1. Academic Validation
  2. Identification of a series of highly potent activators of the Nurr1 signaling pathway

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

  • Bioorg Med Chem Lett. 2007 Jan 1;17(1):193-6. doi: 10.1016/j.bmcl.2006.09.062.
Samuel Hintermann 1 Michele Chiesi Ulrike von Krosigk Danièle Mathé Richard Felber Bastian Hengerer
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, Neuroscience Research, CH-4002 Basel, Switzerland. samuel.hintermann@novartis.com
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.

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