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

doi:10.1002/anie.201304987

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

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

95 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 language	English
Pages (from-to)	10286-10289
Number of pages	4
Journal	Angewandte Chemie - International Edition
Volume	52
Issue number	39
DOIs	https://doi.org/10.1002/anie.201304987
State	Published - 23 Sep 2013

Keywords

click chemistry
fluorescent probes
HIF inhibitors
malate dehydrogenase 2
photoaffinity labeling

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10.1002/anie.201304987

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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.",

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author = "Kyeong Lee and Ban, \{Hyun Seung\} and Ravi Naik and Hong, \{Ye Seul\} and Seohyun Son and Kim, \{Bo Kyung\} and Yan Xia and Song, \{Kyung Bin\} and Lee, \{Hong Sub\} and Misun Won",

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AU - Lee, Kyeong

AU - Ban, Hyun Seung

AU - Naik, Ravi

AU - Hong, Ye Seul

AU - Son, Seohyun

AU - Kim, Bo Kyung

AU - Xia, Yan

AU - Song, Kyung Bin

AU - Lee, Hong Sub

AU - Won, Misun

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AB - 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.

KW - click chemistry

KW - fluorescent probes

KW - HIF inhibitors

KW - malate dehydrogenase 2

KW - photoaffinity labeling

UR - https://www.scopus.com/pages/publications/84884824876

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DO - 10.1002/anie.201304987

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JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 39

ER -

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

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Keywords

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