Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analogue 10 demonstrated complete tumor stasis in a Met-dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials.
[Purpose] The aim of this study was to evaluate the changes in posture and respiratory
functions depending on the duration of smartphone usage. [Subjects and Methods]
Participants were randomly allocated to 2 groups: group 1 (subjects who used smartphones
for <4 hours/day, n=25) and group 2 (subjects who used smartphones for >4 hours/day,
n=25). The craniovertebral angles of all participants were measured and scapular indices
were calculated to assess the change in posture and forced vital capacity, forced
expiratory volume in 1 second, the ratio of forced expiratory volume in 1 second to forced
vital capacity, and peak expiratory flow were measured to assess changes in respiratory
function. [Results] There were significant differences in the craniovertebral angle,
scapular index, and peak expiratory flow depending on the duration of smartphone usage.
[Conclusion] The result of this study showed that prolonged use of smartphones could
negatively affect both, posture and respiratory function.
Affinity selection screening of macrocycle libraries derived from DNA-programmed chemistry identified XIAP BIR2 and BIR3 domain inhibitors that displace bound pro-apoptotic caspases. X-ray cocrystal structures of key compounds with XIAP BIR2 suggested potency-enhancing structural modifications. Optimization of dimeric macrocycles with similar affinity for both domains were potent pro-apoptotic agents in cancer cell lines and efficacious in shrinking tumors in a mouse xenograft model.
[Purpose] The purpose of this study was to determine the effect of aquatic dual-task
training on balance and gait in stroke patients. [Subjects and Methods] Twenty stroke
patients were divided into the experimental (n=10) and control (n=10) groups. Both groups
underwent neurodevelopmental treatment. The experimental group additionally underwent
aquatic dual-task training for 30 minutes a day, 5 days a week, for 6 weeks. Balance was
measured using the Berg balance scale, Five Times Sit-to Stand Test, and Functional Reach
Test. Gait was measured using the 10-Meter Walk Test, Timed Up and Go Test, and Functional
Gait Assessment. [Results] For intragroup comparison, the experimental group showed a
significant change after the experiment in all balance and gait assessment tests. For
intergroup comparison, the experimental group showed relatively more significant change
after the experiment in all balance and gait assessment tests. [Conclusion] Our results
showed that aquatic dual-task training has a positive effect on balance and gait in stroke
patients.
Abstract.[Purpose] The purpose of this study was to investigate the effects of feedback respiratory training on chest expansion and pulmonary function in patients with stroke. [Subjects and Methods] Twenty-seven patients with stroke were randomly assigned to two groups: the feedback respiratory training group (experimental) (n=13) and the control group (control) (n=14). Feedback respiratory training and conventional physical therapy were performed by the experimental group. Conventional physical therapy was performed by the control group. Both groups received training three times per week for four weeks.[Results] Significant improvements were observed in chest expansion after training in the experimental group. Gains in chest expansion were greater in the experimental than in control group. Values of forced vital capacity, forced expiratory volume at one second, peak expiratory flow, vital capacity, expiratory reserve volume, and inspiratory reserve volume in pulmonary function tests increased post-training in the experimental group. With the exception of expiratory reserve volume, all of these pulmonary function test measures showed greater gains in the experimental group than in the control group. [Conclusion] Feedback respiratory training is effective for the improvement of chest expansion and pulmonary function in patients with stroke.
[Purpose] This study evaluated the effects of water and land-based obstacle training on
static balance of chronic stroke patients. [Subjects] The subjects were randomly allocated
to an aqua group (n=15) and a land group (n=15). [Methods] Both groups trained for 40
minutes, 3 times a week for 12 weeks. Static balance was assessed by measuring the mean
velocities of mediolateral (ML) and anteroposterior (AP), and sway area with the eyes
closed. [Results] Following the intervention, both groups showed significant changes in ML
velocity, AP velocity, and sway area. The static balance of the aqua group was
significantly better than the land group. [Conclusion] The results of this study suggest
the feasibility and suitability of obstacle training in water for stroke patients.
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