scholarly journals Discovery of a novel cyclin-dependent kinase 8 inhibitor with an oxindole core for anti-inflammatory treatment

2022 ◽  
Vol 146 ◽  
pp. 112459
Author(s):  
Tony Eight Lin ◽  
Chia-Ron Yang ◽  
Ching-Hsuan Chou ◽  
Jui-Yi Hsu ◽  
Min-Wu Chao ◽  
...  
Keyword(s):  
Cyclin Dependent Kinase ◽  
Anti Inflammatory

scholarly journals 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-thiazolidine-2,4-dione

Molbank ◽  
10.3390/m1083 ◽  
2019 ◽  
Vol 2019 (4) ◽  
pp. M1083
Author(s):  
Uwabagira ◽  
Sarojini
Keyword(s):  
Breast Adenocarcinoma ◽  
Cyclin Dependent Kinase ◽  
Human Breast ◽  
Hemolysis Assay ◽  
Human Breast Adenocarcinoma ◽  
Inflammatory Agent ◽  
Human Blood Cell ◽  
Anti Inflammatory ◽  
Mcf 7

The compound 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-thiazolidine-2,4-dione has been designed, synthesized, and screened for its in vitro antibreast cancer activity, using human breast adenocarcinoma cell lines (MCF-7) and in vitro anti-inflammatory activity. By hemolysis assay, it showed that it has a nonhemolytic and nontoxic effect on human blood cell. The title compound 5, subjected to in vitro activities, showed that it is cytotoxic with an IC50 of 42.30 µM and a good anti-inflammatory agent. The docking results against cyclin dependent kinase 2 (CDK2) (PDB ID: 3QQK) gave insights on its inhibitory activity.

scholarly journals Deletion of Cdk5 in Macrophages Ameliorates Anti-Inflammatory Response during Endotoxemia through Induction of C-Maf and Il-10

2021 ◽  
Vol 22 (17) ◽  
pp. 9648
Author(s):  
Pauline Pfänder ◽  
Ann-Kathrin Eiers ◽  
Ute Burret ◽  
Sabine Vettorazzi
Keyword(s):  
Inflammatory Response ◽  
Interleukin 10 ◽  
Cyclin Dependent Kinase ◽  
Inflammatory Conditions ◽  
Primary Bone ◽  
Anti Inflammatory ◽  
Factor C ◽  
Cyclin Dependent Kinase 5

Immune response control is critical as excessive cytokine production can be detrimental and damage the host. Interleukin-10 (Il-10), an anti-inflammatory cytokine produced primarily by macrophages, is a key regulator that counteracts and controls excessive inflammatory response. Il-10 expression is regulated through the transcription factor c-Maf. Another regulator of Il-10 production is p35, an activator of the cyclin-dependent kinase 5 (Cdk5), which decreases Il-10 production in macrophages, thus increasing inflammation. However, Cdk5 regulation of c-Maf and the involvement of Il-10 production in macrophages has not yet been investigated. We used in vitro primary bone marrow-derived macrophages (BMDMs) lacking Cdk5, stimulated them with lipopolysaccharid (LPS) and observed increased levels of c-Maf and Il-10. In an in vivo mouse model of LPS-induced endotoxemia, mice lacking Cdk5 in macrophages showed increased levels of c-Maf and elevated levels of Il-10 in lungs as well as in plasma, resulting in ameliorated survival. Taken together, we identified Cdk5 as a potential novel regulator of Il-10 production through c-Maf in macrophages under inflammatory conditions. Our results suggest that inhibition of Cdk5 enhances the c-Maf-Il-10 axis and thus potentiates improvement of anti-inflammatory therapy.

758: Inflammatory and Anti-Inflammatory Regulators alter Levels of an Inhibitor of Apoptosis (IAP), Survivin, in T-24 Bladder Cancer Cells

2007 ◽  
Vol 177 (4S) ◽  
pp. 254-254
Author(s):  
Justin J. Cohen ◽  
Bayan T. Takizawa ◽  
Hristos Z. Kaimkliotis ◽  
David J. Rosenberg ◽  
Marcia A. Wheeler ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Cancer Cells ◽  
Inhibitor Of Apoptosis ◽  
Bladder Cancer Cells ◽  
Anti Inflammatory

1216: Oral Treatment with a Vitamin D3 Analogue Shows Anti Inflammatory Effects and Reduces Bladder Overactivity in Rodent Models of Chronic Cystitis

2005 ◽  
Vol 173 (4S) ◽  
pp. 330-330
Author(s):  
Peter Zvara ◽  
Fabio Benigni ◽  
Enrico Baroni ◽  
Marija Zecevic ◽  
Antonia Monno ◽  
...  
Keyword(s):  
Vitamin D3 ◽  
Oral Treatment ◽  
Rodent Models ◽  
Chronic Cystitis ◽  
Anti Inflammatory
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