2-(phosphonomethyl)pentanedioic acid






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1 9622670 Hydrolysis of the neuropeptide N-acetylaspartylglutamate (NAAG) by cloned human glutamate carboxypeptidase II. Brain Res 1998 Jun 8 2
2 10528109 Toxicity induced by a polyglutamated folate analog is attenuated by NAALADase inhibition. Brain Res 1999 Oct 2 1
3 10581082 Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury. Nat Med 1999 Dec 3
4 10668445 Blockade of NAALADase: a novel neuroprotective strategy based on limiting glutamate and elevating NAAG. Ann N Y Acad Sci 1999 2
5 10940354 Neuroprotection produced by the NAALADase inhibitor 2-PMPA in rat cerebellar neurons. Eur J Pharmacol 2000 Aug 18 6
6 11166133 Inhibition of spinal N-acetylated-alpha-linked acidic dipeptidase produces an antinociceptive effect in the rat formalin test. Neuroscience 2001 1
7 11525768 Neuroprotection afforded by NAAG and NAALADase inhibition requires glial cells and metabotropic glutamate receptor activation. Eur J Pharmacol 2001 Aug 24 2
8 11557259 Binding of the glutamate carboxypeptidase II (NAALADase) inhibitor 2-PMPA to rat brain membranes. Eur J Pharmacol 2001 Sep 14 5
9 11698060 Neuroprotection mediated by glutamate carboxypeptidase II (NAALADase) inhibition requires TGF-beta. Eur J Pharmacol 2001 Oct 26 3
10 11720792 Mechanisms for clearance of released N-acetylaspartylglutamate in crayfish nerve fibers: implications for axon-glia signaling. Neuroscience 2001 1
11 11805230 Effect of 2-(phosphono-methyl)-pentanedioic acid on allodynia and afferent ectopic discharges in a rat model of neuropathic pain. J Pharmacol Exp Ther 2002 Feb 2
12 12213057 Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors. J Med Chem 2002 Sep 12 2
13 12358725 Deletion of the glutamate carboxypeptidase II gene in mice reveals a second enzyme activity that hydrolyzes N-acetylaspartylglutamate. J Neurochem 2002 Oct 1
14 12413472 Kinetics and inhibition of glutamate carboxypeptidase II using a microplate assay. Anal Biochem 2002 Nov 1 2
15 12629525 Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA. Neuropsychopharmacology 2003 Mar 3
16 12826236 NAALADase inhibition protects motor neurons against chronic glutamate toxicity. Eur J Pharmacol 2003 Jun 27 2
17 12920850 11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase). Mol Imaging 2002 Apr-Jun 2
18 14607107 Effects of GCP-II inhibition on responses of dorsal horn neurones after inflammation and neuropathy: an electrophysiological study in the rat. Neuropeptides 2003 Oct 7
19 15019832 N-Acetylated alpha-linked acidic dipeptidase expressed in rat adipocytes is localized in the insulin-responsive glucose transporter (GLUT4) intracellular compartments and involved in the insulin-stimulated GLUT4 recruitment. Arch Biochem Biophys 2004 Apr 1 4
20 15030392 Protection against glucose-induced neuronal death by NAAG and GCP II inhibition is regulated by mGluR3. J Neurochem 2004 Apr 4
21 15836619 Regulation of glutamate carboxypeptidase II hydrolysis of N-acetylaspartylglutamate (NAAG) in crayfish nervous tissue is mediated by glial glutamate and acetylcholine receptors. J Neurochem 2005 May 2
22 15953368 Effect of N-acetylaspartylglutamate (NAAG) on non-quantal and spontaneous quantal release of acetylcholine at the neuromuscular synapse of rat. J Neurochem 2005 Jul 2
23 15968081 2-PMPA, a NAAG peptidase inhibitor, attenuates magnetic resonance BOLD signals in brain of anesthetized mice: evidence of a link between neuron NAAG release and hyperemia. J Mol Neurosci 2005 2
24 16220328 2-MPPA, a selective glutamate carboxypeptidase II inhibitor, attenuates morphine tolerance but not dependence in C57/Bl mice. Psychopharmacology (Berl) 2005 Dec 2
