https://ogma.newcastle.edu.au/vital/access/ /manager/Index en-au 5 FMS-like tyrosine kinase 3 (FLT3) inhibitors: molecular docking and experimental studies https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:30110 50 values in the cell proliferation assay, CEP701 was the most potent inhibitor; sunitinib and PKC412 were ranked second and third, respectively. Sunitinib was the most selective inhibitor, followed by PKC421 and CEP701. The potency of sunitinib and to a lesser extent CEP701 in inhibition of FLT3 autophosphorylation was lower than the cell proliferation inhibition, indicating that inhibition of FLT3 downstream proteins may contribute to the cellular effects. It was shown in this study that the docking procedure was able to differentiate FLT3 inhibitors from ineffective compounds. Additionally, interaction with the phosphate binding region in the ATP-binding pocket increased potency at the cost of selectivity. These findings can be applied in designing highly effective and selective inhibitors for FLT3 and other related kinases.]]> Wed 15 Dec 2021 16:10:04 AEDT ]]> Targeting PP2A activation as a novel therapeutic strategy for receptor tyrosine kinase driven leukaemia https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:14165 Wed 11 Apr 2018 13:47:17 AEST ]]> MicroRNA-16 is down-regulated in mutated FLT3 expressing murine myeloid FDC-P1 cells and interacts with Pim-1 https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:15110 Wed 11 Apr 2018 11:57:39 AEST ]]> Targeting Oncogenic Signaling in Mutant FLT3 Acute Myeloid Leukemia: The Path to Least Resistance https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:41430 Wed 03 Aug 2022 14:12:29 AEST ]]> Activation of protein phosphatase 2A in FLT3+ acute myeloid leukemia cells enhances the cytotoxicity of FLT3 tyrosine kinase inhibitors https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:27776 Thu 28 Oct 2021 13:04:26 AEDT ]]> Identifying novel therapeutic targets for the treatment of Acute Myeloid Leukaemia https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:36309 Thu 14 Mar 2024 12:13:37 AEDT ]]> Molecular and phosphoproteomic characterisation of FLT3 inhibitor resistance in acute myeloid leukaemia https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:55549 Thu 06 Jun 2024 09:53:01 AEST ]]> Differences in growth promotion, drug response and intracellular protein trafficking of FLT3 mutants https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:19252 Sat 24 Mar 2018 07:54:55 AEDT ]]>