PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 28159515-1 2017 Here we evaluate the potential for local administration of a small molecule FOLH1/GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) as a novel treatment for inflammatory bowel disease (IBD). 2-(phosphonomethyl)pentanedioic acid 98-133 folate hydrolase 1 Mus musculus 76-81 28159515-1 2017 Here we evaluate the potential for local administration of a small molecule FOLH1/GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) as a novel treatment for inflammatory bowel disease (IBD). 2-(phosphonomethyl)pentanedioic acid 98-133 folate hydrolase 1 Mus musculus 82-87 28159515-1 2017 Here we evaluate the potential for local administration of a small molecule FOLH1/GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) as a novel treatment for inflammatory bowel disease (IBD). 2-(phosphonomethyl)pentanedioic acid 135-141 folate hydrolase 1 Mus musculus 76-81 28159515-1 2017 Here we evaluate the potential for local administration of a small molecule FOLH1/GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) as a novel treatment for inflammatory bowel disease (IBD). 2-(phosphonomethyl)pentanedioic acid 135-141 folate hydrolase 1 Mus musculus 82-87 28159515-2 2017 We found that FOLH1/GCPII enzyme activity was increased in the colorectal tissues of mice with TNBS-induced colitis, and confirmed that 2-PMPA inhibited FOLH1/GCPII enzyme activity ex vivo. 2-(phosphonomethyl)pentanedioic acid 136-142 folate hydrolase 1 Mus musculus 14-19 28159515-2 2017 We found that FOLH1/GCPII enzyme activity was increased in the colorectal tissues of mice with TNBS-induced colitis, and confirmed that 2-PMPA inhibited FOLH1/GCPII enzyme activity ex vivo. 2-(phosphonomethyl)pentanedioic acid 136-142 folate hydrolase 1 Mus musculus 20-25 28159515-2 2017 We found that FOLH1/GCPII enzyme activity was increased in the colorectal tissues of mice with TNBS-induced colitis, and confirmed that 2-PMPA inhibited FOLH1/GCPII enzyme activity ex vivo. 2-(phosphonomethyl)pentanedioic acid 136-142 folate hydrolase 1 Mus musculus 153-158 28159515-2 2017 We found that FOLH1/GCPII enzyme activity was increased in the colorectal tissues of mice with TNBS-induced colitis, and confirmed that 2-PMPA inhibited FOLH1/GCPII enzyme activity ex vivo. 2-(phosphonomethyl)pentanedioic acid 136-142 folate hydrolase 1 Mus musculus 159-164 28285415-3 2017 mGluR2 and mGluR3 knock-out (ko) mice were used to test the hypothesis that mGluR3 mediates the activity of GCPII inhibitors ZJ43 and 2-PMPA in animal models of memory and memory loss. 2-(phosphonomethyl)pentanedioic acid 134-140 glutamate receptor, ionotropic, AMPA3 (alpha 3) Mus musculus 76-82 28763226-1 2017 2-(Phosphonomethyl)pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase-II (GCPII) with efficacy in multiple neurological and psychiatric disease models, but its clinical utility is hampered by low brain penetration due to the inclusion of multiple acidic functionalities. 2-(phosphonomethyl)pentanedioic acid 0-36 folate hydrolase 1 Rattus norvegicus 85-114 28763226-1 2017 2-(Phosphonomethyl)pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase-II (GCPII) with efficacy in multiple neurological and psychiatric disease models, but its clinical utility is hampered by low brain penetration due to the inclusion of multiple acidic functionalities. 2-(phosphonomethyl)pentanedioic acid 0-36 folate hydrolase 1 Rattus norvegicus 116-121 28763226-1 2017 2-(Phosphonomethyl)pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase-II (GCPII) with efficacy in multiple neurological and psychiatric disease models, but its clinical utility is hampered by low brain penetration due to the inclusion of multiple acidic functionalities. 2-(phosphonomethyl)pentanedioic acid 38-44 folate hydrolase 1 Rattus norvegicus 85-114 28763226-1 2017 2-(Phosphonomethyl)pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase-II (GCPII) with efficacy in multiple neurological and psychiatric disease models, but its clinical utility is hampered by low brain penetration due to the inclusion of multiple acidic functionalities. 2-(phosphonomethyl)pentanedioic acid 38-44 folate hydrolase 1 Rattus norvegicus 116-121 28285415-3 2017 mGluR2 and mGluR3 knock-out (ko) mice were used to test the hypothesis that mGluR3 mediates the activity of GCPII inhibitors ZJ43 and 2-PMPA in animal models of memory and memory loss. 2-(phosphonomethyl)pentanedioic acid 134-140 folate hydrolase 1 Mus musculus 108-113 28285415-5 2017 Treatment with ZJ43 or 2-PMPA prior to acquisition trials increased long-term memory in mGluR2, but not mGluR3, ko mice. 2-(phosphonomethyl)pentanedioic acid 23-29 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 88-94 28285415-8 2017 2-PMPA also moderated the effect of ethanol on short-term memory in mGluR2 ko mice but failed to do so in mGluR3 ko mice. 2-(phosphonomethyl)pentanedioic acid 0-6 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 68-74 28251297-0 2017 Glutamate carboxypeptidase II (GCPII) inhibitor 2-PMPA reduces rewarding effects of the synthetic cathinone MDPV in rats: a role for N-acetylaspartylglutamate (NAAG). 2-(phosphonomethyl)pentanedioic acid 48-54 folate hydrolase 1 Homo sapiens 0-29 28251297-0 2017 Glutamate carboxypeptidase II (GCPII) inhibitor 2-PMPA reduces rewarding effects of the synthetic cathinone MDPV in rats: a role for N-acetylaspartylglutamate (NAAG). 2-(phosphonomethyl)pentanedioic acid 48-54 folate hydrolase 1 Homo sapiens 31-36 28251297-15 2017 Systemic administration of the GCPII inhibitor 2-PMPA, or NAAG, attenuates MDPV reward. 2-(phosphonomethyl)pentanedioic acid 47-53 folate hydrolase 1 Homo sapiens 31-36 28326936-0 2017 A role for the locus coeruleus in the analgesic efficacy of N-acetylaspartylglutamate peptidase (GCPII) inhibitors ZJ43 and 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 124-130 folate hydrolase 1 Homo sapiens 97-102 28273495-8 2017 PC-3-derived tumors showed no obvious radioactive uptake; however, the LNCaP-derived tumors showed very high radioactive uptake which was significantly decreased by the selective PSMA inhibitor 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 194-200 keratin 6A Homo sapiens 0-4 28273495-8 2017 PC-3-derived tumors showed no obvious radioactive uptake; however, the LNCaP-derived tumors showed very high radioactive uptake which was significantly decreased by the selective PSMA inhibitor 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 194-200 folate hydrolase 1 Homo sapiens 179-183 27444540-5 2016 Intrigued by these results, we tried a potent GCPII inhibitor, 2-phosphonomethyl pentanedioic acid (2-PMPA), on EAE mice and noticed markedly attenuated EAE clinical signs along with significantly inhibited infiltration of inflammatory cells into CNS. 2-(phosphonomethyl)pentanedioic acid 63-98 folate hydrolase 1 Mus musculus 46-51 27444540-5 2016 Intrigued by these results, we tried a potent GCPII inhibitor, 2-phosphonomethyl pentanedioic acid (2-PMPA), on EAE mice and noticed markedly attenuated EAE clinical signs along with significantly inhibited infiltration of inflammatory cells into CNS. 2-(phosphonomethyl)pentanedioic acid 100-106 folate hydrolase 1 Mus musculus 46-51 27444540-6 2016 Furthermore, 2-PMPA dampened the function of Th1 cell lineage and down-regulated mGluR1 expression in both periphery and CNS contributing to glutamate-mediated immune regulation. 