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Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression
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| Zeitschriftentitel: | Advanced Science |
|---|---|
| Personen und Körperschaften: | , , , , , , , , , , , , |
| In: | Advanced Science, 7, 2020, 9 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
Wiley
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| Schlagwörter: |
| author_facet |
Lin, Qingxiang He, Yuan Wang, Xue Zhang, Yong Hu, Meichun Guo, Weikai He, Yundong Zhang, Tao Lai, Li Sun, Zhenliang Yi, Zhengfang Liu, Mingyao Chen, Yihua Lin, Qingxiang He, Yuan Wang, Xue Zhang, Yong Hu, Meichun Guo, Weikai He, Yundong Zhang, Tao Lai, Li Sun, Zhenliang Yi, Zhengfang Liu, Mingyao Chen, Yihua |
|---|---|
| author |
Lin, Qingxiang He, Yuan Wang, Xue Zhang, Yong Hu, Meichun Guo, Weikai He, Yundong Zhang, Tao Lai, Li Sun, Zhenliang Yi, Zhengfang Liu, Mingyao Chen, Yihua |
| spellingShingle |
Lin, Qingxiang He, Yuan Wang, Xue Zhang, Yong Hu, Meichun Guo, Weikai He, Yundong Zhang, Tao Lai, Li Sun, Zhenliang Yi, Zhengfang Liu, Mingyao Chen, Yihua Advanced Science Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression General Physics and Astronomy General Engineering Biochemistry, Genetics and Molecular Biology (miscellaneous) General Materials Science General Chemical Engineering Medicine (miscellaneous) |
| author_sort |
lin, qingxiang |
| spelling |
Lin, Qingxiang He, Yuan Wang, Xue Zhang, Yong Hu, Meichun Guo, Weikai He, Yundong Zhang, Tao Lai, Li Sun, Zhenliang Yi, Zhengfang Liu, Mingyao Chen, Yihua 2198-3844 2198-3844 Wiley General Physics and Astronomy General Engineering Biochemistry, Genetics and Molecular Biology (miscellaneous) General Materials Science General Chemical Engineering Medicine (miscellaneous) http://dx.doi.org/10.1002/advs.201903483 <jats:title>Abstract</jats:title><jats:p>Rapid metabolism differentiates cancer cells from normal cells and relies on anaplerotic pathways. However, the mechanisms of anaplerosis‐associated enzymes are rarely understood. The lack of potent and selective antimetabolism drugs restrains further clinical investigations. A small molecule ZY‐444 ((<jats:italic>N</jats:italic><jats:sup>4</jats:sup>‐((5‐(4‐(benzyloxy)phenyl)‐2‐thiophenyl)methyl)‐<jats:italic>N</jats:italic><jats:sup>2</jats:sup>‐isobutyl‐2,4‐pyrimidinediamine) is discovered to inhibit cancer cell proliferation specifically, having potent efficacies against tumor growth, metastasis, and recurrence. ZY‐444 binds to cellular pyruvate carboxylase (PC), a key anaplerotic enzyme of the tricarboxylic acid cycle, and inactivates its catalytic activity. PC inhibition suppresses breast cancer growth and metastasis through inhibiting the Wnt/β‐catenin/Snail signaling pathway. Lower PC expression in patient tumors is correlated with significant survival benefits. Comparative profiles of PC expression in cancer versus normal tissues implicate the tumor selectivity of ZY‐444. Overall, ZY‐444 holds promise therapeutically as an anti‐cancer metabolism agent.</jats:p> Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression Advanced Science |
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| title |
Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
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Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_full |
Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_fullStr |
Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_full_unstemmed |
Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_short |
Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_sort |
targeting pyruvate carboxylase by a small molecule suppresses breast cancer progression |
| topic |
General Physics and Astronomy General Engineering Biochemistry, Genetics and Molecular Biology (miscellaneous) General Materials Science General Chemical Engineering Medicine (miscellaneous) |
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http://dx.doi.org/10.1002/advs.201903483 |
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2020 |
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<jats:title>Abstract</jats:title><jats:p>Rapid metabolism differentiates cancer cells from normal cells and relies on anaplerotic pathways. However, the mechanisms of anaplerosis‐associated enzymes are rarely understood. The lack of potent and selective antimetabolism drugs restrains further clinical investigations. A small molecule ZY‐444 ((<jats:italic>N</jats:italic><jats:sup>4</jats:sup>‐((5‐(4‐(benzyloxy)phenyl)‐2‐thiophenyl)methyl)‐<jats:italic>N</jats:italic><jats:sup>2</jats:sup>‐isobutyl‐2,4‐pyrimidinediamine) is discovered to inhibit cancer cell proliferation specifically, having potent efficacies against tumor growth, metastasis, and recurrence. ZY‐444 binds to cellular pyruvate carboxylase (PC), a key anaplerotic enzyme of the tricarboxylic acid cycle, and inactivates its catalytic activity. PC inhibition suppresses breast cancer growth and metastasis through inhibiting the Wnt/β‐catenin/Snail signaling pathway. Lower PC expression in patient tumors is correlated with significant survival benefits. Comparative profiles of PC expression in cancer versus normal tissues implicate the tumor selectivity of ZY‐444. Overall, ZY‐444 holds promise therapeutically as an anti‐cancer metabolism agent.</jats:p> |
