Targeting furin, a cellular proprotein convertase, for COVID-19 prevention and therapeutics

Jiang, Xia; Li, Dabing; Maghsoudloo, Mazaher; Zhang, Xinghai; Ma, Wenzhe; Fu, Junjiang

doi:10.1016/j.drudis.2024.104026

Drug Discovery Today

2024

DOI: 10.1016/j.drudis.2024.104026

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Targeting furin, a cellular proprotein convertase, for COVID-19 prevention and therapeutics

Xia Jiang,

Dabing Li,

Mazaher Maghsoudloo

et al.

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2024

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Cited by 3 publications

References 106 publications

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Structural insights into Furin enzyme inhibition to block SARS-CoV-2 spike protein cleavage: an in-silico approach

Jaganathan,

Kumaradhas

2024

3 Biotech

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Structural insights into Furin enzyme inhibition to block SARS-CoV-2 spike protein cleavage: an in-silico approach

Jaganathan,

Kumaradhas

2024

3 Biotech

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A disintegrin and metalloproteinase domain 10 expression inhibition by the small molecules adenosine, cordycepin and N6, N6-dimethyladenosine and immune regulation in malignant cancers

Zhang,

Fu,

et al. 2024

Front. Immunol.

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A disintegrin and metalloproteinase domain 10 (ADAM10), a member of the ADAM family, is a cellular surface protein with potential adhesion and protease/convertase functions. The expression regulations in cancers by natural products [adenosine (AD) and its analogs, cordycepin (CD), and N6, N6-dimethyladenosine (m62A)], and immune regulation are unclear. As results, AD, CD, and m62A inhibited ADAM10 expression in various cancer cell lines, indicating their roles in anti-cancer agents. Further molecular docking with ADAM10 protein found the binding energies of all docking groups were <-7 kcal/mol for all small-molecules (AD, CD and m62A), suggesting very good binding activities. In addition, analysis of the immunomodulatory roles in cancer showed that ADAM10 was negatively correlated with immunomodulatory genes such as CCL27, CCL14, CCL25, CXCR5, HLA-B, HLA-DOB1, LAG3, TNFRSF18, and TNFRSF4 in bladder urothelial carcinoma, thymoma, breast invasive carcinoma, TGCT, kidney renal papillary cell carcinoma, SKCM and thyroid carcinoma, indicating the immune-promoting roles for ADAM10. LAG3 mRNA levels were reduced by both AD and CD in vivo. ADAM10 is also negatively associated with tumor immunosuppression and interrelated with the immune infiltration of tumors. Overall, the present study determined ADAM10 expression by AD, CD and m62A, and in AD or CD/ADAM10/LAG3 signaling in cancers, and suggested a potential method for immunotherapy of cancers by targeting ADAM10 using the small molecules AD, CD and m62A.

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Development and Prospects of Furin Inhibitors for Therapeutic Applications

Ivachtchenko,

Khvat,

Shkil

2024

IJMS

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Furin, a serine protease enzyme located in the Golgi apparatus of animal cells, plays a crucial role in cleaving precursor proteins into their mature, active forms. It is ubiquitously expressed across various tissues, including the brain, lungs, gastrointestinal tract, liver, pancreas, and reproductive organs. Since its discovery in 1990, furin has been recognized as a significant therapeutic target, leading to the active development of furin inhibitors for potential use in antiviral, antibacterial, anticancer, and other therapeutic applications. This review provides a comprehensive overview of the progress in the development and characterization of furin inhibitors, encompassing peptides, linear and macrocyclic peptidomimetics, and non-peptide compounds, highlighting their potential in the treatment of both infectious and non-infectious diseases.

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Targeting furin, a cellular proprotein convertase, for COVID-19 prevention and therapeutics

Cited by 3 publications

References 106 publications

Structural insights into Furin enzyme inhibition to block SARS-CoV-2 spike protein cleavage: an in-silico approach

Structural insights into Furin enzyme inhibition to block SARS-CoV-2 spike protein cleavage: an in-silico approach

A disintegrin and metalloproteinase domain 10 expression inhibition by the small molecules adenosine, cordycepin and N6, N6-dimethyladenosine and immune regulation in malignant cancers

Development and Prospects of Furin Inhibitors for Therapeutic Applications

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