2-(phosphonomethyl)pentanedioic acid 13-19 glutamate receptor, metabotropic 1 Mus musculus 81-87 27288079-4 2016 Ironically his review was published months following the discovery of the first potent and selective GCPII inhibitor, 2-(phosphonomethyl)pentanedioc acid (2-PMPA) (Jackson et al., 1996). 2-(phosphonomethyl)pentanedioic acid 155-161 folate hydrolase 1 Homo sapiens 101-106 27536732-4 2016 Using a human-to-mouse approach, we next showed a similar enzymatic increase in two well-validated IBD murine models and evaluated the therapeutic effect of the potent FOLH1/ GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) (IC50 = 300 pM). 2-(phosphonomethyl)pentanedioic acid 191-226 folate hydrolase 1 Mus musculus 168-173 27536732-4 2016 Using a human-to-mouse approach, we next showed a similar enzymatic increase in two well-validated IBD murine models and evaluated the therapeutic effect of the potent FOLH1/ GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) (IC50 = 300 pM). 2-(phosphonomethyl)pentanedioic acid 191-226 folate hydrolase 1 Mus musculus 175-180 27536732-5 2016 In the dextran sodium sulfate (DSS) colitis model, 2-PMPA inhibited the GCPII activity in the colonic mucosa by over 90% and substantially reduced the disease activity. 2-(phosphonomethyl)pentanedioic acid 51-57 folate hydrolase 1 Homo sapiens 72-77 27536732-7 2016 In the murine IL-10-/- model of spontaneous colitis, daily 2-PMPA treatment also significantly reduced both macroscopic and microscopic disease severity. 2-(phosphonomethyl)pentanedioic acid 59-65 interleukin 10 Mus musculus 14-19 26930119-1 2016 2-Phosphonomethylpentanedioic acid (1, 2-PMPA) is a potent inhibitor of glutamate carboxypeptidase II which has demonstrated robust neuroprotective efficacy in many neurological disease models. 2-(phosphonomethyl)pentanedioic acid 0-34 folate hydrolase 1 Mus musculus 72-101 26930119-0 2016 Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA). 2-(phosphonomethyl)pentanedioic acid 94-128 folate hydrolase 1 Mus musculus 46-75 26930119-0 2016 Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA). 2-(phosphonomethyl)pentanedioic acid 94-128 folate hydrolase 1 Mus musculus 77-82 26930119-0 2016 Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA). 2-(phosphonomethyl)pentanedioic acid 130-136 folate hydrolase 1 Mus musculus 46-75 26930119-0 2016 Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2-Phosphonomethylpentanedioic Acid (2-PMPA). 2-(phosphonomethyl)pentanedioic acid 130-136 folate hydrolase 1 Mus musculus 77-82 26826008-4 2016 In the study described herein, the dose response of the GCPII inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) was evaluated for preventing cognitive impairment in EAE mice. 2-(phosphonomethyl)pentanedioic acid 72-108 folate hydrolase 1 Mus musculus 56-61 26826008-4 2016 In the study described herein, the dose response of the GCPII inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) was evaluated for preventing cognitive impairment in EAE mice. 2-(phosphonomethyl)pentanedioic acid 110-116 folate hydrolase 1 Mus musculus 56-61 26826008-11 2016 GCPII inhibition is a promising treatment for cognitive impairment in MS, and doses providing equivalent exposures to 100mg/kg 2-PMPA in mice should be evaluated in clinical studies for the prevention and/or treatment of MS-related cognitive impairment. 2-(phosphonomethyl)pentanedioic acid 127-133 folate hydrolase 1 Mus musculus 0-5 26151906-0 2015 Selective CNS Uptake of the GCP-II Inhibitor 2-PMPA following Intranasal Administration. 2-(phosphonomethyl)pentanedioic acid 45-51 folate hydrolase 1 Homo sapiens 28-34 26151906-20 2015 administration of 2-PMPA resulted in complete inhibition of brain GCP-II enzymatic activity ex-vivo confirming target engagement. 2-(phosphonomethyl)pentanedioic acid 18-24 folate hydrolase 1 Homo sapiens 66-72 23025786-0 2012 Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer. 2-(phosphonomethyl)pentanedioic acid 32-68 folate hydrolase 1 Homo sapiens 86-120 25613537-0 2015 PMPA for nephroprotection in PSMA-targeted radionuclide therapy of prostate cancer. 2-(phosphonomethyl)pentanedioic acid 0-4 folate hydrolase 1 Homo sapiens 29-33 25613537-3 2015 Because kidney kinetics differ from tumor kinetics, serial application of PSMA inhibitors such as 2-(phosphonomethyl)pentanedioic acid (PMPA) may improve the kidney-to-tumor ratio. 2-(phosphonomethyl)pentanedioic acid 98-134 folate hydrolase 1 Homo sapiens 74-78 25613537-3 2015 Because kidney kinetics differ from tumor kinetics, serial application of PSMA inhibitors such as 2-(phosphonomethyl)pentanedioic acid (PMPA) may improve the kidney-to-tumor ratio. 2-(phosphonomethyl)pentanedioic acid 136-140 folate hydrolase 1 Homo sapiens 74-78 25613537-4 2015 In this study, we evaluated the effect of PMPA on the biodistribution of 2 promising PSMA ligands. 2-(phosphonomethyl)pentanedioic acid 42-46 folate hydrolase 1 Homo sapiens 85-89 25613537-12 2015 PMPA doses of 0.2-1 mg/kg appear optimal for sustaining nearly complete tumor uptake while simultaneously achieving near-total blocking of specific renal PSMA binding. 2-(phosphonomethyl)pentanedioic acid 0-4 folate hydrolase 1 Homo sapiens 154-158 24055700-1 2014 2-Phosphonomethyl pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase-II, an enzyme which catabolizes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. 2-(phosphonomethyl)pentanedioic acid 0-35 folate hydrolase 1 Rattus norvegicus 84-113 24055700-1 2014 2-Phosphonomethyl pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase-II, an enzyme which catabolizes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. 2-(phosphonomethyl)pentanedioic acid 37-43 folate hydrolase 1 Rattus norvegicus 84-113 23891752-4 2013 Likewise, 2-PMPA (specific GCPII inhibitor developed targeting S1" pocket) completely blocked the NAAG hydrolysis without any effect on Abeta degradation. 