Property Summary

NCBI Gene PubMed Count 16
Grant Count 12
R01 Count 7
Funding $475,360.88
PubMed Score 33.25
PubTator Score 17.53

Knowledge Summary

Patent

No data available

Expression

  Differential Expression (7)

Disease log2 FC p
malignant mesothelioma 2.200 0.000
osteosarcoma -1.148 0.001
intraductal papillary-mucinous neoplasm ... 1.400 0.001
lung cancer 1.300 0.001
diabetes mellitus -1.100 0.005
lung carcinoma 1.400 0.000
ovarian cancer 1.600 0.000

MLP Assay (14)

AID Type Active / Inconclusive / Inactive Description
2130 screening 1683 / 0 / 313418 Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).
2171 screening 1068 / 0 / 446 Fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).
2291 screening 73 / 0 / 15927 Fluorescence polarization-based Maybridge primary biochemical high throughput screening assay to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).
2363 screening 2 / 0 / 0 Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Inhibition of PME-1-mediated demethylation of PP2a
2368 screening 2 / 0 / 0 Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) Gel Filtration Assay
2369 screening 5 / 0 / 18 Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) Inhibition
2371 confirmatory 0 / 0 / 6 Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) IC50: Purified enzyme
463090 other 1 / 0 / 0 Late stage assay provider results from the probe development effort to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1): LC-MS/MS assay to assess binding of compounds to active site
463124 confirmatory 1 / 0 / 0 Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Gel-based Activity-Based Protein Profiling (ABPP) IC50 Set 2
463130 confirmatory 4 / 0 / 1 Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Gel-based Activity-Based Protein Profiling (ABPP) IC50 Set 1
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Gene RIF (8)

PMID Text
25839665 LCMT1-PME-1 methylation equilibrium is critical for regulating mitotic spindle size and thereby proper cell division
24841198 this study suggests that the tightly linked regulatory loop comprised of the SIK2-PP2A and CaMKI and PME-1 networks may function in fine-tuning cell proliferation and stress response.
24253382 PPME1 could be an attractive therapeutic target for a subset of gastric cancer and lung cancer.
22732552 GSK-3beta can inhibit PP2A by increasing the inhibitory L309-demethylation involving upregulation of PME-1 and inhibition of PPMT1
22443683 Data indicate that PP2A holoenzyme biogenesis and activity are controlled by five PP2A modulators, consisting of alpha4, PTPA, LCMT1, PME-1 and TIPRL1, which serve to prevent promiscuous phosphatase activity until the holoenzyme is completely assembled.
21398589 Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors.
19293187 Observations identify PME-1 expression as one mechanism by which ERK pathway activity is maintained in cancer cells and suggest an important functional role for PME-1 in the disease progression of human astrocytic gliomas.
17803990 We propose that stabilization of this inactive, nuclear PP2A pool is a major in vivo function of PME-1.

AA Sequence

MSALEKSMHLGRLPSRPPLPGSGGSQSGAKMRMGPGRKRDFSPVPWSQYFESMEDVEVENETGKDTFRVY      1 - 70
KSGSEGPVLLLLHGGGHSALSWAVFTAAIISRVQCRIVALDLRSHGETKVKNPEDLSAETMAKDVGNVVE     71 - 140
AMYGDLPPPIMLIGHSMGGAIAVHTASSNLVPSLLGLCMIDVVEGTAMDALNSMQNFLRGRPKTFKSLEN    141 - 210
AIEWSVKSGQIRNLESARVSMVGQVKQCEGITSPEGSKSIVEGIIEEEEEDEEGSESISKRKKEDDMETK    211 - 280
KDHPYTWRIELAKTEKYWDGWFRGLSNLFLSCPIPKLLLLAGVDRLDKDLTIGQMQGKFQMQVLPQCGHA    281 - 350
VHEDAPDKVAEAVATFLIRHRFAEPIGGFQCVFPGC                                      351 - 386
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Publication (27)

PMID Year Title
25839665 2015 A LCMT1-PME-1 methylation equilibrium controls mitotic spindle size.
25468996 2014 E-cadherin interactome complexity and robustness resolved by quantitative proteomics.
24841198 2014 Interaction between salt-inducible kinase 2 and protein phosphatase 2A regulates the activity of calcium/calmodulin-dependent protein kinase I and protein phosphatase methylesterase-1.
24275569 2014 An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome.
24253382 2014 Genetic amplification of PPME1 in gastric and lung cancer and its potential as a novel therapeutic target.
24129315 2014 Immunoaffinity enrichment and mass spectrometry analysis of protein methylation.
23186163 2013 Toward a comprehensive characterization of a human cancer cell phosphoproteome.
22732552 2012 Glycogen synthase kinase-3? regulates leucine-309 demethylation of protein phosphatase-2A via PPMT1 and PME-1.
22443683 2013 The biogenesis of active protein phosphatase 2A holoenzymes: a tightly regulated process creating phosphatase specificity.
21406692 2011 System-wide temporal characterization of the proteome and phosphoproteome of human embryonic stem cell differentiation.
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