INT99336

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Context Info
Confidence 0.57
First Reported 2001
Last Reported 2010
Negated 0
Speculated 0
Reported most in Abstract
Documents 30
Total Number 32
Disease Relevance 8.83
Pain Relevance 11.53

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

peptidase activity (FOLH1) plasma membrane (FOLH1) nucleus (FOLH1)
cytoplasm (FOLH1)
Anatomy Link Frequency
nerve 1
brain 1
dorsal horn 1
FOLH1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Glutamate 108 100.00 Very High Very High Very High
Neuropathic pain 22 99.92 Very High Very High Very High
Potency 17 99.84 Very High Very High Very High
Analgesic 56 99.80 Very High Very High Very High
neuralgia 3 99.78 Very High Very High Very High
nociceptor 1 99.78 Very High Very High Very High
Pain 47 99.56 Very High Very High Very High
Dorsal horn 3 99.32 Very High Very High Very High
Dorsal horn neuron 1 99.08 Very High Very High Very High
Pain management 4 98.72 Very High Very High Very High
Disease Link Frequency Relevance Heat
Neuropathic Pain 29 99.92 Very High Very High Very High
Diabetes Mellitus 9 99.56 Very High Very High Very High
Stroke 10 99.08 Very High Very High Very High
Frailty 1 99.04 Very High Very High Very High
Stress 93 98.88 Very High Very High Very High
Pain 23 98.72 Very High Very High Very High
INFLAMMATION 5 98.24 Very High Very High Very High
Hypersensitivity 4 98.16 Very High Very High Very High
Carcinoma 12 98.08 Very High Very High Very High
Neurodegenerative Disease 3 97.84 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
These data suggest that NAALADase inhibition may provide a new approach for the treatment of both neurodegenerative disorders and peripheral neuropathies.
Negative_regulation (inhibition) of NAALADase associated with peripheral neuropathy and neurodegenerative disease
1) Confidence 0.57 Published 2001 Journal J. Med. Chem. Section Abstract Doc Link 11708918 Disease Relevance 0.57 Pain Relevance 0.14
Glutamate carboxypeptidase II (NAALADase) inhibition as a novel therapeutic strategy.
Negative_regulation (inhibition) of NAALADase associated with glutamate
2) Confidence 0.57 Published 2006 Journal Adv. Exp. Med. Biol. Section Title Doc Link 16802724 Disease Relevance 0.18 Pain Relevance 0.57
Enantiospecificity of glutamate carboxypeptidase II inhibition.
Negative_regulation (inhibition) of glutamate carboxypeptidase II associated with glutamate and analgesic
3) Confidence 0.55 Published 2005 Journal J. Med. Chem. Section Title Doc Link 15801825 Disease Relevance 0 Pain Relevance 0.66
Recently, we reported that certain urea-based structures act as potent inhibitors of GCPII (J.
Negative_regulation (inhibitors) of GCPII
4) Confidence 0.50 Published 2004 Journal J. Med. Chem. Section Abstract Doc Link 15027864 Disease Relevance 0.16 Pain Relevance 0.34
These urea-based inhibitors of GCPII thus offer a novel approach to pain management.
Negative_regulation (inhibitors) of GCPII associated with pain management
5) Confidence 0.50 Published 2004 Journal J. Med. Chem. Section Abstract Doc Link 15027864 Disease Relevance 0.37 Pain Relevance 0.79
Interestingly, even at relatively high doses of compounds, GCP II inhibition did not appear to be associated with learning/memory deficits in animals.
Negative_regulation (inhibition) of GCP II
6) Confidence 0.50 Published 2006 Journal Adv. Exp. Med. Biol. Section Abstract Doc Link 16802724 Disease Relevance 0.22 Pain Relevance 0.46
GCP II inhibition may represent a novel glutamate regulating strategy devoid of the side effects that have hampered the development of postsynaptic glutamate receptor antagonists.
Negative_regulation (inhibition) of GCP II associated with glutamate, antagonist and glutamate receptor
7) Confidence 0.50 Published 2006 Journal Adv. Exp. Med. Biol. Section Abstract Doc Link 16802724 Disease Relevance 0.22 Pain Relevance 0.45
Additionally, quantitative neurophysiological testing data and visual analog scales for 'psychedelic effects' in Phase I single dose and repeat dose studies showed GCP II inhibition to be safe and well tolerated by both healthy volunteers and diabetic patients.
Negative_regulation (inhibition) of GCP II associated with diabetes mellitus
8) Confidence 0.50 Published 2006 Journal Adv. Exp. Med. Biol. Section Abstract Doc Link 16802724 Disease Relevance 0.22 Pain Relevance 0.45
Glutamate carboxypeptidase II (NAALADase) inhibition as a novel therapeutic strategy.
Negative_regulation (inhibition) of carboxypeptidase II associated with glutamate
9) Confidence 0.44 Published 2006 Journal Adv. Exp. Med. Biol. Section Title Doc Link 16802724 Disease Relevance 0.18 Pain Relevance 0.57
In the Group A, the greater improvement between T0 and T1 has been reported on PSM items loss of control, irritability, psycho-physiological sensations, confusion, anxiety, depression, physical pain, hyperactivity and agitation (table 1 and figure 1, 2).