2-(phosphonomethyl)pentanedioic acid 10-16 folate hydrolase 1 Homo sapiens 27-32 23733925-5 2013 (99m)Tc-labeled PSMA inhibitors did not bind human prostate cancer PC3 cells, which lack PSMA, demonstrating specificity, and binding was abolished with 2-(phosphonomethyl)pentanedioic acid (PMPA), a structurally unrelated PSMA inhibitor. 2-(phosphonomethyl)pentanedioic acid 191-195 folate hydrolase 1 Homo sapiens 16-20 23025786-0 2012 Radiofluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid as inhibitors of prostate specific membrane antigen (PSMA) for the imaging of prostate cancer. 2-(phosphonomethyl)pentanedioic acid 32-68 folate hydrolase 1 Homo sapiens 122-126 19895667-0 2010 Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism. 2-(phosphonomethyl)pentanedioic acid 27-33 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 85-91 20624932-7 2010 Moreover, treatment of 8-mo-old transgenic mice for 1 mo with 2-(phosphonomethyl)-pentanedioic acid (10 mg/kg, intraperitoneally), a specific GCPII inhibitor, increased cerebral Abeta content. 2-(phosphonomethyl)pentanedioic acid 62-99 folate hydrolase 1 Mus musculus 142-147 20624932-7 2010 Moreover, treatment of 8-mo-old transgenic mice for 1 mo with 2-(phosphonomethyl)-pentanedioic acid (10 mg/kg, intraperitoneally), a specific GCPII inhibitor, increased cerebral Abeta content. 2-(phosphonomethyl)pentanedioic acid 62-99 amyloid beta (A4) precursor protein Mus musculus 178-183 19830782-6 2010 RESULTS: Proliferation of PC-3-PSMA cells grown in the presence of poly-gamma-glutamated folate, was significantly higher than that of PC-3-vector cells, an advantage which was attenuated by the addition of 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 207-213 folate hydrolase 1 Homo sapiens 31-35 19887067-1 2010 We have recently reported that the endogenous mGlu2/3 agonist N-acetylaspartylglutamate (NAAG) and the N-acetylated-alpha-linked-acidic dipeptidase (NAALADase, a NAAG degradation enzyme) inhibitor 2-PMPA significantly inhibit cocaine self-administration and cocaine-induced reinstatement of drug-seeking behavior by attenuating cocaine-enhanced extracellular dopamine and glutamate in the nucleus accumbens. 2-(phosphonomethyl)pentanedioic acid 197-203 folate hydrolase 1 Rattus norvegicus 103-147 19887067-1 2010 We have recently reported that the endogenous mGlu2/3 agonist N-acetylaspartylglutamate (NAAG) and the N-acetylated-alpha-linked-acidic dipeptidase (NAALADase, a NAAG degradation enzyme) inhibitor 2-PMPA significantly inhibit cocaine self-administration and cocaine-induced reinstatement of drug-seeking behavior by attenuating cocaine-enhanced extracellular dopamine and glutamate in the nucleus accumbens. 2-(phosphonomethyl)pentanedioic acid 197-203 folate hydrolase 1 Rattus norvegicus 149-158 19895667-2 2010 In this study, we investigated whether elevation of the endogenous mGluR2/3 ligand N-acetyl-aspartatylglutamate (NAAG) levels by the N-acetylated-alpha-linked-acidic dipeptidase inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) attenuates cocaine self-administration and cocaine-induced reinstatement of drug seeking. 2-(phosphonomethyl)pentanedioic acid 188-224 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 67-73 19895667-2 2010 In this study, we investigated whether elevation of the endogenous mGluR2/3 ligand N-acetyl-aspartatylglutamate (NAAG) levels by the N-acetylated-alpha-linked-acidic dipeptidase inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) attenuates cocaine self-administration and cocaine-induced reinstatement of drug seeking. 2-(phosphonomethyl)pentanedioic acid 226-232 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 67-73 19895667-6 2010 Microinjections of 2-PMPA (3-5 microg/side) or NAAG (3-5 microg/side) into the nucleus accumbens (NAc), but not into the dorsal striatum, also inhibited cocaine-induced reinstatement, an effect that was blocked by intra-NAc injection of LY341495, a selective mGluR2/3 antagonist. 2-(phosphonomethyl)pentanedioic acid 19-25 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 259-265 19895667-11 2010 These findings suggest that 2-PMPA is effective in attenuating cocaine-induced reinstatement of drug-seeking behavior, likely by attenuating cocaine-induced increases in NAc DA and glutamate via pre-synaptic mGluR2/3s. 2-(phosphonomethyl)pentanedioic acid 28-34 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 208-214 18031726-1 2008 The purpose of the present study was to examine the effects of 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a selective inhibitor of N-acetylated-alpha-linked-acidic dipeptidase (NAALADase, glutamate carboxypeptidase II), an enzyme catalyzing the cleavage of glutamate from the neuropeptide N-acetyl-aspartyl-glutamate (NAAG), on memory processes in mice. 2-(phosphonomethyl)pentanedioic acid 63-100 folate hydrolase 1 Mus musculus 193-222 19706750-5 2009 The association of [(123)I]MIP-1072 and [(123)I]MIP-1095 with PSMA was specific; there was no binding to human prostate cancer PC3 cells, which lack PSMA, and binding was abolished by coincubation with a structurally unrelated NAALADase inhibitor, 2-(phosphonomethyl)pentanedioic acid (PMPA). 2-(phosphonomethyl)pentanedioic acid 248-284 folate hydrolase 1 Homo sapiens 62-66 19706750-5 2009 The association of [(123)I]MIP-1072 and [(123)I]MIP-1095 with PSMA was specific; there was no binding to human prostate cancer PC3 cells, which lack PSMA, and binding was abolished by coincubation with a structurally unrelated NAALADase inhibitor, 2-(phosphonomethyl)pentanedioic acid (PMPA). 2-(phosphonomethyl)pentanedioic acid 286-290 folate hydrolase 1 Homo sapiens 62-66 19706750-8 2009 Specific binding to PSMA in vivo was shown by competition with PMPA in LNCaP xenografts, and the absence of uptake in PC3 xenografts. 2-(phosphonomethyl)pentanedioic acid 63-67 folate hydrolase 1 Homo sapiens 20-24 17567119-2 2007 Herein, we report crystal structures of the human GCPII complexed with three glutamate mimetics/derivatives, 2-(phosphonomethyl)pentanedioic acid (2-PMPA), quisqualic acid (QA), and L-serine O-sulfate (L-SOS), at 1.72, 1.62, and 2.10 A resolution, respectively. 2-(phosphonomethyl)pentanedioic acid 109-145 folate hydrolase 1 Homo sapiens 50-55 17567119-2 2007 Herein, we report crystal structures of the human GCPII complexed with three glutamate mimetics/derivatives, 2-(phosphonomethyl)pentanedioic acid (2-PMPA), quisqualic acid (QA), and L-serine O-sulfate (L-SOS), at 1.72, 1.62, and 2.10 A resolution, respectively. 2-(phosphonomethyl)pentanedioic acid 147-153 folate hydrolase 1 Homo sapiens 50-55 17315070-2 2007 A series of novel enantiomerically pure 2-(phosphonomethyl)pentanedioic acid (2-PMPA) based NAALADase inhibitors were synthesized. 