Description
Nilotinibisasecond-generationphenylaminopyridinetyrosinekinaseinhibitorthatisclinicallyusedtotreatBcr-Abl-positivechronicmyelogenousleukemia(CML).NilotinibisanATP-competitiveinhibitorofAbl,c-Kit,andPDGFRthatexhibitsanticancerchemotherapeutic,anti-fibrotic,anti-allergic,andanti-inflammatoryactivities.Incellularandanimalmodelsofhepatocellularcarcinoma,nilotinibincreasesactivationofAMPKandinhibitsproteinphosphatase2A(PP2A),inducingautophagyinvitroandinhibitingtumorxenograftsgrowthinvivo.Inhepaticstellatecells,nilotinibdecreasesexpressionofhistonedeacetylases1,2,and4(HDAC1/2/4),increasingapoptoticcelldeath.Inanimalmodelsofallergicreactionandinflammation,nilotinibinhibitsexpressionofTNF-αandpreventsmastcellhistaminerelease,decreasingpawedemaandpreventingsystemicanaphylaxis.
References
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El-AgamyDS.Anti-allergiceffectsofnilotinibonmastcell-mediatedanaphylaxislikereactions.EurJPharmacol.2012Apr5;680(1-3):115-21.PMID:22329898.
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