scholarly journals Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

2018 ◽  
Vol 13 (9) ◽  
pp. 2758-2770 ◽  
Author(s):  
Kristin M. Riching ◽  
Sarah Mahan ◽  
Cesear R. Corona ◽  
Mark McDougall ◽  
James D. Vasta ◽  
...  
The Analyst ◽  
2019 ◽  
Vol 144 (8) ◽  
pp. 2725-2735 ◽  
Author(s):  
Ali Altharawi ◽  
Khondaker Miraz Rahman ◽  
K. L. Andrew Chan

Fourier transform infrared spectroscopy (FTIR) has been shown to be a promising tool for identifying the mode of action of drugs.


Author(s):  
E. A. Elfont ◽  
R. B. Tobin ◽  
D. G. Colton ◽  
M. A. Mehlman

Summary5,-5'-diphenyl-2-thiohydantoin (DPTH) is an effective inhibitor of thyroxine (T4) stimulation of α-glycerophosphate dehydrogenase in rat liver mitochondria. Because this finding indicated a possible tool for future study of the mode of action of thyroxine, the ultrastructural and biochemical effects of DPTH and/or thyroxine on rat liver mere investigated.Rats were fed either standard or DPTH (0.06%) diet for 30 days before T4 (250 ug/kg/day) was injected. Injection of T4 occurred daily for 10 days prior to sacrifice. After removal of the liver and kidneys, part of the tissue was frozen at -50°C for later biocheailcal analyses, while the rest was prefixed in buffered 3.5X glutaraldehyde (390 mOs) and post-fixed in buffered 1Z OsO4 (376 mOs). Tissues were embedded in Araldlte 502 and the sections examined in a Zeiss EM 9S.Hepatocytes from hyperthyroid rats (Fig. 2) demonstrated enlarged and more numerous mitochondria than those of controls (Fig. 1). Glycogen was almost totally absent from the cytoplasm of the T4-treated rats.


Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
L Moujir ◽  
L de León ◽  
IL Bazzocchi

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