Targeting mPGES-1 as a New Strategy against Neuroblastoma

Comunanza, Valentina

doi:10.1016/j.ebiom.2018.06.008

Cited by 2 publications

(1 citation statement)

References 8 publications

(8 reference statements)

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“…COX-2 has been described as a critical element in the crosstalk between cancer and inflammation in NB and other solid tumors 18 . However, the mechanisms involving COX-2 in tumorigenesis and the therapeutic significance of COX-2 inhibition remain elusive, especially in pediatric tumors 16,30,36,37 . It is not clear, for instance, if leukotriene inhibitors would be safe and effective as adjuvant therapy, at what phase of treatment, or what molecular interactions could be affected by its inhibition.…”

Section: Discussionmentioning

confidence: 99%

Integrative analysis reveals an indirect connection between COX-2/PTGS2 and extracellular matrix proteins in Ch11q-deleted neuroblastoma

Nascimento¹,

Júnior²,

Poncio³

et al. 2021

Preprint

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The COX-2 protein, encoded by the PTGS2 gene, is related to tumor progression in adult and pediatric cancer. In neuroblastoma (NB), COX-2 was associated with loss of heterozygosity on the long arm of chromosome 11 (Ch11q loss of heterozygosity, LOH), defining a subset of aggressive disease. The present study aimed to investigate the protein expression of COX-2 in a set of 82 pre-chemotherapy (CT) and 20 post-CT NB specimens and its correlation with clinical and genomic data. A systems biology approach elucidated the network interaction of PTGS2 and other inflammation-related genes with those codified in the Ch11q deleted regions. The results indicated a significantly higher expression of COX-2 in post-CT samples. In addition, a significant positive correlation between the presence of aberrations in Ch11q and COX-2 levels and an indirect connection between the COX-2 gene and extracellular matrix remodeling (ECM)-related proteins were observed. Our findings suggest that deregulation of ECM proteolysis in Ch11q–deleted NB could elicit stromal alterations, triggering inflammatory responses via COX-2 overexpression, ultimately supporting NB progression.

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Section: Discussionmentioning

confidence: 99%

Integrative analysis reveals an indirect connection between COX-2/PTGS2 and extracellular matrix proteins in Ch11q-deleted neuroblastoma

Nascimento¹,

Júnior²,

Poncio³

et al. 2021

Preprint

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Synthesis and Anticancer Activity of Novel Thiazolo-Coumarin Derivatives

2022

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As a starting point for creating new inhibitor scaffolds, a molecular hybridization approach was applied in designing the novel molecules using coumarin-thiazole hybrids as mPGES-1 enzyme inhibitors. Thus, in present work, the novel thiazolo coumarin derivatives (8-35) were synthesized and characterized by 1H NMR, IR and ESI-MS spectra. All the synthesized molecules (8-35) were also investigated for their anticancer activity on MCF-7 (breast cancer), caco-2 (colon cancer), HeLa (Cervix cancer) cell lines. Studies revealed that compounds (8-14) and (22-28) showed inhibition (IC50) at different concentrations of 12.5, 50, 100 μg/mL and more than 100 μg/mL.

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Targeting mPGES-1 as a New Strategy against Neuroblastoma

Cited by 2 publications

References 8 publications

Integrative analysis reveals an indirect connection between COX-2/PTGS2 and extracellular matrix proteins in Ch11q-deleted neuroblastoma

Integrative analysis reveals an indirect connection between COX-2/PTGS2 and extracellular matrix proteins in Ch11q-deleted neuroblastoma

Synthesis and Anticancer Activity of Novel Thiazolo-Coumarin Derivatives

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