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Aza-retinoids as novel retinoid X receptor-specific agonists

Bioorganic & Medicinal Chemistry Letters, 2006
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Dave W. Robertson   +8 more
openaire   +4 more sources

Diminished teratogenicity of retinoid X receptor-selective synthetic retinoids

Biochemical Pharmacology, 1995
One feature that contraindicates the wide therapeutic use of retinoids is their teratogenicity. Synthetic retinoids are distinguishable from each other on the basis of their partial or exclusive preference in binding and activation of all-trans retinoic acid receptors (RARs) or retinoid X receptors (RXRs). Using mouse embryo limb bud cells in micromass
Heng Jiang   +4 more
openaire   +3 more sources

Retinoid X receptors

The International Journal of Biochemistry & Cell Biology, 1997
Retinoids are metabolites of retinol (vitamin A), which act as signalling molecules in embryogenesis and as stimulators of cellular differentiation. The potency of retinoids as differentiating agents has led to their successful use in treating skin diseases and some forms of cancer.
openaire   +3 more sources

Heterodimerization of the Drosophila ecdysone receptor with retinoid X receptor and ultraspiracle

Nature, 1993
Ecdysone in Drosophila has been a paradigm for steroid hormones since its ability to induce gene activity directly was demonstrated by its effects on moulting and polytene chromosome puffing. The ecdysone receptor (EcR) was recently confirmed as a member of the nuclear receptor superfamily by cloning and characterization in a Drosophila cell line. Here
Thomas He, H. Stunnenberg, Stewart Af
semanticscholar   +4 more sources

Limited Degradation of Retinoid X Receptor by Calpain

Biochemical and Biophysical Research Communications, 1996
Recently, we have found two major physiological forms of retinoid X receptor alpha (RXR alpha): the mature 54 kDa RXR alpha and the truncated 44 kDa RXR alpha lacking a portion of N-terminal A/B domain in human and rodent livers. In this communication, we show that m-calpain was active to digest 54 kDa RXR alpha in the human hepatoma-derived cell line,
Rie Matsushima-Nishiwaki   +4 more
openaire   +3 more sources

Determinants of Retinoid X Receptor Transcriptional Antagonism

Journal of Medicinal Chemistry, 2004
The synthesis and bioactivity of the retinoid X receptor (RXR) antagonist 4-[(3'-n-butyl-5',6',7',8'-tetrahydro-5',5',8',8'-tetramethyl-2'-naphthalenyl)(cyclopropylidene)methyl]benzoic acid and several heteroatom-substituted analogues are described. Ligand design was based on the scaffold of the 3'-methyl RXR-selective agonist analogue and reports that
Marcia I. Dawson   +11 more
openaire   +3 more sources

Docosahexaenoic acid, a ligand for the retinoid X receptor in mouse brain.

Science, 2000
The retinoid X receptor (RXR) is a nuclear receptor that functions as a ligand-activated transcription factor. Little is known about the ligands that activate RXR in vivo. Here, we identified a factor in brain tissue from adult mice that activates RXR in
A. M. D. Urquiza   +6 more
semanticscholar   +1 more source

International Union of Pharmacology. LXIII. Retinoid X Receptors

Pharmacological Reviews, 2006
The physiological effects of retinoic acids (RAs) are mediated by members of two families of nuclear receptors, the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs), which are encoded by three distinct human genes, RXRalpha, RXRbeta, and RXRgamma.
Germain, Pierre   +9 more
openaire   +4 more sources

Cloning of crustacean ecdysteroid receptor and retinoid-X receptor gene homologs and elevation of retinoid-X receptor mRNA by retinoic acid

Molecular and Cellular Endocrinology, 1998
We report the cloning and analysis of ecdysteroid receptor (bpEcR) and retinoid-X receptor (UpRXR) cDNA homologs from the fiddler crab Uca pugilator. The deduced amino acid sequence of this crustacean EcR most closely resembles the insect EcRs within the DNA binding and ligand binding domains (LBDs).
Sandra W. Clifton   +4 more
openaire   +3 more sources

Conformational Effects on Retinoid Receptor Selectivity. 2. Effects of Retinoid Bridging Group on Retinoid X Receptor Activity and Selectivity

Journal of Medicinal Chemistry, 1995
The natural retinoid 9-cis-retinoic acid is an activating ligand for both the retinoic acid receptors (RARs) and the retinoid X receptors (RXRs), which are members of the retinoid/thyroid hormone/steroid hormone family of nuclear receptor proteins that activate gene transcription through specific response elements.
M I, Dawson   +8 more
openaire   +3 more sources

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