2-(phosphonomethyl)pentanedioic acid 40-76 folate hydrolase 1 Homo sapiens 92-101 17372356-0 2007 Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 123-129 folate hydrolase 1 Homo sapiens 6-35 17372356-0 2007 Human glutamate carboxypeptidase II inhibition: structures of GCPII in complex with two potent inhibitors, quisqualate and 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 123-129 folate hydrolase 1 Homo sapiens 62-67 17372356-3 2007 Crystal structures were determined of the extracellular part of GCPII (amino-acid residues 44-750) in complex with two potent inhibitors, quisqualate and 2-PMPA (the strongest GCPII inhibitor to date), at resolutions of 3.0 and 2.2 A, respectively. 2-(phosphonomethyl)pentanedioic acid 154-160 folate hydrolase 1 Homo sapiens 64-69 17372356-3 2007 Crystal structures were determined of the extracellular part of GCPII (amino-acid residues 44-750) in complex with two potent inhibitors, quisqualate and 2-PMPA (the strongest GCPII inhibitor to date), at resolutions of 3.0 and 2.2 A, respectively. 2-(phosphonomethyl)pentanedioic acid 154-160 folate hydrolase 1 Homo sapiens 176-181 17315070-2 2007 A series of novel enantiomerically pure 2-(phosphonomethyl)pentanedioic acid (2-PMPA) based NAALADase inhibitors were synthesized. 2-(phosphonomethyl)pentanedioic acid 78-84 folate hydrolase 1 Homo sapiens 92-101 16403497-0 2006 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. 2-(phosphonomethyl)pentanedioic acid 0-35 folate hydrolase 1 Mus musculus 37-66 16403497-1 2006 This study examined the effect of 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a potent and selective inhibitor of glutamate carboxypeptidase II (GCP II), an enzyme releasing glutamate and N-acetyl-aspartate from synaptical terminals, on the electroconvulsive threshold in mice. 2-(phosphonomethyl)pentanedioic acid 34-71 folate hydrolase 1 Mus musculus 118-147 16403497-1 2006 This study examined the effect of 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a potent and selective inhibitor of glutamate carboxypeptidase II (GCP II), an enzyme releasing glutamate and N-acetyl-aspartate from synaptical terminals, on the electroconvulsive threshold in mice. 2-(phosphonomethyl)pentanedioic acid 34-71 folate hydrolase 1 Mus musculus 149-155 16403497-1 2006 This study examined the effect of 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a potent and selective inhibitor of glutamate carboxypeptidase II (GCP II), an enzyme releasing glutamate and N-acetyl-aspartate from synaptical terminals, on the electroconvulsive threshold in mice. 2-(phosphonomethyl)pentanedioic acid 73-79 folate hydrolase 1 Mus musculus 118-147 16403497-1 2006 This study examined the effect of 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a potent and selective inhibitor of glutamate carboxypeptidase II (GCP II), an enzyme releasing glutamate and N-acetyl-aspartate from synaptical terminals, on the electroconvulsive threshold in mice. 2-(phosphonomethyl)pentanedioic acid 73-79 folate hydrolase 1 Mus musculus 149-155 16403497-15 2006 The reduction of glutamate neurotransmission in the brain, as a consequence of inhibition of GCP II activity by 2-PMPA, was however insufficient to enhance the anticonvulsant activity of conventional antiepileptic drugs, except for valproate, whose antiseizure action against maximal electroconvulsions was potentiated by 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 112-118 folate hydrolase 1 Mus musculus 93-99 15836619-4 2005 This was prevented by 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a GCPII inhibitor, suggesting that stimulation increased the hydrolysis of [3H]NAAG and metabolic recycling of [3H]glutamate. 2-(phosphonomethyl)pentanedioic acid 22-59 folate hydrolase 1 Homo sapiens 72-77 16220328-1 2005 RATIONALE AND OBJECTIVES: We have recently reported that conditioned morphine reward and tolerance to its antinociceptive effect, but not expression of morphine dependence, were attenuated by 2-(phosphonomethyl)pentanedioic acid (2-PMPA), a prototypic inhibitor of glutamate carboxipeptidase II (GCP II), which is an enzyme responsible for the supply of glutamate. 2-(phosphonomethyl)pentanedioic acid 192-228 folate hydrolase 1 Mus musculus 265-294 16220328-1 2005 RATIONALE AND OBJECTIVES: We have recently reported that conditioned morphine reward and tolerance to its antinociceptive effect, but not expression of morphine dependence, were attenuated by 2-(phosphonomethyl)pentanedioic acid (2-PMPA), a prototypic inhibitor of glutamate carboxipeptidase II (GCP II), which is an enzyme responsible for the supply of glutamate. 2-(phosphonomethyl)pentanedioic acid 192-228 folate hydrolase 1 Mus musculus 296-302 15953368-4 2005 The reduction of the H-effect by NAAG was completely removed when N-acetyl-beta-aspartylglutamate (betaNAAG) or 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) was used to inhibit glutamate carboxypeptidase II (GCP II), a presynaptic Schwann cell membrane-associated ectoenzyme that hydrolyzes NAAG to glutamate and N-acetylaspartate. 2-(phosphonomethyl)pentanedioic acid 151-157 folate hydrolase 1 Rattus norvegicus 179-208 15953368-4 2005 The reduction of the H-effect by NAAG was completely removed when N-acetyl-beta-aspartylglutamate (betaNAAG) or 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) was used to inhibit glutamate carboxypeptidase II (GCP II), a presynaptic Schwann cell membrane-associated ectoenzyme that hydrolyzes NAAG to glutamate and N-acetylaspartate. 2-(phosphonomethyl)pentanedioic acid 151-157 folate hydrolase 1 Rattus norvegicus 210-216 15836619-4 2005 This was prevented by 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a GCPII inhibitor, suggesting that stimulation increased the hydrolysis of [3H]NAAG and metabolic recycling of [3H]glutamate. 2-(phosphonomethyl)pentanedioic acid 61-67 folate hydrolase 1 Homo sapiens 72-77 15968081-5 2005 In this study we used the competitive NAAG peptidase inhibitor 2-(phosphonomethyl) pentanedioic acid (2-PMPA) as a probe to interrupt the NAAG-mGluR3- Glu-astrocyte Ca2+ activation sequence. 2-(phosphonomethyl)pentanedioic acid 63-100 glutamate receptor, ionotropic, AMPA3 (alpha 3) Mus musculus 143-149 15968081-5 2005 In this study we used the competitive NAAG peptidase inhibitor 2-(phosphonomethyl) pentanedioic acid (2-PMPA) as a probe to interrupt the NAAG-mGluR3- Glu-astrocyte Ca2+ activation sequence. 2-(phosphonomethyl)pentanedioic acid 102-108 glutamate receptor, ionotropic, AMPA3 (alpha 3) Mus musculus 143-149 15019832-6 2004 Next, we treated rat adipocytes with 2-[phosphonomethy]pentanedionic acid (2-PMPA), a potent NAALADase inhibitor, and studied its effect on the distribution of GLUT4 and 3-O-methyl glucose (3OMG) flux. 2-(phosphonomethyl)pentanedioic acid 75-81 folate hydrolase 1 Rattus norvegicus 93-102 15019832-7 2004 In 2-PMPA-treated adipocytes, there was a significant reduction (by 40%) in the insulin-stimulated GLUT4 translocation to the plasma membrane. 