Article ; Online: KI04 an Aminoglycosides-Derived Molecule Acts as an Inhibitor of Human Connexin46 Hemichannels Expressed in HeLa Cells.
2023 Volume 13, Issue 3
Abstract: Background: Connexins (Cxs) are proteins that help cells to communicate with the extracellular media and with the cytoplasm of neighboring cells. Despite their importance in several human physiological and pathological conditions, their pharmacology is ... ...
Abstract | Background: Connexins (Cxs) are proteins that help cells to communicate with the extracellular media and with the cytoplasm of neighboring cells. Despite their importance in several human physiological and pathological conditions, their pharmacology is very poor. In the last decade, some molecules derived from aminoglycosides have been developed as inhibitors of Cxs hemichannels. However, these studies have been performed in Methods: We transfected HeLa cells with the human Cx46tGFP and characterized the effect of a kanamycin-derived molecule (KI04) on Cx46 hemichannel activity by time-lapse recordings, changes in phosphorylation by Western blot, localization by epifluorescence, and possible binding sites by molecular dynamics (MD). Results: We observed that kanamycin and KI04 were the most potent inhibitors of Cx46 hemichannels among several aminoglycosides, presenting an IC Results: These results demonstrate that KI04 could be used as a Cx46 inhibitor and could help to develop future selective Cx46 inhibitors. |
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MeSH term(s) | Animals ; Humans ; HeLa Cells ; Aminoglycosides ; Escherichia coli/metabolism ; Connexins/metabolism ; Anti-Bacterial Agents ; Kanamycin/pharmacology ; Mammals/metabolism |
Chemical Substances | GJA3 protein, human ; Aminoglycosides ; Connexins ; Anti-Bacterial Agents ; Kanamycin (59-01-8) |
Language | English |
Publishing date | 2023-02-22 |
Publishing country | Switzerland |
Document type | Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S. |
ZDB-ID | 2701262-1 |
ISSN | 2218-273X ; 2218-273X |
ISSN (online) | 2218-273X |
ISSN | 2218-273X |
DOI | 10.3390/biom13030411 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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