PURPOSE Targeting enhancer of zeste homolog 2 (EZH2) can represent a hopeful strategy for oncothe... more PURPOSE Targeting enhancer of zeste homolog 2 (EZH2) can represent a hopeful strategy for oncotherapy. Also, the use of PLGA-based nanoparticles as a novel and rate-controlling carrier system was of our concern. METHODS Benzimidazole derivatives were synthesized, and their structures were clarified. In vitro antitumor activity was evaluated. Then, a modeling study was performed to investigate the ability of the most active compounds to recognize EZH2 active sites. Compound 30 (Drug) was selected to conduct pre-formulation studies and then it was incorporated into polymeric PLGA nanoparticles (NPs). NPs were then fully characterized to select an optimized formula (NP4) that subjected to further evaluation regarding antitumor activity and protein expression levels of EZH2 and EpCAM. RESULTS The results showed the antitumor activity of some synthesized derivatives. Docking outcomes demonstrated that Compound 30 was able to identify EZH2 active sites. NP4 exhibited promising findings and proved to keep the antitumor activity of Compound 30. HEPG-2 was the most sensitive for both Drug and NP4. Protein analysis indicated that Drug and NP4 had targeted EZH2 and the downstream signaling pathway to decline of EpCAM expression. CONCLUSIONS Targeting EZH2 by Compound 30 has potential use in the treatment of cancer especially hepatocellular carcinoma.
Canadian Institute for Knowledge Development (CIKD), 2021
The current pandemic of COVID-19 is considered a worldwide threat to public health caused by a no... more The current pandemic of COVID-19 is considered a worldwide threat to public health caused by a novel type of coronaviridae family called SARS-CoV-2. Owing to the urge of finding a treatment for this virulent virus, many aspects of drug development are swept aside. This review aimed to clarify the double-edged sword of drug repurposing in COVID-19 via summarizing the available treatment options and promising candidates for COVID-19 based on drug repurposing preclinical studies and in-silico approach. Different drugs target SARS CoV-2 main structures under clinical investigation; some showed limited efficacy and severe side effects, while others can be promising solutions. Some drugs suppress the cytokine storm and modulate immune response during viral infection, including anti-interleukin and glucocorticoids. Antiparasitic agents are repurposed for SARS-CoV-2 infection management. Various vaccines and monoclonal antibodies are designed against SARS-CoV-2 and are being evaluated in di...
PURPOSE Targeting enhancer of zeste homolog 2 (EZH2) can represent a hopeful strategy for oncothe... more PURPOSE Targeting enhancer of zeste homolog 2 (EZH2) can represent a hopeful strategy for oncotherapy. Also, the use of PLGA-based nanoparticles as a novel and rate-controlling carrier system was of our concern. METHODS Benzimidazole derivatives were synthesized, and their structures were clarified. In vitro antitumor activity was evaluated. Then, a modeling study was performed to investigate the ability of the most active compounds to recognize EZH2 active sites. Compound 30 (Drug) was selected to conduct pre-formulation studies and then it was incorporated into polymeric PLGA nanoparticles (NPs). NPs were then fully characterized to select an optimized formula (NP4) that subjected to further evaluation regarding antitumor activity and protein expression levels of EZH2 and EpCAM. RESULTS The results showed the antitumor activity of some synthesized derivatives. Docking outcomes demonstrated that Compound 30 was able to identify EZH2 active sites. NP4 exhibited promising findings and proved to keep the antitumor activity of Compound 30. HEPG-2 was the most sensitive for both Drug and NP4. Protein analysis indicated that Drug and NP4 had targeted EZH2 and the downstream signaling pathway to decline of EpCAM expression. CONCLUSIONS Targeting EZH2 by Compound 30 has potential use in the treatment of cancer especially hepatocellular carcinoma.
Canadian Institute for Knowledge Development (CIKD), 2021
The current pandemic of COVID-19 is considered a worldwide threat to public health caused by a no... more The current pandemic of COVID-19 is considered a worldwide threat to public health caused by a novel type of coronaviridae family called SARS-CoV-2. Owing to the urge of finding a treatment for this virulent virus, many aspects of drug development are swept aside. This review aimed to clarify the double-edged sword of drug repurposing in COVID-19 via summarizing the available treatment options and promising candidates for COVID-19 based on drug repurposing preclinical studies and in-silico approach. Different drugs target SARS CoV-2 main structures under clinical investigation; some showed limited efficacy and severe side effects, while others can be promising solutions. Some drugs suppress the cytokine storm and modulate immune response during viral infection, including anti-interleukin and glucocorticoids. Antiparasitic agents are repurposed for SARS-CoV-2 infection management. Various vaccines and monoclonal antibodies are designed against SARS-CoV-2 and are being evaluated in di...
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