2-(phosphonomethyl)pentanedioic acid 3-9 solute carrier family 2 member 4 Rattus norvegicus 99-104 15019832-8 2004 The 3OMG flux in insulin-stimulated adipocytes was also delayed (51% of control) by 2-PMPA treatment, indicating that 2-PMPA impairs insulin-stimulated GLUT4 recruitment and the uptake of glucose. 2-(phosphonomethyl)pentanedioic acid 84-90 solute carrier family 2 member 4 Rattus norvegicus 152-157 15019832-8 2004 The 3OMG flux in insulin-stimulated adipocytes was also delayed (51% of control) by 2-PMPA treatment, indicating that 2-PMPA impairs insulin-stimulated GLUT4 recruitment and the uptake of glucose. 2-(phosphonomethyl)pentanedioic acid 118-124 solute carrier family 2 member 4 Rattus norvegicus 152-157 14607107-2 2003 It is hydrolysed by glutamate carboxypeptidase II (GCPII); thus, the GCP-II inhibitor 2-[phosphono-methyl]-pentanedioic acid (2-PMPA) protects endogenous NAAG from degradation, allowing its effects to be studied in vivo. 2-(phosphonomethyl)pentanedioic acid 86-124 folate hydrolase 1 Rattus norvegicus 20-49 15030392-2 2004 In the current study, we have determined that the GCP II inhibitor 2-(phosphonomethyl) pentanedioic acid (2-PMPA) is protective against glucose-induced programmed cell death (PCD) and neurite degeneration in dorsal root ganglion (DRG) neurons in a cell culture model of diabetic neuropathy. 2-(phosphonomethyl)pentanedioic acid 67-104 folate hydrolase 1 Homo sapiens 50-56 15030392-2 2004 In the current study, we have determined that the GCP II inhibitor 2-(phosphonomethyl) pentanedioic acid (2-PMPA) is protective against glucose-induced programmed cell death (PCD) and neurite degeneration in dorsal root ganglion (DRG) neurons in a cell culture model of diabetic neuropathy. 2-(phosphonomethyl)pentanedioic acid 106-112 folate hydrolase 1 Homo sapiens 50-56 15030392-4 2004 2-PMPA neuroprotection is completely reversed by the mGluR3 antagonist (S)-alpha-ethylglutamic acid (EGLU). 2-(phosphonomethyl)pentanedioic acid 0-6 glutamate receptor, ionotropic, AMPA3 (alpha 3) Mus musculus 53-59 15030392-6 2004 Furthermore, we show that two mGluR3 agonists, the direct agonist (2R,4R)-4-aminopyrrolidine-2, 4-dicarboxylate (APDC) and N-acetyl-aspartyl-glutamate (NAAG) provide protection to neurons exposed to high glucose conditions, consistent with the concept that 2-PMPA neuroprotection is mediated by increased NAAG activity. 2-(phosphonomethyl)pentanedioic acid 257-263 glutamate receptor, ionotropic, AMPA3 (alpha 3) Mus musculus 30-36 14607107-2 2003 It is hydrolysed by glutamate carboxypeptidase II (GCPII); thus, the GCP-II inhibitor 2-[phosphono-methyl]-pentanedioic acid (2-PMPA) protects endogenous NAAG from degradation, allowing its effects to be studied in vivo. 2-(phosphonomethyl)pentanedioic acid 86-124 folate hydrolase 1 Rattus norvegicus 51-56 14607107-2 2003 It is hydrolysed by glutamate carboxypeptidase II (GCPII); thus, the GCP-II inhibitor 2-[phosphono-methyl]-pentanedioic acid (2-PMPA) protects endogenous NAAG from degradation, allowing its effects to be studied in vivo. 2-(phosphonomethyl)pentanedioic acid 86-124 folate hydrolase 1 Rattus norvegicus 69-75 14607107-2 2003 It is hydrolysed by glutamate carboxypeptidase II (GCPII); thus, the GCP-II inhibitor 2-[phosphono-methyl]-pentanedioic acid (2-PMPA) protects endogenous NAAG from degradation, allowing its effects to be studied in vivo. 2-(phosphonomethyl)pentanedioic acid 126-132 folate hydrolase 1 Rattus norvegicus 20-49 14607107-2 2003 It is hydrolysed by glutamate carboxypeptidase II (GCPII); thus, the GCP-II inhibitor 2-[phosphono-methyl]-pentanedioic acid (2-PMPA) protects endogenous NAAG from degradation, allowing its effects to be studied in vivo. 2-(phosphonomethyl)pentanedioic acid 126-132 folate hydrolase 1 Rattus norvegicus 51-56 14607107-2 2003 It is hydrolysed by glutamate carboxypeptidase II (GCPII); thus, the GCP-II inhibitor 2-[phosphono-methyl]-pentanedioic acid (2-PMPA) protects endogenous NAAG from degradation, allowing its effects to be studied in vivo. 2-(phosphonomethyl)pentanedioic acid 126-132 folate hydrolase 1 Rattus norvegicus 69-75 14607107-7 2003 NAAG is an agonist at the inhibitory metabotropic glutamate receptor mGluR3, and 2-PMPA may inhibit nociceptive transmission in normal animals by elevating synaptic NAAG levels, allowing it to activate mGluR3 and thus reducing transmitter release from afferent nerve terminals. 2-(phosphonomethyl)pentanedioic acid 81-87 glutamate receptor, ionotropic, AMPA3 (alpha 3) Mus musculus 202-208 12826236-5 2003 The potent NAALADase inhibitor, 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), was tested in an in vitro model of chronic glutamate-mediated motor neuron degeneration. 2-(phosphonomethyl)pentanedioic acid 32-69 folate hydrolase 1B (pseudogene) Homo sapiens 11-20 12826236-5 2003 The potent NAALADase inhibitor, 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), was tested in an in vitro model of chronic glutamate-mediated motor neuron degeneration. 2-(phosphonomethyl)pentanedioic acid 71-77 folate hydrolase 1B (pseudogene) Homo sapiens 11-20 12629525-0 2003 Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 164-170 folate hydrolase 1 Mus musculus 103-132 12629525-0 2003 Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 164-170 folate hydrolase 1 Mus musculus 134-140 12629525-2 2003 The aim of this study was to investigate effects of GCP II inhibition with the selective inhibitor, 2-PMPA, on: (a) development of tolerance to the antinociceptive effects, (b) withdrawal, and (c) conditioned reward produced by morphine in C57/Bl mice. 2-(phosphonomethyl)pentanedioic acid 100-106 folate hydrolase 1 Mus musculus 52-58 12213057-8 2002 On the basis of the GCPII model, the structures of GCPII in complex with its potent inhibitors 2-(phosphonomethyl)pentanedioic acid (PMPA) and 4,4"-phosphinicobis(butane-1,3-dicarboxylic acid) (PBDA) were built by a computational docking method. 2-(phosphonomethyl)pentanedioic acid 95-131 folate hydrolase 1 Homo sapiens 51-56 12413472-9 2002 Inhibition studies with the GCPII inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) demonstrated competitive inhibition with a K(i)=0.2nM. 2-(phosphonomethyl)pentanedioic acid 44-80 folate hydrolase 1 Homo sapiens 28-33 12413472-9 2002 Inhibition studies with the GCPII inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) demonstrated competitive inhibition with a K(i)=0.2nM. 2-(phosphonomethyl)pentanedioic acid 82-88 folate hydrolase 1 Homo sapiens 28-33 12358725-13 2002 The IC50 value for 2-PMPA was about 1 nm for wild-type brain membrane NAAG peptidase activity consistent with its activity against cloned ratand human GCPII, and 88 nm for the activity in brain membranes of the null mutants. 