NAAG peptidase inhibitors and their potential for diagnosis and therapy

Jia Zhou, Joseph H. Neale, Martin G. Pomper, Alan P. Kozikowski

Research output: Contribution to journalReview articlepeer-review

200 Scopus citations


Modulation of N-acetyl-L-aspartyl-L-glutamate peptidase activity with small-molecule inhibitors holds promise for a wide variety of diseases that involve glutamatergic transmission, and has implications for the diagnosis and therapy of cancer. This new class of compounds, of which at least one has entered clinical trials and proven to be well tolerated, has demonstrated efficacy in experimental models of pain, schizophrenia, amyotrophic lateral sclerosis, traumatic brain injury and, when appropriately functionalized, can image prostate cancer. Further investigation of these promising drug candidates will be needed to bring them to the marketplace. The recent publication of the X-ray crystal structure for the enzymatic target of these compounds should facilitate the development of other new agents with enhanced activity that could improve both the diagnosis and treatment of neurological disorders.

Original languageEnglish (US)
Pages (from-to)1015-1026
Number of pages12
JournalNature Reviews Drug Discovery
Issue number12
StatePublished - Dec 2005
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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