Identification of novel subtype selective RAR agonists
(2005) In Biochemical Pharmacology 71(1-2). p.156-162- Abstract
Drugs targeting retinoid receptors have been developed to treat a variety of therapeutic indications, but their success has been limited in part due to lack of selectivity. A novel functional cell-based assay R-SAT™ was employed to screen a small molecule chemical library and identify a variety of novel RAR agonists with various subtype selectivities, including RARβ/γ and RARγ selective agonists. A novel class of synthetic compounds that distinguishes between the different RARβ isoforms is described. This pharmacophore displays anti-proliferative activity and induces differentiation in a neuronal cell line, consistent with a classical retinoid mechanism of action while providing unique subtype selectivity. These novel subtype selective... (More)
Drugs targeting retinoid receptors have been developed to treat a variety of therapeutic indications, but their success has been limited in part due to lack of selectivity. A novel functional cell-based assay R-SAT™ was employed to screen a small molecule chemical library and identify a variety of novel RAR agonists with various subtype selectivities, including RARβ/γ and RARγ selective agonists. A novel class of synthetic compounds that distinguishes between the different RARβ isoforms is described. This pharmacophore displays anti-proliferative activity and induces differentiation in a neuronal cell line, consistent with a classical retinoid mechanism of action while providing unique subtype selectivity. These novel subtype selective RAR agonists could serve as powerful tools to probe into subtype and isoform-specific retinoid function.
(Less)
- author
- Piu, Fabrice ; Gauthier, Natalie K. ; Olsson, Roger LU ; Currier, Erika A. ; Lund, Birgitte W. ; Croston, Glenn E. ; Hacksell, Uli and Brann, Mark R.
- publishing date
- 2005-12-19
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Biochemical Pharmacology
- volume
- 71
- issue
- 1-2
- pages
- 156 - 162
- publisher
- Elsevier
- external identifiers
-
- pmid:16303118
- scopus:28244470800
- ISSN
- 0006-2952
- DOI
- 10.1016/j.bcp.2005.10.025
- language
- English
- LU publication?
- no
- id
- 211db813-26aa-48e8-abd3-4737c67d0af9
- date added to LUP
- 2019-10-02 10:31:48
- date last changed
- 2024-01-16 12:46:01
@article{211db813-26aa-48e8-abd3-4737c67d0af9, abstract = {{<p>Drugs targeting retinoid receptors have been developed to treat a variety of therapeutic indications, but their success has been limited in part due to lack of selectivity. A novel functional cell-based assay R-SAT™ was employed to screen a small molecule chemical library and identify a variety of novel RAR agonists with various subtype selectivities, including RARβ/γ and RARγ selective agonists. A novel class of synthetic compounds that distinguishes between the different RARβ isoforms is described. This pharmacophore displays anti-proliferative activity and induces differentiation in a neuronal cell line, consistent with a classical retinoid mechanism of action while providing unique subtype selectivity. These novel subtype selective RAR agonists could serve as powerful tools to probe into subtype and isoform-specific retinoid function.</p>}}, author = {{Piu, Fabrice and Gauthier, Natalie K. and Olsson, Roger and Currier, Erika A. and Lund, Birgitte W. and Croston, Glenn E. and Hacksell, Uli and Brann, Mark R.}}, issn = {{0006-2952}}, language = {{eng}}, month = {{12}}, number = {{1-2}}, pages = {{156--162}}, publisher = {{Elsevier}}, series = {{Biochemical Pharmacology}}, title = {{Identification of novel subtype selective RAR agonists}}, url = {{http://dx.doi.org/10.1016/j.bcp.2005.10.025}}, doi = {{10.1016/j.bcp.2005.10.025}}, volume = {{71}}, year = {{2005}}, }