TY - JOUR
T1 - NAAG peptidase inhibitors and their potential for diagnosis and therapy
AU - Zhou, Jia
AU - Neale, Joseph H.
AU - Pomper, Martin G.
AU - Kozikowski, Alan P.
PY - 2005/12/1
Y1 - 2005/12/1
N2 - 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.
AB - 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.
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U2 - 10.1038/nrd1903
DO - 10.1038/nrd1903
M3 - Review article
C2 - 16341066
AN - SCOPUS:33644700192
VL - 4
SP - 1015
EP - 1026
JO - Nature Reviews Drug Discovery
JF - Nature Reviews Drug Discovery
SN - 1474-1776
IS - 12
ER -