Identification of Malate Dehydrogenase2 as a Target Protein of the HIF-1 Inhibitor LW6 using Chemical Probes

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 and MDH2 was identified as a target protein of LW6. Th...

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Published inAngewandte Chemie International Edition Vol. 52; no. 39; p. 10286
Main Authors Lee, Kyeong, Ban, Hyun Seung, Naik, Ravi, Hong, Ye Seul, Son, Seohyun, Kim, Bo-Kyung, Xia, Yan, Song, Kyung Bin, Lee, Hong-Sub, Won, Misun
Format Journal Article
LanguageEnglish
Published Weinheim Wiley Subscription Services, Inc 23.09.2013
EditionInternational ed. in English
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Summary: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 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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201304987