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  • MAPK
  • The purpose of this study was to investigate the usefulness of a p38 MAPK inhibitor for promoting proliferation of human corneal endothelial cells (HCECs). (arvojournals.org)
  • Activation of substrates of p38 MAPK and cell cycle regulatory proteins were evaluated by western blotting. (arvojournals.org)
  • p38 MAP Kinase (MAPK), also called RK or CSBP (Cytokinin Specific Binding Protein), is the mammalian orthologue of the yeast Hog1p MAP kinase, which participates in a signaling cascade controlling cellular responses to cytokines and stress. (wikipedia.org)
  • extracellular
  • The proliferative effects of ROCK on vascular endothelial cells is due to the activation of extracellular signal-regulated kinase (ERK). (wikipedia.org)
  • activity
  • In an effort to identify additional CaMK inhibitors that exhibit more potent activity in triggering leukemia cell differentiation, we synthesized 45 analogues of KN-62 and determined their ability to induce HL-60 cell differentiation. (washington.edu)
  • The gene splicing converted a protein with 70 amino acids into one of 109 amino acids, and did not change the inhibitory potency to PKA, but changed it from a protein that had no detectable PKG inhibitory activity to one that now inhibited PKG in the nanomolar range. (biochemj.org)
  • Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10-30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells. (wikipedia.org)
  • In June 2006, a phase I clinical trial found nilotinib has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib, another tyrosine kinase inhibitor currently used as a first-line treatment. (wikipedia.org)
  • The protein product of Proto-oncogene RAS can increase activity of p38, and thereby cause excessively high activity of transcription factor NF-κB. (wikipedia.org)
  • blockade
  • ii) the oncogenic switch to another pathway that rescues cancer cells from kinase blockade. (unina.it)
  • proliferation
  • Safingol is also a putative inhibitor of sphingosine kinase 1 (SphK), which catalyzes the production of sphingosine 1-phosphate (S1P), an important mediator of cancer cell growth, proliferation, invasion, and angiogenesis. (wikipedia.org)
  • signaling cascade
  • ii) thyroid cancer cells escape treatment with vemurafenib by switching to another signaling pathway and that inhibitors of the IGF1R/PI3K/AKT signaling cascade may be exploited to overcome resistance of thyroid cancer cells lines to BRAF PKI. (unina.it)
  • conformation
  • Like PIM1, PIM2 shows a bi-lobal kinase architecture with a constitutively active closed conformation. (wikipedia.org)
  • Typically, kinases' active state is characterized by the presence of the conserved lysine, a closed lobe conformation, and a well-structured activation segment. (wikipedia.org)
  • The crystal structures show that the unphosphorylated activation segment forms many polar interactions with the lower kinase lobe, which stabilizes the active conformation. (wikipedia.org)
  • The bound BIM1 inhibitor blocks the ATP-binding site and puts the kinase domain into an intermediate open conformation. (wikipedia.org)