Journal ArticleDOI
Identification of novel subtype selective RAR agonists.
Fabrice Piu,Natalie K Gauthier,Roger Olsson,Erika A. Currier,Birgitte W. Lund,Glenn Croston,Uli Hacksell,Mark R. Brann +7 more
TLDR
A novel functional cell-based assay R-SATtrade mark was employed to screen a small molecule chemical library and identify a variety of novel RAR agonists with various subtype selectivities, including RARbeta/gamma and RARgamma selective agonists.About:
This article is published in Biochemical Pharmacology.The article was published on 2005-12-19. It has received 35 citations till now.read more
Citations
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Journal ArticleDOI
Liposomal formulation of retinoids designed for enzyme triggered release.
Palle Jacob Pedersen,Sidsel K. Adolph,Arun Kumar Subramanian,Ahmad Arouri,Thomas Lars Andresen,Ole G. Mouritsen,Robert Madsen,Mikkel Madsen,Günther H.J. Peters,Mads Hartvig Clausen +9 more
TL;DR: Four different retinoid phospholipid prodrugs are synthesized and it is shown that they form particles in the liposome size region with average diameters of 94-118 nm and releasing cytotoxic retinoids and lysolipids.
Journal ArticleDOI
Identification of a small molecule SIRT2 inhibitor with selective tumor cytotoxicity.
TL;DR: A novel SIRT2 inhibitor with high content analysis suggested that AC-93253 significantly triggered apoptosis and may serve as a novel chemical scaffold for structure-activity relationship study and future lead development.
Journal ArticleDOI
Retinoid Receptors and Therapeutic Applications of RAR/RXR Modulators
Albane le Maire,Susana Alvarez,Pattabhiraman Shankaranarayanan,Angel R. de Lera,William Bourguet,Hinrich Gronemeyer +5 more
TL;DR: Strategies in the design of selective RXR and RAR modulators are described and the structural mechanisms by which the diverse pharmacological classes of compounds modulate receptor functions are reviewed.
Journal ArticleDOI
Retinoids Stimulate Periosteal Bone Resorption by Enhancing the Protein RANKL, a Response Inhibited by Monomeric Glucocorticoid Receptor
H. Herschel Conaway,Amir Pirhayati,Emma Persson,Ulrika Pettersson,Olle Svensson,Catharina Lindholm,Petra Henning,Jan Tuckermann,Ulf H. Lerner,Ulf H. Lerner +9 more
TL;DR: The data suggest that ATRA enhances periosteal bone resorption by increasing the RANKL/OPG ratio via RARα receptors, a response that can be inhibited by monomeric GR.
Journal ArticleDOI
Identification of the first synthetic steroidogenic factor 1 inverse agonists: pharmacological modulation of steroidogenic enzymes.
Andria L. Del Tredici,Carsten B. Andersen,Erika A. Currier,Steven R. Ohrmund,Luke C. Fairbain,Birgitte W. Lund,Norman Nash,Roger Olsson,Fabrice Piu +8 more
TL;DR: 4-(heptyloxy)phenol (AC-45594), a prototype inverse agonist lead, was used to show that SF-1 constitutive activity can be pharmacologically modulated by a synthetic ligand.
References
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Journal ArticleDOI
Drug-like properties and the causes of poor solubility and poor permeability
TL;DR: There are currently about 10000 drug-like compounds, and true diversity does not exist in experimental combinatorial chemistry screening libraries because current ADME experimental screens are multi-mechanisms, and predictions get worse as more data accumulates.
Journal ArticleDOI
Retinoic acid induces neuronal differentiation of a cloned human embryonal carcinoma cell line in vitro
TL;DR: Observations constitute the first instance of extensive somatic differentiation of a clonal human EC cell line in vitro when exposed to retinoic acid.
Journal ArticleDOI
Differentially expressed isoforms of the mouse retinoic acid receptor beta generated by usage of two promoters and alternative splicing.
A. Zelent,Cathy Mendelsohn,Philippe Kastner,Andrée Krust,Jean-Marie Garnier,F. Ruffenach,Pierre Leroy,Pierre Chambon +7 more
TL;DR: The conservation of RAR‐beta isoform sequences from mouse to human, as seen by cross‐hybridization on Southern blots or DNA sequence analysis, as well as their differential patterns of expression in various mouse tissues, corroborates this view.
Journal ArticleDOI
Impaired Locomotion and Dopamine Signaling in Retinoid Receptor Mutant Mice
Wojciech Krȩ Ż El,Norbert B. Ghyselinck,Tarek A. Samad,Valérie Dupé,Philippe Kastner,Emiliana Borrelli,Pierre Chambon +6 more
TL;DR: In the adult mouse, single and compound null mutations in the genes for retinoic acid receptor beta and retinoid X receptors beta and gamma resulted in locomotor defects related to dysfunction of the mesolimbic dopamine signaling pathway.
Journal ArticleDOI
Retinoic acid receptor beta mediates the growth-inhibitory effect of retinoic acid by promoting apoptosis in human breast cancer cells.
TL;DR: RAR beta can mediate retinoid action in breast cancer cells by promoting apoptosis and loss of RAR beta, therefore, may contribute to the tumorigenicity of human mammary epithelial cells.
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Beta-arrestin 2 modulates the activity of nuclear receptor RAR beta2 through activation of ERK2 kinase.
Fabrice Piu,N K Gauthier,F Wang +2 more