2. Academic Validation
  3. Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease

Development of a novel NURR1/NOT agonist from hit to lead and candidate for the potential treatment of Parkinson's disease

  • Bioorg Med Chem Lett. 2019 Apr 1;29(7):929-932. doi: 10.1016/j.bmcl.2019.01.024.
Dominique Lesuisse 1,  André Malanda 2,  Jean-François Peyronel 2,  Yannick Evanno 2,  Patrick Lardenois 2,  Danielle De-Peretti 2,  Pierre-Yves Abécassis 3,  Pascal Barnéoud 4,  Pascale Brunel 5,  Marie-Claude Burgevin 6,  Céline Cegarra 4,  Florian Auger 2,  Amélie Dommergue 2,  Corinne Lafon 7,  Luc Even 2,  Joanna Tsi 2,  Thy Phuong Hieu Luc 2,  Antonio Almario 2,  Anne Olivier 6,  Marie-Noëlle Castel 8,  Véronique Taupin 4,  Thomas Rooney 4,  Xavier Vigé 6
Affiliations

Affiliations

  • 1 Rare and Neurologic Disease Research, Sanofi, 1 av Pierre Brossolette, Chilly Mazarin F-91935, France. Electronic address: dominique.lesuisse@sanofi.com.
  • 2 Medicinal Chemistry, Sanofi, 1 av Pierre Brossolette, Chilly Mazarin F-91385, France.
  • 3 DMPK, Sanofi, 13 quai Jules Guesde, Vitry-sur-Seine F-94403, France.
  • 4 Rare and Neurologic Disease Research, Sanofi, 1 av Pierre Brossolette, Chilly Mazarin F-91935, France.
  • 5 Preclinical Safety, Sanofi, 3, digue d' Alfortville, Alfortville F-94140, France.
  • 6 Translational Science, Sanofi, 1 av Pierre Brossolette, Chilly Mazarin F-91385, France.
  • 7 CNS Department, Sanofi, 195 route d'Espagne, F-31036 Toulouse, France.
  • 8 CNS Department, 13, quai Jules Guesde, F-94403 Vitry-sur-Seine Cedex, France.
PMID: 30773432 DOI: 10.1016/j.bmcl.2019.01.024
Abstract

In the course of a programme aimed at identifying Nurr1/NOT agonists for potential treatment of Parkinson's disease, a few hits from high throughput screening were identified and characterized. A combined optimization pointed to a very narrow and stringent structure activity relationship. A comprehensive program of optimization led to a potent and safe candidate drug displaying neuroprotective and anti-inflammatory activity in several in vitro and in vivo models.

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