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Literature DB >> 17035009

Identification of a series of highly potent activators of the Nurr1 signaling pathway.

Samuel Hintermann¹, Michele Chiesi, Ulrike von Krosigk, Danièle Mathé, Richard Felber, Bastian Hengerer.

Abstract

The nuclear receptor Nurr1 (NR4A2) is critically involved in the development and maintenance of midbrain dopaminergic neurons and is believed to function independently of endogenous activation. The hit identification and SAR studies leading to isoxazolo-pyridinone 7e, a highly potent, brain penetrable activator of the Nurr1 signaling pathway, are described.

Entities: Chemical Gene

Mesh：

Substances：

Year: 2006 PMID： 17035009 DOI： 10.1016/j.bmcl.2006.09.062

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

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Identification of a series of highly potent activators of the Nurr1 signaling pathway.

Review 1. The role of histone acetylation in memory formation and cognitive impairments.

2. The nuclear receptor, Nor-1, markedly increases type II oxidative muscle fibers and resistance to fatigue.

3. Derivation of a retinoid X receptor scaffold from peroxisome proliferator-activated receptor gamma ligand 1-Di(1H-indol-3-yl)methyl-4-trifluoromethylbenzene.

Review 4. Structure-dependent activation of gene expression by bis-indole and quinoline-derived activators of nuclear receptor 4A2.

Review 5. NURR1 in Parkinson disease--from pathogenesis to therapeutic potential.

6. Low dose bexarotene treatment rescues dopamine neurons and restores behavioral function in models of Parkinson's disease.

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