2-(phosphonomethyl)pentanedioic acid 19-25 folate hydrolase 1 Homo sapiens 151-156 12213057-8 2002 On the basis of the GCPII model, the structures of GCPII in complex with its potent inhibitors 2-(phosphonomethyl)pentanedioic acid (PMPA) and 4,4"-phosphinicobis(butane-1,3-dicarboxylic acid) (PBDA) were built by a computational docking method. 2-(phosphonomethyl)pentanedioic acid 133-137 folate hydrolase 1 Homo sapiens 51-56 11698060-5 2001 To verify this, Enzyme-Linked Immunosorbent Assays (ELISAs) were performed on media from both control and ischemic cultures treated with the GCP II inhibitor, 2-(phosphonomethyl)-pentanedioic acid (2-PMPA). 2-(phosphonomethyl)pentanedioic acid 159-196 folate hydrolase 1 Homo sapiens 141-147 12920850-8 2002 Blockade with unlabeled MCG or 2-(phosphonomethyl)pentanedioic acid (PMPA), another potent inhibitor of GCP II, provided sevenfold and threefold reductions, respectively, in binding to target tissue. 2-(phosphonomethyl)pentanedioic acid 31-67 folate hydrolase 1 Mus musculus 104-110 12920850-8 2002 Blockade with unlabeled MCG or 2-(phosphonomethyl)pentanedioic acid (PMPA), another potent inhibitor of GCP II, provided sevenfold and threefold reductions, respectively, in binding to target tissue. 2-(phosphonomethyl)pentanedioic acid 69-73 folate hydrolase 1 Mus musculus 104-110 11805230-5 2002 In the present study, we determined the effect of a GCP II inhibitor, 2-(phosphono-methyl)-pentanedioic acid (2-PMPA), on allodynia and ectopic afferent discharges in an animal model of neuropathic pain. 2-(phosphonomethyl)pentanedioic acid 70-108 folate hydrolase 1 Rattus norvegicus 52-58 11805230-5 2002 In the present study, we determined the effect of a GCP II inhibitor, 2-(phosphono-methyl)-pentanedioic acid (2-PMPA), on allodynia and ectopic afferent discharges in an animal model of neuropathic pain. 2-(phosphonomethyl)pentanedioic acid 110-116 folate hydrolase 1 Rattus norvegicus 52-58 11698060-6 2001 We found that 2-PMPA attenuated ischemia-induced declines in TGF-beta. 2-(phosphonomethyl)pentanedioic acid 14-20 transforming growth factor beta 1 Homo sapiens 61-69 11698060-8 2001 In both in vitro and in vivo models of cerebral ischemia, TGF-beta Ab reversed the neuroprotection by 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 102-108 transforming growth factor beta 1 Homo sapiens 58-66 11525768-2 2001 Previously, NAAG and 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a potent and selective NAALADase inhibitor, were found to be neuroprotective in neuronal/glial co-cultures and in animals following transient middle cerebral artery occlusion. 2-(phosphonomethyl)pentanedioic acid 21-58 folate hydrolase 1 Homo sapiens 92-101 11557259-0 2001 Binding of the glutamate carboxypeptidase II (NAALADase) inhibitor 2-PMPA to rat brain membranes. 2-(phosphonomethyl)pentanedioic acid 67-73 folate hydrolase 1 Rattus norvegicus 15-44 11557259-1 2001 2-Phosphonomethyl pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase II (NAALADase), and has shown robust neuroprotective activity in both in vitro and in vivo models of ischemia. 2-(phosphonomethyl)pentanedioic acid 0-35 folate hydrolase 1 Rattus norvegicus 84-113 11557259-1 2001 2-Phosphonomethyl pentanedioic acid (2-PMPA) is a potent and selective inhibitor of glutamate carboxypeptidase II (NAALADase), and has shown robust neuroprotective activity in both in vitro and in vivo models of ischemia. 2-(phosphonomethyl)pentanedioic acid 37-43 folate hydrolase 1 Rattus norvegicus 84-113 11557259-9 2001 The binding of [(3)H]2-PMPA also showed tissue specificity in that tissues previously reported to be devoid of GCPII enzymatic activity were devoid of [(3)H]2-PMPA binding. 2-(phosphonomethyl)pentanedioic acid 21-27 folate hydrolase 1 Rattus norvegicus 111-116 11557259-10 2001 [(3)H]2-PMPA binding represents an additional probe for the study of GCPII activity, and may be useful as a high throughput screening assay. 2-(phosphonomethyl)pentanedioic acid 6-12 folate hydrolase 1 Rattus norvegicus 69-74 11525768-2 2001 Previously, NAAG and 2-(phosphonomethyl)-pentanedioic acid (2-PMPA), a potent and selective NAALADase inhibitor, were found to be neuroprotective in neuronal/glial co-cultures and in animals following transient middle cerebral artery occlusion. 2-(phosphonomethyl)pentanedioic acid 60-66 folate hydrolase 1 Homo sapiens 92-101 10940354-0 2000 Neuroprotection produced by the NAALADase inhibitor 2-PMPA in rat cerebellar neurons. 2-(phosphonomethyl)pentanedioic acid 52-58 folate hydrolase 1 Rattus norvegicus 32-41 11720792-8 2001 There was a beta-NAAG-, quisqualate- and 2-(phosphonomethyl)-pentanedioic acid-inhibitable glutamate carboxypeptidase II activity in the membrane fraction of central nerve fibers, but not in axonal or glial cytoplasmic fractions. 2-(phosphonomethyl)pentanedioic acid 41-78 folate hydrolase 1 Homo sapiens 91-120 11166133-4 2001 Recently, a specific inhibitor of N-acetylated-alpha-linked acidic dipeptidase, 2-(phosphonomethyl)pentanedioic acid, has been reported. 2-(phosphonomethyl)pentanedioic acid 80-116 folate hydrolase 1 Rattus norvegicus 34-78 20575858-4 2000 Recently, a potent and selective NAALADase inhibitor termed 2-(phosphonomethyl)pentanedioic acid (2-PMPA) was identified that has a 300 pM Ki for NAALADase inhibition. 2-(phosphonomethyl)pentanedioic acid 60-96 folate hydrolase 1 Rattus norvegicus 33-42 20575858-4 2000 Recently, a potent and selective NAALADase inhibitor termed 2-(phosphonomethyl)pentanedioic acid (2-PMPA) was identified that has a 300 pM Ki for NAALADase inhibition. 2-(phosphonomethyl)pentanedioic acid 60-96 folate hydrolase 1 Rattus norvegicus 146-155 20575858-4 2000 Recently, a potent and selective NAALADase inhibitor termed 2-(phosphonomethyl)pentanedioic acid (2-PMPA) was identified that has a 300 pM Ki for NAALADase inhibition. 2-(phosphonomethyl)pentanedioic acid 98-104 folate hydrolase 1 Rattus norvegicus 33-42 20575858-4 2000 Recently, a potent and selective NAALADase inhibitor termed 2-(phosphonomethyl)pentanedioic acid (2-PMPA) was identified that has a 300 pM Ki for NAALADase inhibition. 2-(phosphonomethyl)pentanedioic acid 98-104 folate hydrolase 1 Rattus norvegicus 146-155 10940354-1 2000 The present study examined the neuroprotective actions of the N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) in four in vitro models of neurotoxicity. 