Structurally Unique Inhibitors of Human Mitogen-Activated Protein Kinase Phosphatase-1 Identified in a Pyrrole Carboxamide Library

John S. Lazo; John Skoko; Stefan Werner; Branko Mitasev; Ahmet Bakan; Fumito Koizumi; Archibong Yellow-Duke; İvet Bahar; Kay M. Brummond

doi:10.1124/jpet.107.122242

Keywords

PhosphataseKinaseDual-specificity phosphataseProtein tyrosine phosphataseBiochemistryProtein kinase AMAPK/ERK pathwayChemistryMitogen-activated protein kinaseDocking (animal)Active siteEnzymeBiologyMedicine

Affiliated Institutions

Related Publications

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

Georgia Hatzivassiliou , Kyung Song , Ivana Yen +18 more

Activating mutations in KRAS and BRAF are found in more than 30% of all human tumours and 40% of melanoma, respectively, thus targeting this pathway could have broad therapeutic...

2010 Nature 1590 citations

Transcriptional Pathway Signatures Predict MEK Addiction and Response to Selumetinib (AZD6244)

Jonathan R. Dry , Sandra Pavey , Christine A. Pratilas +26 more

Abstract Selumetinib (AZD6244, ARRY-142886) is a selective, non–ATP-competitive inhibitor of mitogen-activated protein/extracellular signal–regulated kinase kinase (MEK)-1/2. Th...

2010 Cancer Research 259 citations

c-Src Is Required for Oxidative Stress-mediated Activation of Big Mitogen-activated Protein Kinase 1 (BMK1)

Jun‐ichi Abe , Masafumi Takahashi , Mari Ishida +2 more

Big mitogen-activated kinase 1 (BMK1) or extracellular signal-regulated kinase-5 (ERK5) has recently been identified as a new member of the mitogen-activated protein kinase fami...

1997 Journal of Biological Chemistry 272 citations

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

Poulikos I. Poulikakos , Chao Zhang , Gideon Bollag +2 more

Tumours with mutant BRAF are dependent on the RAF–MEK–ERK signalling pathway for their growth. We found that ATP-competitive RAF inhibitors inhibit ERK signalling in cells with ...

2010 Nature 1772 citations

A MAP Kinase Targeted by Endotoxin and Hyperosmolarity in Mammalian Cells

Jiahuai Han , Jeffrey Lee , L. Bibbs +1 more

Mammalian cells respond to endotoxic lipopolysaccharide (LPS) by activation of protein kinase cascades that lead to new gene expression. A protein kinase, p38, that was tyrosine...

1994 Science 2651 citations

Publication Info

Year: 2007
Type: article
Volume: 322
Issue: 3
Pages: 940-947
Citations: 24
Access: Closed

External Links

View on DOI.org

Social Impact

Altmetric

Structurally Unique Inhibitors of Human Mitogen-Activated Protein Kinase Phosphatase-1 Identified in a Pyrrole Carboxamide Library

PlumX Metrics

Social media, news, blog, policy document mentions

Citation Metrics

OpenAlex

Cite This

APA Style

                            
                                
                                    John S. Lazo, 
                                
                                    John Skoko, 
                                
                                    Stefan Werner
                                
                                et al.
                            
                            (2007). 
                            Structurally Unique Inhibitors of Human Mitogen-Activated Protein Kinase Phosphatase-1 Identified in a Pyrrole Carboxamide Library. 
                            Journal of Pharmacology and Experimental Therapeutics
                            , 322
                            (3)
                            , 940-947.
                            https://doi.org/10.1124/jpet.107.122242
                        

Identifiers

DOI: 10.1124/jpet.107.122242