Title : Probe Report for PME-1 Inhibitors - Bachovchin_2010_Probe.Report__2 |
Author(s) : Bachovchin DA , Speers AE , Zuhl AM , Brown SJ , Cravatt BF , Fernandez V , Spicer T , Mercer BA , Ferguson J , Hodder P , Rosen HR |
Ref : Probe Report , : , 2010 |
Abstract :
Recent findings have identified protein phosphatase methylesterase-1 (PME-1) as a protector of sustained ERK pathway activity in malignant gliomas. PME-1 is a protein methylesterase that functions in the regulation of protein phosphatase 2A (PP2A) by reversible methylation. Biochemical elucidation of PME-1 would thus greatly benefit from the development of potent and selective chemical inhibitors. The probe compound ML136 (CID-44607965), containing a sulfonyl acrylonitrile core, represents the first potent, selective inhibitor of PME-1. Moreover, the probe does not appear to exhibit cytotoxicity. Thus, ML136 should serve as a useful tool for in vitro and in situ research assays in which it is desirable to specifically block PME-1 activity. |
PubMedSearch : Bachovchin_2010_Probe.Report__2 |
PubMedID: 21433379 |
Bachovchin DA, Speers AE, Zuhl AM, Brown SJ, Cravatt BF, Fernandez V, Spicer T, Mercer BA, Ferguson J, Hodder P, Rosen HR (2010)
Probe Report for PME-1 Inhibitors
Probe Report
:
Bachovchin DA, Speers AE, Zuhl AM, Brown SJ, Cravatt BF, Fernandez V, Spicer T, Mercer BA, Ferguson J, Hodder P, Rosen HR (2010)
Probe Report
: