Browsing by Author "Chang, K-Y"

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BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML
(2012-01-31)
Lin, W-H
;
Jiaang, W-T
;
Chen, C-W
;
Yen, K-J
;
Hsieh, S-Y
BACKGROUND: Activating mutations of Fms-like tyrosine kinase 3 (FLT3) constitute a major driver in the pathogenesis of acute myeloid leukaemia (AML). Hence, pharmacological inhibitors of FLT3 are of therapeutic interest for AML. METHODS: The effects of inhibition of FLT3 activity by a novel potent FLT3 inhibitor, BPR1J-097, were investigated using in vitro and in vivo assays. RESULTS: The 50% inhibitory concentration (IC50) of BPR1J-097 required to inhibit FLT3 kinase activity ranged from 1 to 10 nM, and the 50% growth inhibition concentrations (GC(50)s) were 21 +/- 7 and 46 +/- 14 nM for MOLM-13 and MV4-11 cells, respectively. BPR1J-097 inhibited FLT3/signal transducer and activator of transcription 5 phosphorylation and triggered apoptosis in FLT3-driven AML cells. BPR1J-097 also showed favourable pharmacokinetic property and pronounced dose-dependent tumour growth inhibition and regression in FLT3-driven AML murine xenograft models. CONCLUSION: These results indicate that BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities and suggest that BPR1J-097 may be further developed in preclinical and clinical studies as therapeutics in AML treatments. British Journal of Cancer (2012) 106, 475-481. doi: 10.1038/bjc.2011.564 www.bjcancer.com Published online 20 December 2011 (C) 2012 Cancer Research UK
Quantification of Rossolimo reflexes: A sensitive marker for spondylotic myelopathy
(2011-02-01)
Chang, C-W
;
Chang, K-Y
;
Lin, S-M
;
管理學院
;
College of Management
Study design: Prospective study. Objectives: To assess and quantify Rossolimo reflexes using an electrophysiological test, and correlate the findings with the severity of spinal cord dysfunction in cervical and thoracic spondylotic myelopathy (CTSM). Setting: A university neurorehabilitation center. Methods: We enlisted 42 patients with CTSM between the fifth cervical and the ninth thoracic cord levels. Using electrophysiological assessments, Rossolimo reflexes were evaluated in all patients. Conduction latencies and amplitude of muscle action potentials (MAPs) of the reflexes were measured, analyzed and compared with the grading of spinal cord dysfunction and the cord compression ratios. Results: We found a high diagnostic sensitivity of quantified Rossolimo reflex in patients with CTSM. A positive correlation exists between the MAP amplitude of Rossolimo reflexes and the different grades of spinal cord dysfunction. A negative linear relationship was found between the MAP amplitude of Rossolimo reflexes and the cord compression ratios in CTSM patients. Conclusion: Rossolimo reflexes can be measured by electrophysiological assessments, and we demonstrate a quantification method for an established neurological sign. Not only is the Rossolimo reflex found to be a highly sensitive test in clinical neurological examination but the electrophysiological assessment for this reflex can also serve as an objective marker for evaluation of the severity of spinal cord dysfunction in CTSM. Spinal Cord (2011) 49, 211-214; doi: 10.1038/sc.2010.81; published online 13 July 2010