TargetRx Atlas

MRNA basic information

  • mRNA ID:ENST00000396832
  • Gene Name:CSNK1E
  • mRNA database:Ensembl
  • mRNA expression :down-regulated
  • mRNA Method:qRT-PCR
  • mRNA Pathway:NA
  • Evidence:validated
  • (mRNA-drug)

Drug basic information

  • Drug ID:DB04770
  • Drug Name:O6-(R)-ROSCOVITINE
  • Drug Method:down-regulated the gene expression

Disease basic infommation

  • Disease:polycystic kidney disease
  • Tissue:tissues

Other information

  • Title:Casein kinase 1E and 1A as novel players in polycystic kidney disease and mechanistic targets for (R)-roscovitine and (S)-CR8
  • Journal:American Journal of Physiology-renal Physiology
  • Published:2018
  • PubMed ID:29537311
  • Abstract:Following the discovery of (R)-roscovitine＇s beneficial effects in three polycystic kidney disease (PKD) mouse models, cyclin-dependent kinases (CDKs) inhibitors have been investigated as potential treatments. We have used various affinity chromatography approaches to identify the molecular targets of roscovitine and its more potent analog (S)-CR8 in human and murine polycystic kidneys. These methods revealed casein kinases 1 (CK1) as additional targets of the two drugs. CK1蔚 expression at the mRNA and protein levels is enhanced in polycystic kidneys of 11 different PKD mouse models as well as in human polycystic kidneys. A shift in the pattern of CK1α isoforms is observed in all PKD mouse models. Furthermore, the catalytic activities of both CK1蔚 and CK1α are increased in mouse polycystic kidneys. Inhibition of CK1蔚 and CK1α may thus contribute to the long-lasting attenuating effects of roscovitine and (S)-CR8 on cyst development. CDKs and CK1s may constitute a dual therapeutic target to develop kinase inhibitory PKD drug candidates.
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