2-(phosphonomethyl)pentanedioic acid 129-165 folate hydrolase 1 Rattus norvegicus 62-106 10940354-1 2000 The present study examined the neuroprotective actions of the N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) in four in vitro models of neurotoxicity. 2-(phosphonomethyl)pentanedioic acid 129-165 folate hydrolase 1 Rattus norvegicus 108-117 10940354-1 2000 The present study examined the neuroprotective actions of the N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) in four in vitro models of neurotoxicity. 2-(phosphonomethyl)pentanedioic acid 167-173 folate hydrolase 1 Rattus norvegicus 62-106 10940354-1 2000 The present study examined the neuroprotective actions of the N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) in four in vitro models of neurotoxicity. 2-(phosphonomethyl)pentanedioic acid 167-173 folate hydrolase 1 Rattus norvegicus 108-117 10940354-6 2000 Unlike 2-PMPA, the endogenous NAALADase substrate and mGlu(3) receptor agonist N-acetyl-aspartyl-glutamate (NAAG) was neuroprotective against all four injury mechanisms and compared to 2-PMPA, exhibited a different "phosphate effect" on neuroprotection. 2-(phosphonomethyl)pentanedioic acid 185-191 folate hydrolase 1 Rattus norvegicus 30-39 10528109-5 1999 We report that, at high concentrations (300 microM-30 mM), a folic acid hexaglutamate analog is dose-dependently toxic to dissociated rat cortical cultures and that this toxicity is reversed by 2-PMPA, a potent and selective NAALADase inhibitor. 2-(phosphonomethyl)pentanedioic acid 194-200 folate hydrolase 1 Rattus norvegicus 225-234 10581082-2 1999 We demonstrate that the newly described NAALADase inhibitor 2-PMPA (2-(phosphonomethyl)pentanedioic acid) robustly protects against ischemic injury in a neuronal culture model of stroke and in rats after transient middle cerebral artery occlusion. 2-(phosphonomethyl)pentanedioic acid 60-66 folate hydrolase 1 Rattus norvegicus 40-49 10581082-2 1999 We demonstrate that the newly described NAALADase inhibitor 2-PMPA (2-(phosphonomethyl)pentanedioic acid) robustly protects against ischemic injury in a neuronal culture model of stroke and in rats after transient middle cerebral artery occlusion. 2-(phosphonomethyl)pentanedioic acid 68-104 folate hydrolase 1 Rattus norvegicus 40-49 10581082-3 1999 Consistent with inhibition of NAALADase, we show that 2-PMPA increases NAAG and attenuates the ischemia-induced rise in glutamate. 2-(phosphonomethyl)pentanedioic acid 54-60 folate hydrolase 1 Rattus norvegicus 30-39 9622670-5 1998 Addition of GCP II inhibitors beta-NAAG, quisqualic acid and 2-(phosphonomethyl)pentanedioic acid (PMPA) inhibited hydrolysis of 2.5 nM NAAG with IC50s of 201 nM, 155 nM and 98 pM, respectively. 2-(phosphonomethyl)pentanedioic acid 61-97 golgin B1 Homo sapiens 12-15 10668445-3 1999 Using the suture model of transient middle cerebral artery occlusion (MCAO) in rats, the prototype NAALADase inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) dramatically reduced extracellular glutamate accumulation measured by microdialysis both during a 2-hour occlusion and during reperfusion, consistent with an effect on glutamate supply. 2-(phosphonomethyl)pentanedioic acid 119-155 folate hydrolase 1 Rattus norvegicus 99-108 10668445-3 1999 Using the suture model of transient middle cerebral artery occlusion (MCAO) in rats, the prototype NAALADase inhibitor 2-(phosphonomethyl)pentanedioic acid (2-PMPA) dramatically reduced extracellular glutamate accumulation measured by microdialysis both during a 2-hour occlusion and during reperfusion, consistent with an effect on glutamate supply. 2-(phosphonomethyl)pentanedioic acid 157-163 folate hydrolase 1 Rattus norvegicus 99-108 9622670-5 1998 Addition of GCP II inhibitors beta-NAAG, quisqualic acid and 2-(phosphonomethyl)pentanedioic acid (PMPA) inhibited hydrolysis of 2.5 nM NAAG with IC50s of 201 nM, 155 nM and 98 pM, respectively. 2-(phosphonomethyl)pentanedioic acid 99-103 golgin B1 Homo sapiens 12-15 34976589-4 2022 Although several GCPII inhibitors, such as 2-PMPA, elevate brain NAAG levels and restore cognitive function in preclinical studies when given at high systemic doses or via direct brain injection, none are clinically available due to poor bioavailability and limited brain penetration. 2-(phosphonomethyl)pentanedioic acid 43-49 folate hydrolase 1 Mus musculus 17-22 35396969-12 2022 The uptake of Al18F-PSMA-Q in 22Rv1 cells and tumors can be substantially blocked by 2-PMPA. 2-(phosphonomethyl)pentanedioic acid 85-91 folate hydrolase 1 Homo sapiens 20-24 33748101-11 2021 Moreover, U87 or U251 conditioned medium could upregulated PSMA expression and induce similar effects on phenotypes of HUVECs, all of which could be partially attenuated by 2-PMPA treatment. 2-(phosphonomethyl)pentanedioic acid 173-179 small nucleolar RNA, C/D box 87 Homo sapiens 10-13 34984651-5 2022 2-(Phosphonomethyl)pentanedioic acid (2PMPA) is a potent GCPII inhibitor which robustly blocks glutamate release from NAAG but is highly polar with limited tissue penetration. 2-(phosphonomethyl)pentanedioic acid 0-36 folate hydrolase 1 Homo sapiens 57-62 34984651-5 2022 2-(Phosphonomethyl)pentanedioic acid (2PMPA) is a potent GCPII inhibitor which robustly blocks glutamate release from NAAG but is highly polar with limited tissue penetration. 2-(phosphonomethyl)pentanedioic acid 38-43 folate hydrolase 1 Homo sapiens 57-62 34984651-7 2022 Systemic D-2PMPA therapy (20 mg/kg 2PMPA equivalent; IP 2 x /week) was found to localize in muscle macrophages in SOD1G93A mice and completely normalize the enhanced GCPII activity. 2-(phosphonomethyl)pentanedioic acid 35-40 folate hydrolase 1 Mus musculus 166-171 33748101-11 2021 Moreover, U87 or U251 conditioned medium could upregulated PSMA expression and induce similar effects on phenotypes of HUVECs, all of which could be partially attenuated by 2-PMPA treatment. 2-(phosphonomethyl)pentanedioic acid 173-179 folate hydrolase 1 Homo sapiens 59-63 34014547-6 2021 For example, 2-(phosphonomethyl) pentanedioic acid (2-PMPA), one of the glutamate carboxypeptidase II (GCP II) inhibitors that prevent the conversion of NAAG to glutamate, has been shown to suppress cancer growth [6, 7]. 2-(phosphonomethyl)pentanedioic acid 52-58 folate hydrolase 1 Homo sapiens 72-101 33434438-9 2021 In the PSMA blocking study using 2-phosphonomethoxypropyl adenine (2-PMPA), the 64Cu-PSMA I&T signal significantly decreased in the 22RV1 tumor region. 2-(phosphonomethyl)pentanedioic acid 67-73 folate hydrolase 1 Homo sapiens 7-11 33434438-9 2021 In the PSMA blocking study using 2-phosphonomethoxypropyl adenine (2-PMPA), the 64Cu-PSMA I&T signal significantly decreased in the 22RV1 tumor region. 