Neurokinin-3 Receptor-Specific Antagonists Talnetant and Osanetant Show Distinct Mode of Action in Cellular Ca2+ Mobilization but Display Similar Binding Kinetics and Identical Mechanism of Binding in Ligand Cross-Competition

2006 ◽  
Vol 71 (3) ◽  
pp. 902-911 ◽  
Author(s):  
Gaochao Tian ◽  
Dee Wilkins ◽  
Clay W. Scott
Keyword(s):  
Mode Of Action ◽  
Binding Kinetics ◽  
Distinct Mode ◽  
Neurokinin 3 Receptor ◽  
Cross Competition

scholarly journals GPI0363 inhibits the interaction of RNA polymerase with DNA in Staphylococcus aureus

RSC Advances ◽  
2019 ◽  
Vol 9 (65) ◽  
pp. 37889-37894 ◽  
Author(s):  
Atmika Paudel ◽  
Suresh Panthee ◽  
Hiroshi Hamamoto ◽  
Kazuhisa Sekimizu
Keyword(s):  
Staphylococcus Aureus ◽  
Rna Polymerase ◽  
Mode Of Action ◽  
Distinct Mode

GPI0363 has a distinct mode of action via SigA and is active against bacteria resistant to clinically used RNAP inhibitors.

Characterization ofCaenorhabditis elegansExonuclease-3 and Evidence That a Mg2+-Dependent Variant Exhibits a Distinct Mode of Action on Damaged DNA†

Biochemistry ◽  
2005 ◽  
Vol 44 (38) ◽  
pp. 12835-12848 ◽  
Author(s):  
Andrea Shatilla ◽  
Alexander A. Ishchenko ◽  
Murat Saparbaev ◽  
Dindial Ramotar
Keyword(s):  
Mode Of Action ◽  
Distinct Mode ◽  
Damaged Dna

scholarly journals Ethacridine inhibits SARS-CoV-2 by inactivating viral particles

2021 ◽  
Vol 17 (9) ◽  
pp. e1009898
Author(s):  
Xiaoquan Li ◽  
Peter Lidsky ◽  
Yinghong Xiao ◽  
Chien-Ting Wu ◽  
Miguel Garcia-Knight ◽  
...  
Keyword(s):  
Mode Of Action ◽  
High Throughput Screening ◽  
Cell Types ◽  
Host Cells ◽  
Main Mode ◽  
Distinct Mode ◽  
Human Nasal Epithelial Cells ◽  
Viral Particles ◽  
Potent Drug ◽  
Air Liquid Interface

The respiratory disease COVID-19 is caused by the coronavirus SARS-CoV-2. Here we report the discovery of ethacridine as a potent drug against SARS-CoV-2 (EC50 ~ 0.08 μM). Ethacridine was identified via high-throughput screening of an FDA-approved drug library in living cells using a fluorescence assay. Plaque assays, RT-PCR and immunofluorescence imaging at various stages of viral infection demonstrate that the main mode of action of ethacridine is through inactivation of viral particles, preventing their binding to the host cells. Consistently, ethacridine is effective in various cell types, including primary human nasal epithelial cells that are cultured in an air-liquid interface. Taken together, our work identifies a promising, potent, and new use of the old drug via a distinct mode of action for inhibiting SARS-CoV-2.

Effects of 5-5'-Diphenyl-2-thiohydantoin (DPTH) and Thyroxine on the Ultrastructure and Chemical Composition of Rat Liver

1971 ◽  
Vol 29 ◽  
pp. 570-571
Author(s):  
E. A. Elfont ◽  
R. B. Tobin ◽  
D. G. Colton ◽  
M. A. Mehlman
Keyword(s):  
Chemical Composition ◽  
Rat Liver ◽  
Future Study ◽  
Mode Of Action ◽  
Liver Mitochondria ◽  
Rat Liver Mitochondria ◽  
Effective Inhibitor ◽  
Biochemical Effects ◽  
Glycerophosphate Dehydrogenase ◽  
Stimulation Of

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.

Mode of action of 6-oxophenolic triterpenoids against Bacillus subtilis

Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
L Moujir ◽  
L de León ◽  
IL Bazzocchi
Keyword(s):  
Bacillus Subtilis ◽  
Mode Of Action
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