Novel copper complex inhibits the proteasome in skin squamous cell carcinoma induced by DMBA in mice.

The proteasomal system is becoming a target for the treatment of several diseases, especially in cancer therapy. The present study aims to develop a novel copper complex that inhibits the proteasome in skin squamous cell carcinoma. New molecules based on the copper complex were synthesized for the first time to assess their potential as proteasome inhibitors, specifically targeting squamous cell carcinoma induced by 7,12-dimethylbenz(a)anthracene (DMBA) in mouse models.

identification of 20S proteasome-β5 subunit inhibitors using structure-based virtual screening.

Proteasome inhibitors have effective anti-tumor activity in cell culture and can induce apoptosis by interfering with the degradation of cell cycle proteins. 20S Proteasome is acknowledged to be a satisfactory target that has persistent properties against the human immune defense and is obligatory for the degradation of some vital proteins. This study aimed to identify potential inhibitors against 20S proteasome, specifically the β5 subunit, using structure-based virtual screening and molecular docking to reduce the number of ligands that should be eligible for experimental assays.

Functional and quantitative evaluation of the 20S proteasome in serum and intracellular in145 moroccan patients with hematologic malignancies.

Background: Regulatory degradation of intracellular proteins plays an essential role in most biological processes, particularly in the control of cell proliferation and differentiation. In eukaryotes, intracellular proteolysis is largely provided by the Ubiquitin / Proteasome system. Alterations and dysfunction of protein degradation by the Ubiquitin / Proteasome system, such as transcription factors, cell cycle regulators or tumor suppressor proteins, have been linked to human.

The role of the ubiquitin-proteasome pathway in skin cancer development: 26S proteasome-activated NF-κB signal transduction.

The Ubiquitin-Proteasome System plays a central role in signal transduction associated with stress, in the skin in particular by the control of NF-κB pathways. Under normal conditions, the inhibitory protein IκB is phosphorylated by kinases, then ubiquitinated and ends up at the proteasome to be degraded. The present short review discusses recent progress in the inhibition of NF-κB activation by proteasome inhibitors prevents the degradation of protein IκB, which accumulates in the cytosol, and there by the activation of NF-κB.

Antitumor Effect of Extracts on DMBA-Induced Skin Carcinoma Are Mediated by Proteasome Inhibition.

The aim of this work is to evaluate the antitumor effect mediated by the proteasome inhibitors of extracts on skin carcinogenesis. Female Swiss albino mice were divided into five groups depending on the combination of skin cancer-inducing 7,12-dimethylbenz(a)anthracene (DMBA) and extract of treatments. Histology of the affected skin and measurement of proteasome activity were performed to demonstrate the effect of on mice.

Phytochemical screening, antioxidant activity and inhibitory potential of Ficus carica and Olea europaea leaves.

It is our interest to screen Oela europaea L and Ficus carica L leaf extract for total phenolic, flavonoid contents and to evaluate their free radical scavenging and Ferric reducing power (FRAP) using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Data shows that Olea europaea and Ficus carica have strong antioxidant potency to scavenge free radical at an optimal phenolic and flavonoid concentration. Results further suggest a strong correlation between antioxidant activities, phenolic and flavonoid contents.