Results 161 to 170 of about 51,241 (200)
Modification at the Lipophilic Domain of RXR Agonists Differentially Influences Activation of RXR Heterodimers [PDF]
ACS Medicinal Chemistry Letters, 2010 RXR permissive heterodimers are reported to be activated differently depending upon the chemical structure of RXR agonists, but the relationship of agonist structure to differential heterodimer activation has not been explored in detail. In this study, we performed systematic conversion of the alkoxy side chain of 5a (6-[ethyl-(3-isopropoxy-4 ...
Hiroki Kakuta
exaly +3 more sources
Some of the next articles are maybe not open access.
Related searches:
Related searches:
Activation of specific RXR heterodimers by an antagonist of RXR homodimers
Nature, 1996Retinoid X receptor (RXR) plays a central role in the regulation of many intracellular receptor signalling pathways and can mediate ligand-dependent transcription, acting as a homodimer or as a heterodimer. Here we identify an antagonist towards RXR homodimers which also functions as an agonist when RXR is paired as a heterodimer to specific partners ...
D S, Lala +8 more
openaire +2 more sources
RAR/RXR and PPAR/RXR signaling in neurological and psychiatric diseases
Progress in Neurobiology, 2008Retinoids are important signals in brain development. They regulate gene transcription by binding to retinoic acid receptors (RAR) and, as was discovered recently, a peroxisome proliferator-activated receptor (PPAR). Traditional ligands of PPAR are best known for their functions in lipid metabolism and inflammation.
Sabien, van Neerven +2 more
openaire +2 more sources
Natural ligands of RXR receptors
2020Given the role of retinoid X receptors (RXRs) as promiscuous partners of heterodimeric complexes with other members of the Nuclear Receptor (NR) superfamily, RXR ligands (rexinoids) play fundamental roles in gene transcription, since upon ligand binding either transcriptionally activate the "permissive" subclass of heterodimers or synergize with ...
Patricia, García +2 more
openaire +2 more sources
2014
Retinoid X Receptors (RXR) were initially identified as nuclear receptors binding with stereo-selectivity the vitamin A derivative 9-cis retinoic acid, although the relevance of this molecule as endogenous activator of RXRs is still elusive. Importantly, within the nuclear receptor superfamily, RXRs occupy a peculiar place, as they are obligatory ...
Gilardi F, Desvergne B
openaire +3 more sources
Retinoid X Receptors (RXR) were initially identified as nuclear receptors binding with stereo-selectivity the vitamin A derivative 9-cis retinoic acid, although the relevance of this molecule as endogenous activator of RXRs is still elusive. Importantly, within the nuclear receptor superfamily, RXRs occupy a peculiar place, as they are obligatory ...
Gilardi F, Desvergne B
openaire +3 more sources
Discovery and SAR of Natural-Product-Inspired RXR Agonists with Heterodimer Selectivity to PPARδ-RXR
ACS Chemical Biology, 2020A known natural product, magnaldehyde B, was identified as an agonist of retinoid X receptor (RXR) α. Magnaldehyde B was isolated from Magnolia obovata (Magnoliaceae) and synthesized along with more potent analogs for screening of their RXRα agonistic activities.
Ken-ichi Nakashima +10 more
openaire +2 more sources
Advances in drug design with RXR modulators
Expert Opinion on Drug Discovery, 2012Retinoid X receptors (subtypes RXRα or NR2B1, RXRβ or NR2B2 and RXRγ or NR2B3, which originate from three distinct genes) are promiscuous partners with heterodimeric associations to other members of the Nuclear Receptor (NR) superfamily. Some of the heterodimers are "permissive" and transcriptionally active in the presence of either an RXR ligand ...
Belen Vaz, Angel R De Lera
exaly +3 more sources
Bioorganic and Medicinal Chemistry Letters, 2010
Retinoid X receptors (RXRs) function as homo- or heterodimers with other nuclear receptors, such as peroxisome proliferator-activated receptors (PPARs), which are targets for treatment of hyperlipidemia and type 2 diabetes, or liver X receptors (LXRs), which are involved in glucose/lipid metabolism.
Hiroki Kakuta
exaly +3 more sources
Retinoid X receptors (RXRs) function as homo- or heterodimers with other nuclear receptors, such as peroxisome proliferator-activated receptors (PPARs), which are targets for treatment of hyperlipidemia and type 2 diabetes, or liver X receptors (LXRs), which are involved in glucose/lipid metabolism.
Hiroki Kakuta
exaly +3 more sources
Blood, 2007
[Comment on Taschner et al, page 971][1]The nuclear receptor superfamily contains members with known ligands, orphans, and RXR playing a subservient role as heterodimer partner. Taschner and colleagues demonstrate that RXRα may be more than a stepchild.
Kathleen A. Hoag, Denise E. Lackey
openaire +1 more source
[Comment on Taschner et al, page 971][1]The nuclear receptor superfamily contains members with known ligands, orphans, and RXR playing a subservient role as heterodimer partner. Taschner and colleagues demonstrate that RXRα may be more than a stepchild.
Kathleen A. Hoag, Denise E. Lackey
openaire +1 more source
Design and synthesis of fluorinated RXR modulators
Bioorganic & Medicinal Chemistry Letters, 2003Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the position of fluorination, and improvement in pharmacological profile was demonstrated in some cases.
D L, Gernert +12 more
openaire +2 more sources