Mechanism of action of ferrocene derivatives on the catalytic activity of topoisomerase IIα and β—Distinct mode of action of two derivatives

2005 ◽  
Vol 438 (2) ◽  
pp. 206-216 ◽  
Author(s):  
A.D. Sai Krishna ◽  
Gayatri Panda ◽  
Anand K. Kondapi
Keyword(s):  
Catalytic Activity ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Ferrocene Derivatives ◽  
Distinct Mode ◽  
Topoisomerase Iiα

Comparative mode-of-action analysis following manual and automated phenotype detection in Xenopus laevis

MedChemComm ◽  
2014 ◽  
Vol 5 (3) ◽  
pp. 386-396 ◽  
Author(s):  
Georgios Drakakis ◽  
Adam E. Hendry ◽  
Kimberley Hanson ◽  
Suzanne C. Brewerton ◽  
Michael J. Bodkin ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Xenopus Laevis ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Action Analysis

Given the increasing utilization of phenotypic screens in drug discovery also the subsequent mechanism-of-action analysis gains increased attention.

scholarly journals The Phosphoenolpyruvate:Sugar Phosphotransferase System Is Involved in Sensitivity to the Glucosylated Bacteriocin Sublancin

2015 ◽  
Vol 59 (11) ◽  
pp. 6844-6854 ◽  
Author(s):  
C. V. Garcia De Gonzalo ◽  
E. L. Denham ◽  
R. A. T. Mars ◽  
J. Stülke ◽  
W. A. van der Donk ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Phosphotransferase System ◽  
Content Type ◽  
Gram Positive Bacteria ◽  
Distinct Mechanism ◽  
Genomic Studies ◽  
Increased Sensitivity ◽  
Bacterial Sensitivity

ABSTRACTThe mode of action of a group of glycosylated antimicrobial peptides known as glycocins remains to be elucidated. In the current study of one glycocin, sublancin, we identified the phosphoenolpyruvate:sugar phosphotransferase system (PTS) ofBacillusspecies as a key player in bacterial sensitivity. Sublancin kills several Gram-positive bacteria, such asBacillusspecies andStaphylococcus aureus, including methicillin-resistantS. aureus(MRSA). Unlike other classes of bacteriocins for which the PTS is involved in their mechanism of action, we show that the addition of PTS-requiring sugars leads to increased resistance rather than increased sensitivity, suggesting that sublancin has a distinct mechanism of action. Collectively, our present mutagenesis and genomic studies demonstrate that the histidine-containing phosphocarrier protein (HPr) and domain A of enzyme II (PtsG) in particular are critical determinants for bacterial sensitivity to sublancin.

scholarly journals Ferrocenes as Potential Anticancer Drugs: Determination of the Mechanism of Action

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 16
Author(s):  
Hrstka ◽  
Skoupilová ◽  
Bartošík ◽  
Sommerová ◽  
Karban ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Cell Lines ◽  
Mechanism Of Action ◽  
Anticancer Agents ◽  
Organometallic Compounds ◽  
Differential Pulse ◽  
Vital Role ◽  
Intracellular Accumulation ◽  
Ferrocene Derivatives

Chemotherapy is an essential treatment that still plays a vital role in cancer treatment worldwide. The ferrocene derivatives of the general formula [Fe{(η5‑C5H4CH2(p‑C6H4)CH2(N‑het)}2] bearing modified six and five membered N-heterocycles were tested in vitro for their cytotoxic properties against ovarian cancer cell lines A2780 and SK-OV-3. These ferrocene complexes displayed cytotoxicity in low micromolar concentrations against both cell lines. To study cellular uptake of particular ferrocenes into tumor cells, we used differential pulse voltammetry and ICP-MS. We confirmed the crucial role of transferrin receptors in the process of intracellular accumulation of these ferrocenes. Interestingly, the rate of intracellular accumulation of particular ferrocenes clearly mirrored the cytotoxicity of these organometallic compounds. Deeper investigation of the mechanism by which ferrocenes kill tumor cells revealed induction of apoptosis associated with significant increase of reactive oxygen species. In conclusion, our screening identified several ferrocene derivatives exerting promising cytostatic activity in vitro. Further investigation led to the identification of the mechanism of action of these potential anticancer agents, which represents an important milestone in preclinical anticancer drug discovery programs. This work was supported by the project MEYS-NPS I-LO1413, MH CZ-DRO (MMCI, 00209805) and Czech Science Foundation project 17-05838S.

Mechanism of Action of Progestins in the Treatment of Hormone-dependent Breast Cancer.

