Publication: Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection
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Asquith, C. R. M., Sil, B. C., Laitinen, T., Tizzard, G. J., Coles, S. J., Poso, A., Hofmann-Lehmann, R., & Hilton, S. T. (2019). Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. Bioorganic & Medicinal Chemistry, 27(18), 4174–4184. https://doi.org/10.1016/j.bmc.2019.07.047
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Focused libraries of multi-substituted epidithiodiketopiperazines (ETP) were prepared and evaluated for efficacy of inhibiting the nucleocapsid protein function of the Feline Immunodeficiency Virus (FIV) as a model for HIV. This activity was compared and contrasted to observed toxicity utilising an in-vitro cell culture approach. This resulted in the identification of several promising lead compounds with nanomolar potency in cells with low toxicity and a favorable therapeutic index.
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- Asquith, Christopher R M
- Sil, Bruno C
- Laitinen, Tuomo
- Tizzard, Graham J
- Coles, Simon J
- Poso, Antti
- Hilton, Stephen T
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Asquith, C. R. M., Sil, B. C., Laitinen, T., Tizzard, G. J., Coles, S. J., Poso, A., Hofmann-Lehmann, R., & Hilton, S. T. (2019). Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. Bioorganic & Medicinal Chemistry, 27(18), 4174–4184. https://doi.org/10.1016/j.bmc.2019.07.047
