Autor: |
Mattia Mori, Stefano Ciaco, Yves Mély, Anastasia Karioti |
Jazyk: |
angličtina |
Rok vydání: |
2020 |
Předmět: |
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Zdroj: |
Molecules, Vol 25, Iss 22, p 5434 (2020) |
Druh dokumentu: |
article |
ISSN: |
1420-3049 |
DOI: |
10.3390/molecules25225434 |
Popis: |
The HIV-1 nucleocapsid protein (NC) is a desirable target in antiretroviral therapy due to its high conservation among HIV-1 strains, and to its multiple and crucial roles in the HIV-1 replication cycle. Natural products represent a valuable source of NC inhibitors, with the catechol group being a privileged scaffold in NC inhibition. By coupling molecular modeling with NMR spectroscopy and fluorescence-based assays, we disclosed lithospermic acid, a catechol derivative extracted from Salvia miltiorrhizza, as a potent and chemically stable non-covalent inhibitor of the NC. Being different from other catechol derivative reported so far, lithospermic acid does not undergo spontaneous oxidation in physiological conditions, thus becoming a profitable starting point for the development of efficient NC inhibitors. |
Databáze: |
Directory of Open Access Journals |
Externí odkaz: |
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