2-(phosphonomethyl)pentanedioic acid 67-73 folate hydrolase 1 Homo sapiens 85-89 34014547-6 2021 For example, 2-(phosphonomethyl) pentanedioic acid (2-PMPA), one of the glutamate carboxypeptidase II (GCP II) inhibitors that prevent the conversion of NAAG to glutamate, has been shown to suppress cancer growth [6, 7]. 2-(phosphonomethyl)pentanedioic acid 52-58 folate hydrolase 1 Homo sapiens 103-109 31503493-1 2019 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) is a potent (IC50=300 pM) and selective inhibitor of glutamate carboxypeptidase II (GCPII) with efficacy in multiple neurological and psychiatric disease preclinical models, and more recently in models of inflammatory bowel disease (IBD) and cancer. 2-(phosphonomethyl)pentanedioic acid 0-37 folate hydrolase 1 Mus musculus 100-129 33092792-4 2020 Here, we showed that 2-phosphonomethylpentanedioic acid (2-PMPA), a potent inhibitor of the distant M28 family member glutamate carboxypeptidase II (GCPII), rather than the typical M14 inhibitor 2-benzylsuccinic acid, could efficiently inhibit CCP activities. 2-(phosphonomethyl)pentanedioic acid 21-55 folate hydrolase 1 Homo sapiens 118-147 33092792-4 2020 Here, we showed that 2-phosphonomethylpentanedioic acid (2-PMPA), a potent inhibitor of the distant M28 family member glutamate carboxypeptidase II (GCPII), rather than the typical M14 inhibitor 2-benzylsuccinic acid, could efficiently inhibit CCP activities. 2-(phosphonomethyl)pentanedioic acid 21-55 folate hydrolase 1 Homo sapiens 149-154 33092792-4 2020 Here, we showed that 2-phosphonomethylpentanedioic acid (2-PMPA), a potent inhibitor of the distant M28 family member glutamate carboxypeptidase II (GCPII), rather than the typical M14 inhibitor 2-benzylsuccinic acid, could efficiently inhibit CCP activities. 2-(phosphonomethyl)pentanedioic acid 57-63 folate hydrolase 1 Homo sapiens 118-147 33092792-4 2020 Here, we showed that 2-phosphonomethylpentanedioic acid (2-PMPA), a potent inhibitor of the distant M28 family member glutamate carboxypeptidase II (GCPII), rather than the typical M14 inhibitor 2-benzylsuccinic acid, could efficiently inhibit CCP activities. 2-(phosphonomethyl)pentanedioic acid 57-63 folate hydrolase 1 Homo sapiens 149-154 33092792-5 2020 2-PMPA inhibited the recombinant Nna1 (a.k.a. 2-(phosphonomethyl)pentanedioic acid 0-6 ATP/GTP binding carboxypeptidase 1 Homo sapiens 33-37 33092792-8 2020 Homology modeling predicted that the R-form of 2-PMPA is more favorable to bind Nna1, unlike that GCPII prefers to S-form. 2-(phosphonomethyl)pentanedioic acid 47-53 ATP/GTP binding carboxypeptidase 1 Homo sapiens 80-84 32383887-3 2020 The aim of this study was to investigate the option of using fast-cleared, small-molecular-weight PSMA inhibitors (PSMA-11, 2-PMPA, and ZJ-43) to reduce the kidney uptake of [177Lu]Lu-PSMA-ALB-56, a previously developed albumin-binding PSMA radioligand. 2-(phosphonomethyl)pentanedioic acid 124-130 albumin Mus musculus 220-227 31503493-1 2019 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) is a potent (IC50=300 pM) and selective inhibitor of glutamate carboxypeptidase II (GCPII) with efficacy in multiple neurological and psychiatric disease preclinical models, and more recently in models of inflammatory bowel disease (IBD) and cancer. 2-(phosphonomethyl)pentanedioic acid 0-37 folate hydrolase 1 Mus musculus 131-136 31503493-1 2019 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) is a potent (IC50=300 pM) and selective inhibitor of glutamate carboxypeptidase II (GCPII) with efficacy in multiple neurological and psychiatric disease preclinical models, and more recently in models of inflammatory bowel disease (IBD) and cancer. 2-(phosphonomethyl)pentanedioic acid 39-45 folate hydrolase 1 Mus musculus 100-129 31503493-1 2019 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) is a potent (IC50=300 pM) and selective inhibitor of glutamate carboxypeptidase II (GCPII) with efficacy in multiple neurological and psychiatric disease preclinical models, and more recently in models of inflammatory bowel disease (IBD) and cancer. 2-(phosphonomethyl)pentanedioic acid 39-45 folate hydrolase 1 Mus musculus 131-136 30237214-8 2019 Dynamic PET imaging confirmed PSMA-specific (as demonstrated by coinjection of 2-PMPA) uptake into the LNCaP xenograft (4.5% +- 1.8 percentage injected dose per gram) and the kidneys (106% +- 23 percentage injected dose per gram). 2-(phosphonomethyl)pentanedioic acid 79-85 folate hydrolase 1 Homo sapiens 30-34 29580851-4 2018 An in vitro binding assay revealed that 800CW-SCE, 680LT-SCE, and 750-SCE exhibited higher binding affinity than 2-PMPA, which is known as a PSMA inhibitor. 2-(phosphonomethyl)pentanedioic acid 113-119 folate hydrolase 1 Homo sapiens 141-145 29853810-12 2018 Tumor uptake (% ID/cm3) of 68Ga-PSMA-11 based on functional volume correlated well with the PSMA expression in a linear manner (y = 9.35x + 2.59, R2 = 0.8924, and p < 0.0001); however, low dose 2-PMPA causes rapid renal clearance of increased tumor/kidney uptake of 68Ga-PSMA-11. 2-(phosphonomethyl)pentanedioic acid 198-204 folate hydrolase 1 Homo sapiens 33-37 29853810-12 2018 Tumor uptake (% ID/cm3) of 68Ga-PSMA-11 based on functional volume correlated well with the PSMA expression in a linear manner (y = 9.35x + 2.59, R2 = 0.8924, and p < 0.0001); however, low dose 2-PMPA causes rapid renal clearance of increased tumor/kidney uptake of 68Ga-PSMA-11. 2-(phosphonomethyl)pentanedioic acid 198-204 folate hydrolase 1 Homo sapiens 93-97 29853810-12 2018 Tumor uptake (% ID/cm3) of 68Ga-PSMA-11 based on functional volume correlated well with the PSMA expression in a linear manner (y = 9.35x + 2.59, R2 = 0.8924, and p < 0.0001); however, low dose 2-PMPA causes rapid renal clearance of increased tumor/kidney uptake of 68Ga-PSMA-11. 2-(phosphonomethyl)pentanedioic acid 198-204 folate hydrolase 1 Homo sapiens 93-97 29853810-14 2018 Low dose 2-PMPA preadministration might be a choice to decrease kidney uptake of 68Ga-PSMA-11. 2-(phosphonomethyl)pentanedioic acid 9-15 folate hydrolase 1 Homo sapiens 87-91 29680672-5 2018 PMPA (2-(phosphonomethyl)-pentanedioic acid), a specific inhibitor of PSMA, blocked the uptake of FTL into LNCaP cells, but did not affect the uptake of FTL into PSMA-deficient and folate receptor-positive KB cells. 2-(phosphonomethyl)pentanedioic acid 0-4 folate hydrolase 1 Homo sapiens 70-74 29680672-5 2018 PMPA (2-(phosphonomethyl)-pentanedioic acid), a specific inhibitor of PSMA, blocked the uptake of FTL into LNCaP cells, but did not affect the uptake of FTL into PSMA-deficient and folate receptor-positive KB cells. 2-(phosphonomethyl)pentanedioic acid 6-43 folate hydrolase 1 Homo sapiens 70-74