2005
DOI: 10.1016/j.exphem.2004.09.006
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Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist

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Cited by 181 publications
(144 citation statements)
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“…The selectivity of eltrombopag for the TPO-receptor rather than other growth factor receptors was demonstrated by assays measuring STAT activation or reporter gene expression in various transfected and non-transfected cell lines. The assays confirmed the ability of eltrombopag to activate signalling in cells expressing the TPO receptor but showed that it had no effect on cells expressing only interferon-γ, granulocyte macrophage-colony stimulating factor (GM-CSF), G-CSF, erythropoietin or interleukin-3 receptors [36]. The fact that eltrombopag lacks activity against cells expressing growth factor receptors other than TPO, even those acting through the JAK/STAT signalling pathway, suggests that the activation of JAK/STAT by eltrombopag is due to the specific activation of the TPO receptor [37].…”
Section: Eltrombopagmentioning
confidence: 86%
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“…The selectivity of eltrombopag for the TPO-receptor rather than other growth factor receptors was demonstrated by assays measuring STAT activation or reporter gene expression in various transfected and non-transfected cell lines. The assays confirmed the ability of eltrombopag to activate signalling in cells expressing the TPO receptor but showed that it had no effect on cells expressing only interferon-γ, granulocyte macrophage-colony stimulating factor (GM-CSF), G-CSF, erythropoietin or interleukin-3 receptors [36]. The fact that eltrombopag lacks activity against cells expressing growth factor receptors other than TPO, even those acting through the JAK/STAT signalling pathway, suggests that the activation of JAK/STAT by eltrombopag is due to the specific activation of the TPO receptor [37].…”
Section: Eltrombopagmentioning
confidence: 86%
“…The response of normal human TPO receptors has been elucidated by measuring growth and differentiation of human bone marrow in vitro. These studies demonstrated human and chimpanzee-specific stimulation of TPOreceptor-expressing cells via activation of STAT5, with no eltrombopag-induced STAT activation observed in other species tested, including cynomolgus macaques, rhesus monkeys, pigs, dogs, ferrets, rabbits, rats and mice [36]. The selectivity of eltrombopag for the TPO-receptor rather than other growth factor receptors was demonstrated by assays measuring STAT activation or reporter gene expression in various transfected and non-transfected cell lines.…”
Section: Eltrombopagmentioning
confidence: 89%
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“…Newer TPO receptor agonists have no sequence homology with the native molecule and are not expected to provoke crossreactive antibodies. Results from recent trials with these agents provide in vivo evidence that boosting platelet production is an effective therapeutic strategy [59,60,64,65]. Four TPO receptor agonists are currently being evaluated in patients with ITP-romiplostim (Amgen, Thousand Oaks, CA), eltrombopag or SB-497115 (GlaxoSmithKline, Collegeville, PA), AKR-501 (MGI Pharma, Bloomington, MN), and LGD-4665 (Ligand Pharmaceuticals, San Diego, CA).…”
Section: Emerging Therapies Target Platelet Productionmentioning
confidence: 99%
“…[8,9] Obwohl die Inhibierung von Protein-Protein-Interaktionen (PPIs) mittels kleiner Moleküle lange Zeit als die ultimative Herausforderung in der Wirkstoffentwicklung galt, wurden nur sehr wenige Beispiele für solche PPI-Inhibitoren beschrieben. [10][11][12][13] Demgegenüber gibt es klare mechanistischkonzeptionelle Argumente dafür, dass PPI-Stabilisatoren großes Potential haben kçnnten. [14] LFA-1-Aktivatoren wären ein vielversprechender Ansatz für die Behandlung einer seltenen Erbkrankheit, bekannt als Leukozytenadhäsi-onsdeffizienz (LAD), oder als mçgliche Verstärker in der Tumorimmuntherapie.…”
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