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Literature summary for 3.1.1.89 extracted from

  • Bachovchin, D.A.; Mohr, J.T.; Speers, A.E.; Wang, C.; Berlin, J.M.; Spicer, T.P.; Fernandez-Vega, V.; Chase, P.; Hodder, P.S.; Schuerer, S.C.; Nomura, D.K.; Rosen, H.; Fu, G.C.; Cravatt, B.F.
    Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors (2011), Proc. Natl. Acad. Sci. USA, 108, 6811-6816.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
dimethyl 3-cyclopentyl-4-oxo-3-phenylcyclobutane-1,2-dicarboxylate in both MDA-MB-231 and HEK-293T cells, highly potent and selective inhibition of the enzyme with IC50 values of 11.1 nM and 6.4 nM. Analysis reveals complete and selective in situ inhibition of PME-1 with no activity against more than 50 other serine hydrolases detected in MDA-MB-231 and HEK-293T cells. In both cell lines, inhibition results in significant reductions in the levels of demethylated PP2A Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
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Homo sapiens
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MDA-MB-231 cell
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Homo sapiens
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