25 16403497 2-phosphonomethyl-pentanedioic acid (glutamate carboxypeptidase II inhibitor) increases threshold for electroconvulsions and enhances the antiseizure action of valproate against maximal electroshock-induced seizures in mice. Eur J Pharmacol 2006 Feb 15 6
26 17315070 Design, synthesis and pharmacological activity of novel enantiomerically pure phosphonic acid-based NAALADase inhibitors. Org Biomol Chem 2007 Mar 7 2
27 17372356 Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA. Acta Crystallogr D Biol Crystallogr 2007 Apr 4
28 17567119 Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II. J Med Chem 2007 Jul 12 2
29 18031726 Effects of selective inhibition of N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) on mice in learning and memory tasks. Eur J Pharmacol 2008 Jan 28 1
30 19706750 Preclinical evaluation of novel glutamate-urea-lysine analogues that target prostate-specific membrane antigen as molecular imaging pharmaceuticals for prostate cancer. Cancer Res 2009 Sep 1 3
31 19830782 Expression of prostate-specific membrane antigen (PSMA), increases cell folate uptake and proliferation and suggests a novel role for PSMA in the uptake of the non-polyglutamated folate, folic acid. Prostate 2010 Feb 15 1
32 19887067 Oral administration of the NAALADase inhibitor GPI-5693 attenuates cocaine-induced reinstatement of drug-seeking behavior in rats. Eur J Pharmacol 2010 Feb 10 2
33 19895667 Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism. J Neurochem 2010 Jan 5
34 20575858 NAALADase inhibition reduces alcohol consumption in the alcohol-preferring (P) line of rats. Addict Biol 2000 Oct 1 4
35 20624932 Glutamate carboxypeptidase II: an amyloid peptide-degrading enzyme with physiological function in the brain. FASEB J 2010 Nov 2
36 23025786 Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer. J Med Chem 2012 Nov 26 2
37 23733925 99mTc-labeled small-molecule inhibitors of prostate-specific membrane antigen for molecular imaging of prostate cancer. J Nucl Med 2013 Aug 1
38 23891752 S1 pocket of glutamate carboxypeptidase II: a new binding site for amyloid-β degradation. Biochem Biophys Res Commun 2013 Sep 6 1
39 24055700 Bioanalytical method for evaluating the pharmacokinetics of the GCP-II inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA). J Pharm Biomed Anal 2014 Jan 2
40 25613537 PMPA for nephroprotection in PSMA-targeted radionuclide therapy of prostate cancer. J Nucl Med 2015 Feb 5
41 26151906 Selective CNS Uptake of the GCP-II Inhibitor 2-PMPA following Intranasal Administration. PLoS One 2015 2
42 26826008 Dose-dependent inhibition of GCPII to prevent and treat cognitive impairment in the EAE model of multiple sclerosis. Brain Res 2016 Mar 15 3
43 26930119 Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA). J Med Chem 2016 Mar 24 5
44 27288079 Still NAAG'ing After All These Years: The Continuing Pursuit of GCPII Inhibitors. Adv Pharmacol 2016 1
45 27444540 Blocking glutamate carboxypeptidase II inhibits glutamate excitotoxicity and regulates immune responses in experimental autoimmune encephalomyelitis. FEBS J 2016 Sep 3
46 27536732 <i>FOLH1</i>/GCPII is elevated in IBD patients, and its inhibition ameliorates murine IBD abnormalities. JCI Insight 2016 Aug 4 4
47 28159515 Local enema treatment to inhibit FOLH1/GCPII as a novel therapy for inflammatory bowel disease. J Control Release 2017 Oct 10 8
48 28251297 Glutamate carboxypeptidase II (GCPII) inhibitor 2-PMPA reduces rewarding effects of the synthetic cathinone MDPV in rats: a role for N-acetylaspartylglutamate (NAAG). Psychopharmacology (Berl) 2017 Jun 3
49 28273495 <sup>99m</sup>Tc-labeling and evaluation of a HYNIC modified small-molecular inhibitor of prostate-specific membrane antigen. Nucl Med Biol 2017 May 2
50 28285415 NAAG Peptidase Inhibitors Act via mGluR3: Animal Models of Memory, Alzheimer's, and Ethanol Intoxication. Neurochem Res 2017 Sep 4