Abstract
Tracking the target: To identify a protein that binds directly to the HIF-1α inhibitor LW6, a series of new chemical probes were synthesized with a clickable tag and/or a photoactivatable moiety. LW6 was found to be localized to the mitochondria (see picture) and MDH2 was identified as a target protein of LW6. These results indicate that the HIF-1α inhibitory activity of LW6 is a consequence of MDH2 suppression.
Original language | English |
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Pages (from-to) | 10286-10289 |
Number of pages | 4 |
Journal | Angewandte Chemie - International Edition |
Volume | 52 |
Issue number | 39 |
DOIs | |
State | Published - 23 Sep 2013 |
Keywords
- click chemistry
- fluorescent probes
- HIF inhibitors
- malate dehydrogenase 2
- photoaffinity labeling