isoform-selective RARβ2 receptor agonist that discriminates between nuclear receptor isoforms having identical ligand binding domains, 2 will be useful as a pharmacological research tool but also a valuable starting point for drug development.</p>}},
author = {{Lund, Birgitte W. and Piu, Fabrice and Gauthier, Natalie K. and Eeg, Anne and Currier, Erika and Sherbukhin, Vladimir and Brann, Mark R. and Hacksell, Uli and Olsson, Roger}},
issn = {{0022-2623}},
language = {{eng}},
month = {{11}},
number = {{24}},
pages = {{7517--7519}},
publisher = {{The American Chemical Society (ACS)}},
series = {{Journal of Medicinal Chemistry}},
title = {{Discovery of a potent, orally available, and isoform-selective retinoic acid β2 receptor agonist}},
url = {{http://dx.doi.org/10.1021/jm050891r}},
doi = {{10.1021/jm050891r}},
volume = {{48}},
year = {{2005}},
}