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貨期:
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用途:
For Research Use Only. Not for use in diagnostic or therapeutic procedures.
Demethylates proteins that have been reversibly carboxymethylated. Demethylates PPP2CB (in vitro) and PPP2CA. Binding to PPP2CA displaces the manganese ion and inactivates the enzyme.
基因功能參考文獻:
Authors found that PME-1 is exported from the nucleus to the cytoplasm upon H2O2 treatment and redistributes dem-p-PP2Ac in subcellular compartments. These findings offer new insight into the regulation of PME-1 localization and PP2A demethylation under oxidative stress. PMID: 30340029
We demonstrate that NNMT outcompetes leucine carboxyl methyl transferase 1 (LCMT1) for methyl transfer from principal methyl donor SAM in biological systems. Inhibiting NNMT increased the availability of methyl groups for LCMT1 to methylate PP2A, resulting in the inhibition of oncogenic serine/threonine kinases (STK). PMID: 27810903
Studies indicate that protein phosphatase methylesterase-1 (PME-1) negatively regulates protein phosphatase 2A (PP2A) activity by highly complex mechanisms. PMID: 27913678
Data suggest that discovery of more potent protein phosphatase methylesterase-1 (PME-1) inhibitors may be beneficial for the treatment of endometrial cancer. PMID: 27048286
LCMT1-PME-1 methylation equilibrium is critical for regulating mitotic spindle size and thereby proper cell division PMID: 25839665
PPME1 could be an attractive therapeutic target for a subset of gastric cancer and lung cancer. PMID: 24253382
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. PMID: 22443683
GSK-3beta can inhibit PP2A by increasing the inhibitory L309-demethylation involving upregulation of PME-1 and inhibition of PPMT1 PMID: 22732552
Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors. PMID: 21398589
We propose that stabilization of this inactive, nuclear PP2A pool is a major in vivo function of PME-1. PMID: 17803990
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. PMID: 19293187