1975 ◽  
Vol 61 (6) ◽  
pp. 501-508 ◽  
Author(s):  
Francesco Di Carlo ◽  
Giovanni Pacilio ◽  
Giuseppe Conti
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptors ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Binding Capacity ◽  
Specific Receptors ◽  
High Concentrations ◽  
Good Agreement

The in vitro interference of some gestagens with the binding of 3H-17 β-oestradiol to cytosol specific receptors was investigated with a view to elucidating the mechanism of action of progestins in the treatment of human hormone-dependent breast cancer. A decrease (up to 85 %) of oestradiol binding capacity was observed with high concentrations of progesterone, clogestone and medrogestone. These findings are in good agreement with those previously obtained by the same progestins in our laboratory on rat uterine estrogen receptors in vitro or in vivo. These results provide support for the hypothesis that the mode of action of progestins in the therapy of mammary and perhaps uterine carcinomas is to some extent related to the inhibition of oestradiol binding to cytosol specific receptors.

Antidepressant Drugs and Migraine

Cephalalgia ◽  
1985 ◽  
Vol 5 (2_suppl) ◽  
pp. 225-228 ◽  
Author(s):  
N Martucci ◽  
V Manna ◽  
A Agnoli
Keyword(s):  
Mechanism Of Action ◽  
Clinical Studies ◽  
Mode Of Action ◽  
Antidepressant Drugs ◽  
Antidepressant Activity

There is evidence that some antidepressant drugs, above all amitriptyline and mianserine, are beneficial in the prophylaxis of migraine. The mechanism of action of antidepressants in migraine is likely to be complex. Mood disturbances accompanying migraine syndromes suggest a mode of action of such a class of drugs. In the last few years some clinical studies tend to show that the antimigraine effects of these drugs seem relatively independent of the antidepressant activity.

Antifungals

2016 ◽  
Author(s):  
M. Estée Török ◽  
Fiona J. Cooke ◽  
Ed Moran
Keyword(s):  
Mechanism Of Action ◽  
Mode Of Action ◽  
Antifungal Agents ◽  
Clinical Use ◽  
Mechanisms Of Resistance ◽  
Action Mechanisms

This chapter provides a systematic summary of antifungal agents, grouped by class and mechanism of action. Each summary provides information on the mode of action, mechanisms of resistance, pharmacology, and clinical use.

scholarly journals Fish Oil in the Treatment of Ulcerative Colitis

1990 ◽  
Vol 4 (7) ◽  
pp. 420-423 ◽  
Author(s):  
C Ó'Moráin ◽  
A Tobin ◽  
T McColl ◽  
Y Suzuki
Keyword(s):  
Ulcerative Colitis ◽  
Arachidonic Acid ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Rectal Mucosa ◽  
Leukotriene B4 ◽  
Biologically Active ◽  
Active Ulcerative Colitis ◽  
Pilot Studies ◽  
Lysosomal Membrane Stability

Patients with active ulcerative colitis have increased levels of leukotriene B4 in their rectal mucosa. Eicosapentaenoic acid (EPA) competitively inhibits the cyclo-oxgenase pathway and reduces the formation of cyclo-oxygenase pathway products. EPA is a good substrate for lipoxygenase enzymes and is efficiently converted to leukotriene 85, which is less biologically active. The conversion of EPA to leukotriene B5 is as efficient as that of arachidonic acid to teukotriene B4. Two pilot studies showed benefit of EPA in the treatment of ulcerative colitis. Two of three controlled studies suggest that EPA is more effective than placebo in the treatment of active chronic ulcerative colitis. The mechanism of action is probably reduction of leukotriene B4, but EPA could increase cell and lysosomal membrane stability, or it may exert its effect by reducing interleukin-l. More controlled studies and detailed investigation into the mode of action of EPA are required.

Paper 5: Some Experiments on the Mode of Action of a Diesel Smoke Suppressant Additive

1968 ◽  
Vol 183 (5) ◽  
pp. 179-206 ◽  
Author(s):  
B. E. Knight ◽  
C. H. T. Wang
Keyword(s):  
Low Temperature ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Engine Performance ◽  
Marginal Effect ◽  
Carbon Formation ◽  
Early Stages ◽  
Quantitative Measurements ◽  
Smoke Suppressant ◽  
Burn Out

The use of a smoke suppressant additive is very effective in reducing smoke but has only a marginal effect upon all aspects of engine performance. Photographed flame in the engine appeared to burn out earlier with the additive and at a time when gas temperatures were high. Thus, the additive was not just a catalyst for low-temperature burning of carbon. Quantitative measurements of carbon formation could not be achieved, so it is not possible to state with certainty whether the additive reduces carbon formation. The photographs do not show an observable difference of carbon formation. The most likely mechanism of action of the additive is by assisting the burning of carbon at the early stages of the engine expansion stroke.

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