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An enolase inhibitor for the targeted treatment of ENO1-deleted cancers

by Jiang, Yongying , Pisaneschi, Federica , Mandal, Pijus , Xu, Quanyu , Peng, Zhenghong , Wu, Qi , Hammoudi, Naima , DePinho, Ronald A. , Sun, Yuting , Asara, John M. , Zielinski, Rafal , Wang, Xiaobo , Barekatain, Yasaman , Georgiou, Dimitra K. , Khadka, Sunada , Leonard, Paul G. , Bornmann, William , Pando, Susana Castro , Czako, Barbara , Satani, Nikunj , Priebe, Waldemar , Maxwell, David , Kang, Zhijun , Yan, Victoria C. , Marszalek, Joseph R. , Arthur, Kenisha , Tran, Theresa , Muller, Florian L. , Pham, Cong-Dat , Ackroyd, Jeffrey J. , Lin, Yu-Hsi

in 631/154/309/2144 / 631/45/320 / 631/67/1922 / 631/67/2327 / Anemia / Animals / Antineoplastic Agents - therapeutic use / Biomarkers, Tumor - genetics / Biomedical and Life Sciences / Brain tumors / Cancer / Cell Line, Tumor / Cells / Competition / DNA-Binding Proteins - genetics / Enzyme Inhibitors - therapeutic use / Enzymes / Female / Gene deletion / Glioma / Glioma - drug therapy / Glioma cells / Glycolysis / Glycolysis - drug effects / Humans / Isoforms / Lethality / Life Sciences / Macaca fascicularis / Male / Metabolism / Mice / Mice, SCID / Neoplasms - drug therapy / Neoplasms - genetics / Permeability / Phosphopyruvate hydratase / Phosphopyruvate Hydratase - antagonists & inhibitors / Phosphopyruvate Hydratase - genetics / Precision Medicine / Sequence Deletion / Structure-Activity Relationship / Toxicity / Tumor Suppressor Proteins - genetics / Variance analysis / Xenograft Model Antitumor Assays

2020

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2020

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Journal Article

An enolase inhibitor for the targeted treatment of ENO1-deleted cancers

Jiang, Yongying,

Pisaneschi, Federica,

Mandal, Pijus,

Xu, Quanyu,

Peng, Zhenghong,

Wu, Qi,

Hammoudi, Naima,

DePinho, Ronald A.,

Sun, Yuting,

Asara, John M.,

Zielinski, Rafal,

Wang, Xiaobo,

Barekatain, Yasaman,

Georgiou, Dimitra K.,

Khadka, Sunada,

Leonard, Paul G.,

Bornmann, William,

Pando, Susana Castro,

Czako, Barbara,

Satani, Nikunj,

Priebe, Waldemar,

Maxwell, David,

Kang, Zhijun,

Yan, Victoria C.,

Marszalek, Joseph R.,

Arthur, Kenisha,

Tran, Theresa,

Muller, Florian L.,

Pham, Cong-Dat,

Ackroyd, Jeffrey J.,

Lin, Yu-Hsi

2020

Overview

Inhibiting glycolysis remains an aspirational approach for the treatment of cancer. We have previously identified a subset of cancers harbouring homozygous deletion of the glycolytic enzyme enolase (ENO1) that have exceptional sensitivity to inhibition of its redundant paralogue, ENO2, through a therapeutic strategy known as collateral lethality. Here, we show that a small-molecule enolase inhibitor, POMHEX, can selectively kill ENO1 -deleted glioma cells at low-nanomolar concentrations and eradicate intracranial orthotopic ENO1 -deleted tumours in mice at doses well-tolerated in non-human primates. Our data provide an in vivo proof of principle of the power of collateral lethality in precision oncology and demonstrate the utility of POMHEX for glycolysis inhibition with potential use across a range of therapeutic settings. Oncogenic transformation can render cancer cells dependent on aberrant expression of glycolytic enzyme isoforms. Lin et al. describe a novel enolase inhibitor, POMHEX, that can selectively kill ENO1 -deleted glioblastomas.

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Publisher

Nature Publishing Group UK,Nature Publishing Group

Subject

/ Anemia

/ Animals

/ Antineoplastic Agents - therapeutic use