scholarly journals Molecular mechanism of action and safety of 5-(3-chlorophenyl)-4-hexyl-2,4-dihydro-3H-1,2,4-triazole-3-thione - a novel anticonvulsant drug candidate

2017 ◽  
Vol 14 (8) ◽  
pp. 741-749 ◽  
Author(s):  
Barbara Kaproń ◽  
Jarogniew Łuszczki ◽  
Agata Paneth ◽  
Monika Wujec ◽  
Agata Siwek ◽  
...  
Keyword(s):  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Anticonvulsant Drug ◽  
Drug Candidate ◽  
Molecular Mechanism Of Action

scholarly journals A3Adenosine Receptor Allosteric Modulator Induces an Anti-Inflammatory Effect:In VivoStudies and Molecular Mechanism of Action

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Shira Cohen ◽  
Faina Barer ◽  
Sara Bar-Yehuda ◽  
Adriaan P. IJzerman ◽  
Kenneth A. Jacobson ◽  
...  
Keyword(s):  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Mononuclear Cells ◽  
White Blood Cells ◽  
Drug Candidate ◽  
Allosteric Modulator ◽  
Allosteric Modulators ◽  
Molecular Mechanism Of Action ◽  
Anti Inflammatory ◽  
Inflammatory Effect

The A3adenosine receptor (A3AR) is overexpressed in inflammatory cells and in the peripheral blood mononuclear cells of individuals with inflammatory conditions. Agonists to the A3AR are known to induce specific anti-inflammatory effects upon chronic treatment. LUF6000 is an allosteric compound known to modulate the A3AR and render the endogenous ligand adenosine to bind to the receptor with higher affinity. The advantage of allosteric modulators is their capability to target specifically areas where adenosine levels are increased such as inflammatory and tumor sites, whereas normal body cells and tissues are refractory to the allosteric modulators due to low adenosine levels. LUF6000 administration induced anti-inflammatory effect in 3 experimental animal models of rat adjuvant induced arthritis, monoiodoacetate induced osteoarthritis, and concanavalin A induced liver inflammation in mice. The molecular mechanism of action points to deregulation of signaling proteins including PI3K, IKK, IκB, Jak-2, and STAT-1, resulting in decreased levels of NF-κB, known to mediate inflammatory effects. Moreover, LUF6000 induced a slight stimulatory effect on the number of normal white blood cells and neutrophils. The anti-inflammatory effect of LUF6000, mechanism of action, and the differential effects on inflammatory and normal cells position this allosteric modulator as an attractive and unique drug candidate.

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

2019 ◽  
Author(s):  
John Eaton ◽  
Richard A. Ruberto ◽  
Anneke Kramm ◽  
Vasanthi S. Viswanathan ◽  
Stuart Schreiber
Keyword(s):  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Therapeutic Target ◽  
Biologically Active ◽  
Drug Resistant ◽  
Nitrile Oxides ◽  
Molecular Mechanism Of Action

<div><div><div><p>GPX4 represents a promising yet difficult-to-drug therapeutic target for the treatment of, among others, drug-resistant cancers. While most GPX4 inhibitors rely on a chloroacetamide moiety to modify covalently the protein’s catalytic selenocysteine residue, the discovery and mechanistic elucidation of structurally diverse GPX4-inhibiting molecules has uncovered novel electrophilic warheads that bind and inhibit GPX4. Here we report our discovery that diacylfuroxans can act as masked nitrile oxides that inhibit GPX4 covalently. These observations illuminate a novel molecular mechanism of action for biologically active furoxans and also suggest that nitrile oxides may be uniquely suited to targeting GPX4.</p></div></div></div>

Dietary selenomethionine ameliorates lipopolysaccharide-induced renal inflammatory injury in broilers via regulating the PI3K/AKT pathway to inhibit necroptosis

2021 ◽  
Author(s):  
Yue Zhang ◽  
Xue Qi ◽  
Xiaoming Chen ◽  
Jinxi Zhang ◽  
Wenyue Zhang ◽  
...  
Keyword(s):  
Protective Effect ◽  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Kidney Tissue ◽  
Akt Pathway ◽  
Inflammatory Injury ◽  
Molecular Mechanism Of Action

We explore the protective effect of dietary SeMet on the kidney tissue of broilers and determine its potential molecular mechanism of action.

Cellular and molecular mechanism of action of raloxifene on vascular tissue

Bone ◽  
2007 ◽  
Vol 41 (6) ◽  
pp. S2
Author(s):  
B Rauschemberger ◽  
P Cutini ◽  
M Sandoval ◽  
N Polini ◽  
V Massheimer
Keyword(s):  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Vascular Tissue ◽  
Molecular Mechanism Of Action
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