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| author | Lin, Qingxiang, He, Yuan, Wang, Xue, Zhang, Yong, Hu, Meichun, Guo, Weikai, He, Yundong, Zhang, Tao, Lai, Li, Sun, Zhenliang, Yi, Zhengfang, Liu, Mingyao, Chen, Yihua |
| author_facet | Lin, Qingxiang, He, Yuan, Wang, Xue, Zhang, Yong, Hu, Meichun, Guo, Weikai, He, Yundong, Zhang, Tao, Lai, Li, Sun, Zhenliang, Yi, Zhengfang, Liu, Mingyao, Chen, Yihua, Lin, Qingxiang, He, Yuan, Wang, Xue, Zhang, Yong, Hu, Meichun, Guo, Weikai, He, Yundong, Zhang, Tao, Lai, Li, Sun, Zhenliang, Yi, Zhengfang, Liu, Mingyao, Chen, Yihua |
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| description | <jats:title>Abstract</jats:title><jats:p>Rapid metabolism differentiates cancer cells from normal cells and relies on anaplerotic pathways. However, the mechanisms of anaplerosis‐associated enzymes are rarely understood. The lack of potent and selective antimetabolism drugs restrains further clinical investigations. A small molecule ZY‐444 ((<jats:italic>N</jats:italic><jats:sup>4</jats:sup>‐((5‐(4‐(benzyloxy)phenyl)‐2‐thiophenyl)methyl)‐<jats:italic>N</jats:italic><jats:sup>2</jats:sup>‐isobutyl‐2,4‐pyrimidinediamine) is discovered to inhibit cancer cell proliferation specifically, having potent efficacies against tumor growth, metastasis, and recurrence. ZY‐444 binds to cellular pyruvate carboxylase (PC), a key anaplerotic enzyme of the tricarboxylic acid cycle, and inactivates its catalytic activity. PC inhibition suppresses breast cancer growth and metastasis through inhibiting the Wnt/β‐catenin/Snail signaling pathway. Lower PC expression in patient tumors is correlated with significant survival benefits. Comparative profiles of PC expression in cancer versus normal tissues implicate the tumor selectivity of ZY‐444. Overall, ZY‐444 holds promise therapeutically as an anti‐cancer metabolism agent.</jats:p> |
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| spelling | Lin, Qingxiang He, Yuan Wang, Xue Zhang, Yong Hu, Meichun Guo, Weikai He, Yundong Zhang, Tao Lai, Li Sun, Zhenliang Yi, Zhengfang Liu, Mingyao Chen, Yihua 2198-3844 2198-3844 Wiley General Physics and Astronomy General Engineering Biochemistry, Genetics and Molecular Biology (miscellaneous) General Materials Science General Chemical Engineering Medicine (miscellaneous) http://dx.doi.org/10.1002/advs.201903483 <jats:title>Abstract</jats:title><jats:p>Rapid metabolism differentiates cancer cells from normal cells and relies on anaplerotic pathways. However, the mechanisms of anaplerosis‐associated enzymes are rarely understood. The lack of potent and selective antimetabolism drugs restrains further clinical investigations. A small molecule ZY‐444 ((<jats:italic>N</jats:italic><jats:sup>4</jats:sup>‐((5‐(4‐(benzyloxy)phenyl)‐2‐thiophenyl)methyl)‐<jats:italic>N</jats:italic><jats:sup>2</jats:sup>‐isobutyl‐2,4‐pyrimidinediamine) is discovered to inhibit cancer cell proliferation specifically, having potent efficacies against tumor growth, metastasis, and recurrence. ZY‐444 binds to cellular pyruvate carboxylase (PC), a key anaplerotic enzyme of the tricarboxylic acid cycle, and inactivates its catalytic activity. PC inhibition suppresses breast cancer growth and metastasis through inhibiting the Wnt/β‐catenin/Snail signaling pathway. Lower PC expression in patient tumors is correlated with significant survival benefits. Comparative profiles of PC expression in cancer versus normal tissues implicate the tumor selectivity of ZY‐444. Overall, ZY‐444 holds promise therapeutically as an anti‐cancer metabolism agent.</jats:p> Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression Advanced Science |
| spellingShingle | Lin, Qingxiang, He, Yuan, Wang, Xue, Zhang, Yong, Hu, Meichun, Guo, Weikai, He, Yundong, Zhang, Tao, Lai, Li, Sun, Zhenliang, Yi, Zhengfang, Liu, Mingyao, Chen, Yihua, Advanced Science, Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression, General Physics and Astronomy, General Engineering, Biochemistry, Genetics and Molecular Biology (miscellaneous), General Materials Science, General Chemical Engineering, Medicine (miscellaneous) |
| title | Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_full | Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_fullStr | Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_full_unstemmed | Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_short | Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| title_sort | targeting pyruvate carboxylase by a small molecule suppresses breast cancer progression |
| title_unstemmed | Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Breast Cancer Progression |
| topic | General Physics and Astronomy, General Engineering, Biochemistry, Genetics and Molecular Biology (miscellaneous), General Materials Science, General Chemical Engineering, Medicine (miscellaneous) |
| url | http://dx.doi.org/10.1002/advs.201903483 |