Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease

Craig W. Lindsley, Colleen M. Niswender, Darren W. Engers, Corey R. Hopkins

Research output: Contribution to journalReview article

35 Citations (Scopus)

Abstract

This article describes recent advances in the development and biological evaluation of small molecule mGluR4 positive allosteric modulators (PAMs), and, to a lesser extent, orthosteric agonists. Due to its expression in the basal ganglia, the Family 3 GPCR metabotropic glutamate receptor subtype 4 (mGluR4) has recently garnered a great deal of attention as a putative target for the treatment of Parkinson's disease and a variety of other CNS disorders. Until 2008, with the exception of the prototypical mGluR4 PAM (-)-PHCCC, very few small molecule tools existed to probe the role of selective activation of mGluR4. This review will focus on the explosion of novel mGluR4 PAMs reported in the past year and the further preclinical validation of mGluR4 activation as a potentially groundbreaking treatment for Parkinson's disease.

Original languageEnglish (US)
Pages (from-to)949-963
Number of pages15
JournalCurrent Topics in Medicinal Chemistry
Volume9
Issue number10
DOIs
StatePublished - Dec 1 2009

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Parkinson Disease
Explosions
Basal Ganglia
metabotropic glutamate receptor 4

Keywords

  • Allosteric
  • Dopamine
  • Glutamate
  • Metabotropic
  • PHCCC
  • Parkinson's disease
  • Positive allosteric modulator
  • mGluR4

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease. / Lindsley, Craig W.; Niswender, Colleen M.; Engers, Darren W.; Hopkins, Corey R.

In: Current Topics in Medicinal Chemistry, Vol. 9, No. 10, 01.12.2009, p. 949-963.

Research output: Contribution to journalReview article

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