Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

Chao Yang; Wanhe Wang; Linmin Chen; Jiaxin Liang; Sheng Lin; Ming Yuen Lee; Dik Lung Ma; Chung Hang Leung

doi:10.1039/c6cc04938a

Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

Chao Yang
, Wanhe Wang
, Linmin Chen
, Jiaxin Liang
, Sheng Lin
, Ming Yuen Lee
, Dik Lung Ma^*
, Chung Hang Leung^*

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

40 Citations (Scopus)

Abstract

We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL-HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL-HIF1α interaction.

Original language	English
Pages (from-to)	12837-12840
Number of pages	4
Journal	Chemical Communications
Volume	52
Issue number	87
Early online date	5 Oct 2016
DOIs	https://doi.org/10.1039/c6cc04938a
Publication status	Published - 11 Nov 2016

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10.1039/c6cc04938a

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@article{36c03d0784fa4f6fbaea41bb42489af2,

title = "Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening",

abstract = "We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL-HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL-HIF1α interaction.",

author = "Chao Yang and Wanhe Wang and Linmin Chen and Jiaxin Liang and Sheng Lin and Lee, \{Ming Yuen\} and Ma, \{Dik Lung\} and Leung, \{Chung Hang\}",

note = "Funding Information: This work was supported by Hong Kong Baptist University (FRG2/15-16/002), the Health and Medical Research Fund (HMRF/14130522), the Research Grants Council (HKBU/12301115, HKBU/204612, and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme(A-HKBU201/12-Oligoswitch), the National Natural Science Foundation of China (21575121), the Guangdong Province Natural Science Foundation (2015A030313816), the Hong Kong Baptist University Century Club Sponsorship Scheme 2016, the Interdisciplinary Research Matching Scheme (RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (098/2014/A2), (MYRG2015-00137-ICMSQRCM, MRG044/LCH/2015/ICMS). Publisher copyright: {\textcopyright} The Royal Society of Chemistry 2016",

year = "2016",

month = nov,

day = "11",

doi = "10.1039/c6cc04938a",

language = "English",

volume = "52",

pages = "12837--12840",

journal = "Chemical Communications",

issn = "1359-7345",

publisher = "Royal Society of Chemistry",

number = "87",

}

TY - JOUR

T1 - Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

AU - Yang, Chao

AU - Wang, Wanhe

AU - Chen, Linmin

AU - Liang, Jiaxin

AU - Lin, Sheng

AU - Lee, Ming Yuen

AU - Ma, Dik Lung

AU - Leung, Chung Hang

N1 - Funding Information: This work was supported by Hong Kong Baptist University (FRG2/15-16/002), the Health and Medical Research Fund (HMRF/14130522), the Research Grants Council (HKBU/12301115, HKBU/204612, and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme(A-HKBU201/12-Oligoswitch), the National Natural Science Foundation of China (21575121), the Guangdong Province Natural Science Foundation (2015A030313816), the Hong Kong Baptist University Century Club Sponsorship Scheme 2016, the Interdisciplinary Research Matching Scheme (RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (098/2014/A2), (MYRG2015-00137-ICMSQRCM, MRG044/LCH/2015/ICMS). Publisher copyright: © The Royal Society of Chemistry 2016

PY - 2016/11/11

Y1 - 2016/11/11

N2 - We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL-HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL-HIF1α interaction.

AB - We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL-HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL-HIF1α interaction.

UR - https://www.scopus.com/pages/publications/84992695221

U2 - 10.1039/c6cc04938a

DO - 10.1039/c6cc04938a

M3 - Journal article

C2 - 27709157

AN - SCOPUS:84992695221

SN - 1359-7345

VL - 52

SP - 12837

EP - 12840

JO - Chemical Communications

JF - Chemical Communications

IS - 87

ER -

Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

Abstract

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