Effect of IKK-2 Inhibitor on Local Th1 and Th2 Type Inflammation

Ligacheva, A. A.; Ivanova, Aneta; Belsky, Yu. P.; Belska, N. V.; Trofimova, E. S.; Данилец, М. Г.; Дыгай, А. М.

doi:10.1007/s10517-013-2078-4

Cited by 2 publications

(2 citation statements)

References 14 publications

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“…Ligacheva et al [ 63 ] seeking to identify ĸβ-kinase inhibitor capable of reducing Th1 (paw edema model) and Th2 (ovalbumin-induced immediate local hypersensitivity) responses in mice, noted that 2-amino-thiophenic derivatives rich in electron donor clusters, such as compound 20 ( Figure 5 ), contain fluorophenyl, amide and carbamate groups. The evaluated compound reduced edema in a similar way to (diclofenac), and was able to reduce the edema by 1.3 times as compared to 1.6 times for diclofenac.…”

Section: The Role Of Thiophene Derivatives In Inflammationmentioning

confidence: 99%

Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

et al. 2021

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Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive action in improving symptoms, without effectively promoting the cure. However, recent advances in the fields of pharmacology, medicinal chemistry, and chemoinformatics have provided valuable information and opportunities for development of new anti-inflammatory drug candidates. For drug design and discovery, thiophene derivatives are privileged structures. Thiophene-based compounds, like the commercial drugs Tinoridine and Tiaprofenic acid, are known for their anti-inflammatory properties. The present review provides an update on the role of thiophene-based derivatives in inflammation. Studies on mechanisms of action, interactions with receptors (especially against cyclooxygenase (COX) and lipoxygenase (LOX)), and structure-activity relationships are also presented and discussed. The results demonstrate the importance of thiophene-based compounds as privileged structures for the design and discovery of novel anti-inflammatory agents. The studies reveal important structural characteristics. The presence of carboxylic acids, esters, amines, and amides, as well as methyl and methoxy groups, has been frequently described, and highlights the importance of these groups for anti-inflammatory activity and biological target recognition, especially for inhibition of COX and LOX enzymes.

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Section: The Role Of Thiophene Derivatives In Inflammationmentioning

confidence: 99%

Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

et al. 2021

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“…72 More recently, TCPA1 has been shown to reduce the severity of type 1 helper T-cell (Th1)–mediated local immune responses. 73 Multiple autoimmune disease are considered to be broadly Th1-mediated, including multiple sclerosis (MS), type 1 insulin-dependent diabetes mellitus, and posterior uveitis, and although a variety of factors contribute to the complex symptoms of each disease, the abrogation of Th1-type responses via NF-κB modulation could potentially help to alleviate such conditions. Another novel IKK inhibitor, 3-[(dodecylthiocarbonyl)methyl]glutarimide (DTCM-glutarimide), has been found to have anti-inflammatory activity both in vitro and in vivo.…”

Section: Targeting the Ikk Complexmentioning

confidence: 99%

Modulation of NF-κB Signaling as a Therapeutic Target in Autoimmunity

2016

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Autoimmune diseases arise from the loss of tolerance to endogenous self-antigens, resulting in a heterogeneous range of chronic conditions that cause considerable morbidity and mortality worldwide. In Western countries, over 5% of the population is affected by some form of autoimmune disease, with enhanced or inappropriate activation of nuclear factor (NF)–κB implicated in a number of these conditions. Although treatment strategies for autoimmunity have improved significantly in recent years, current therapeutics are still not capable of achieving satisfactory disease management in all patients, and as such, the therapeutic modulation of NF-κB is an attractive target in autoimmunity. To date, no NF-κB inhibitors have progressed to the clinic for the treatment of autoimmunity, but a variety of promising approaches targeting multiple stages of the NF-κB pathway are currently being explored. This review focuses on the current strategies being investigated for the inhibition of the NF-κB pathway in autoimmune diseases and considers potential future strategies for the therapeutic targeting of this crucial transcription factor.

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Effect of IKK-2 Inhibitor on Local Th1 and Th2 Type Inflammation

Cited by 2 publications

References 14 publications

Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

Modulation of NF-κB Signaling as a Therapeutic Target in Autoimmunity

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