Identification of malate dehydrogenase 2 as a target protein of the HIF-1 inhibitor LW6 using chemical probes

Kyeong Lee, Hyun Seung Ban, Ravi Naik, Ye Seul Hong, Seohyun Son, Bo Kyung Kim, Yan Xia, Kyung Bin Song, Hong Sub Lee, Misun Won

Research output: Contribution to journalArticlepeer-review

86 Scopus citations

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 languageEnglish
Pages (from-to)10286-10289
Number of pages4
JournalAngewandte Chemie - International Edition
Volume52
Issue number39
DOIs
StatePublished - 23 Sep 2013

Keywords

  • click chemistry
  • fluorescent probes
  • HIF inhibitors
  • malate dehydrogenase 2
  • photoaffinity labeling

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