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dc.contributor.authorNajajreh, Yousef
dc.contributor.authorKhamaisie, Hazem
dc.contributor.authorRuimi, Nili
dc.contributor.authorKhatib, Soliman
dc.contributor.authorKatzhendler, Joshua
dc.contributor.authorRuthardt, Martin
dc.contributor.authorMahajna, Jamal
dc.date.accessioned2018-09-03T10:42:14Z
dc.date.available2018-09-03T10:42:14Z
dc.date.issued2012-12-05
dc.identifier.issn1573-4978
dc.identifier.urihttps://dspace.alquds.edu/handle/20.500.12213/815
dc.description.abstractChronic myeloid leukemia (CML) is characterized by the presence of p210Bcr-Abl which exhibits an abnormal kinase activity. Selective Abl kinase inhibitors have been successfully established for the treatment of CML. Despite high rates of clinical response, CML patients can develop resistance against these kinase inhibitors mainly due to point mutations within the Abl protein kinase domain. Previously, we have identified oleic acid as the active component in the mushroom Daedalea gibbosa that inhibited the kinase activity of Bcr-Abl. Here, we report that the oleyl amine derivatives, S-1-(1-Hydroxymethyl-2-methyl-propyl)- 3-octadec-9-enyl-urea [oleylaminocarbonyl-L-Nvalinol, oroleylaminocarbonyl-S-2-isopropyl-N-ethanolamine, oleylamine-carbonyl-L-valinol] (cpd 6) and R-1-(1-Hydroxymethyl- 2-methyl-propyl)-3-octadec-9-enyl-urea [oleylamineocarbonyl- D-N-valinol, oleylaminocarbonyl-R-2-isopropyl- N-ethanolamine, or oleylamine-carbonyl-D-valinol] (cpd 7), inhibited the activity of the native and T315I mutated Bcr-Abl. Furthermore, cpd 6 and 7 exhibited higher activity towards the oncogenic Bcr-Abl in comparison to native c-Abl in SupB15 Ph-positive ALL cell line.en_US
dc.description.sponsorshipThis work was supported, in part, by DFG-RU 728/3-2 to MR, YN and JM.en_US
dc.language.isoen_USen_US
dc.publisherSpringeren_US
dc.subjectOleylamineen_US
dc.subjectL-/D-Valinolen_US
dc.subjectAnti-tumor activityen_US
dc.subjectOleic aciden_US
dc.subjectBcr-Ablen_US
dc.subjectKinaseen_US
dc.subjectCMLen_US
dc.titleOleylamine-carbonyl-valinol inhibits auto-phosphorylation activity of native and T315I mutated Bcr-Abl, and exhibits selectivity towards oncogenic Bcr-Abl in SupB15 ALL cell linesen_US
dc.typeArticleen_US


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