title: Progress in the discovery and development of glutamate carboxypeptidase II inhibitors.
abstract: During the past 10 years, substantial progress has been made in the discovery and development of small molecule glutamate carboxypeptidase II (GCP II) inhibitors. These inhibitors have provided the necessary tools to investigate the physiological role of GCP II as well as the potential therapeutic benefits of its inhibition in neurological disorders of glutamatergic dysregulation. This review article details key GCP II inhibitors discovered in the last decade and important findings from preclinical and clinical studies.
authors.affiliation: MGI Pharma, Inc., 6611 Tributary Street, Baltimore, MD 21224, USA. takashi.tsukamoto@mgipharma.com
authors.forename: Takashi
authors.initials: T
authors.lastname: Tsukamoto
authors.forename: Krystyna M
authors.initials: KM
authors.lastname: Wozniak
authors.forename: Barbara S
authors.initials: BS
authors.lastname: Slusher
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use; D015195:Drug Design; D043425:Glutamate Carboxypeptidase II / Q000037:antagonists & inhibitors* / Q000737:chemistry; D005977:Glutarates / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000737:chemistry / Q000627:therapeutic use; D009943:Organophosphorus Compounds / Q000737:chemistry / Q000627:therapeutic use; D010721:Phosphinic Acids / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000627:therapeutic use