Negative_regulation (loss) of PSM associated with pain, depression, anxiety disorder, attention deficit hyperactivity disorder and confusion
10) Confidence 0.43 Published 2010 Journal Health Qual Life Outcomes Section Body Doc Link PMC2850330 Disease Relevance 0.56 Pain Relevance 0.14
The pharmacophore subpocket is very sensitive to structural changes, and thus, it appears important to keep one of the glutamic acid moieties intact to maintain the potency of the GCPII inhibitors.
Negative_regulation (inhibitors) of GCPII associated with potency
11) Confidence 0.43 Published 2004 Journal J. Med. Chem. Section Abstract Doc Link 15027864 Disease Relevance 0.25 Pain Relevance 0.46
A novel series of phosphinic acid based inhibitors of the neuropeptidase NAALADase are described in this work.
Negative_regulation (inhibitors) of NAALADase
12) Confidence 0.42 Published 2001 Journal J. Med. Chem. Section Abstract Doc Link 11708918 Disease Relevance 0.28 Pain Relevance 0.10
Design and pharmacological activity of phosphinic acid based NAALADase inhibitors.
Negative_regulation (inhibitors) of NAALADase
13) Confidence 0.42 Published 2001 Journal J. Med. Chem. Section Title Doc Link 11708918 Disease Relevance 0.33 Pain Relevance 0.12
The expression of PSMA is down-regulated by androgen, after androgen deprivation therapy, its expression is strongly elevated[6,26-28], Thus, PSMA is a potential target for the immunotherapy to carcinoma of prostate.
Negative_regulation (deprivation) of PSMA associated with carcinoma
14) Confidence 0.42 Published 2004 Journal J Transl Med Section Body Doc Link PMC517950 Disease Relevance 1.22 Pain Relevance 0
In contrast, both enantiomers of 3 inhibited GCP II with nearly equal potency.
Negative_regulation (inhibited) of GCP II associated with potency
15) Confidence 0.40 Published 2005 Journal J. Med. Chem. Section Abstract Doc Link 15801825 Disease Relevance 0 Pain Relevance 0.17
Two representative glutamate carboxypeptidase II (GCP II) inhibitors, 2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid 2 and 2-(3-mercaptopropyl)pentanedioic acid 3, were synthesized in high optical purities (>97%ee).
Negative_regulation (inhibitors) of glutamate carboxypeptidase II associated with glutamate
16) Confidence 0.40 Published 2005 Journal J. Med. Chem. Section Abstract Doc Link 15801825 Disease Relevance 0 Pain Relevance 0.09
Two representative glutamate carboxypeptidase II (GCP II) inhibitors, 2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid 2 and 2-(3-mercaptopropyl)pentanedioic acid 3, were synthesized in high optical purities (>97%ee).
Negative_regulation (inhibitors) of GCP II associated with glutamate
17) Confidence 0.40 Published 2005 Journal J. Med. Chem. Section Abstract Doc Link 15801825 Disease Relevance 0 Pain Relevance 0.09
In the group treated with REAC, the psychometric evaluation after the therapy's cycle showed a significant reduction of PSM total scores, from 107.8 ± 23,13 at T0 to 87.1 ± 16,21 at T1 (p < 0.5), while in the control group no significant variation in decreasing stress-related symptomatology has been noted (107.86 ± 25,80 at T0 and 106.32 ± 25,88 at T1 (p = NS).


Negative_regulation (reduction) of PSM associated with stress
18) Confidence 0.38 Published 2010 Journal Health Qual Life Outcomes Section Abstract Doc Link PMC2850330 Disease Relevance 0.54 Pain Relevance 0.06
The protocol of the auricular treatment with REAC seems to reduce the subjective perception of stress, as "psychometrically" demonstrated by the significant reduction in PSM test total score.
Negative_regulation (reduction) of PSM associated with stress
19) Confidence 0.38 Published 2010 Journal Health Qual Life Outcomes Section Abstract Doc Link PMC2850330 Disease Relevance 0.54 Pain Relevance 0.09
Inhibition of brain GCPII may have therapeutic potential in the treatment of certain disease states arising from pathologically overactivated glutamate receptors.
Negative_regulation (Inhibition) of GCPII in brain associated with glutamate receptor and disease
20) Confidence 0.37 Published 2004 Journal J. Med. Chem. Section Abstract Doc Link 15027864 Disease Relevance 0.10 Pain Relevance 0.29

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