RGD Reference Report - Evidence for estrogenic contamination of the MAPK inhibitor PD98059. - Rat Genome Database

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Evidence for estrogenic contamination of the MAPK inhibitor PD98059.

Authors: Long, X  Gize, EA  Nephew, K  Bigsby, RM 
Citation: Long X, etal., Endocrinology 2001 Dec;142(12):5390-3.
RGD ID: 727330
Pubmed: PMID:11713241   (View Abstract at PubMed)
DOI: DOI:10.1210/endo.142.12.8649   (Journal Full-text)

PD98059 blocks phosphorylation and activation of MAPK proteins, ERK1 and ERK2. In the course of examining the effect of PD98059 on estrogen-induced transcription of reporter genes in a human breast cancer cell line and in yeast, we found that two of four different batches of PD98059 produced estrogenic effects in a dose-dependent manner. In a competitive binding assay, these preparations of PD98059 displaced radiolabeled estradiol from ER alpha. Furthermore, in the yeast assay, addition of a coactivator protein, AIB1, enhanced the transcriptional effect of PD98059, indicating that it induces receptor-coactivator interactions. Although concentrations of PD98059 required to activate ER alpha in these experimental systems are 10(4)- to 10(5) higher than the concentration of estradiol required to do the same, the concentrations required to block MAPK activation are well above those which would produce maximal estrogenic effects. Thus, when PD98059 is used in estrogen-responsive cells, contaminating estrogenic activity may confound interpretation of experimental results.



Gene Ontology Annotations    Click to see Annotation Detail View

Biological Process

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
Ncoa3Ratpositive regulation of DNA-binding transcription factor activity  IDA  RGD 
Ncoa3Ratpositive regulation of intracellular estrogen receptor signaling pathway  IDA  RGD 

Molecular Function

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
Ncoa3Ratnuclear receptor coactivator activity  IDA  RGD 

Objects Annotated

Genes (Rattus norvegicus)
Ncoa3  (nuclear receptor coactivator 3)


Additional Information