Rational design of selective allosteric inhibitors of PHGDH and serine synthesis with anti-tumor activity
Wang, Qian, Liberti, Maria V., Liu, Pei, Deng, Xiaobing, Liu, Ying, Locasale, Jason W., Lai, Luhua·2017·Cell Chemical Biology
Cited by (156)
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- The “serine code” of metabolic reprogramming: multidimensional roles of the serine synthesis pathway in tumors and novel breakthroughs for targeted therapyPeng Su, Ying Yang, Hong Zheng · 2026 · Frontiers in Immunology
- Parkin on serine: a Parkinson disease gene suppresses serine synthesis in cancerWilliam Brian Dalton · 2020 · Journal of Clinical Investigation
- Cancer MetabolismMichael A. Reid, Sydney M. Sanderson, Jason W. Locasale · 2020 · Elsevier eBooks
- Efficient Inhibition of SmNACE by Coordination Complexes Is Abolished by S. mansoni Sequestration of MetalHélène Muller‐Steffner, Sylvain A. Jacques, Isabelle Kuhn, Michael D. Schultz, Davide Botta, Paul Osswald, Clarisse Maechling, Frances E. Lund, Esther Kellenberger · 2017 · ACS Chemical Biology
- Modifying dietary amino acids in cancer patientsJosephine Connolly-Schoonen, Steven F. Biamonte, Lorraine Danowski, David C. Montrose · 2022 · International review of cytology
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- Serine synthesis pathway upregulated by E-cadherin is essential for the proliferation and metastasis of breast cancersGeonhui Lee, Claudia Wong, Anna Cho, Junior J. West, Ashleigh J. Crawford, Gabriella C. Russo, Bishwa Ranjan Si, Jung-Woo Kim, Lauren A. Hoffner, Cholsoon Jang et al. · 2023 · bioRxiv (Cold Spring Harbor Laboratory)
- Reprogramming of amino acid metabolism in breast cancerMeijin Wang, Yunlu Zhang, Zhenhua Li, Li Fu · 2025 · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer
- Emerging roles for methionine metabolism in immune cell fate and functionShaojuan Liu, Xiao‐Tian Tang, Min Huang, Jianian Tang, Yiwen Yang · 2025 · Frontiers in Immunology
- Synthesis and biological evaluation of innovative thiourea derivatives as PHGDH inhibitorsJiawei Xiang, Lei Tao, Yue Zhou, Yuping Tan, Zicheng Li, Yinglan Zhao, Qingxiang Sun, Youfu Luo · 2020 · Chemical Papers
- Expression of Glucose Metabolism-Related Proteins in Adrenal NeoplasmsEun‐Kyung Kim, Hye Min Kim, Ja Seung Koo · 2021 · Pathobiology
- Designing Cyclic-Constrained Peptides to Inhibit Human Phosphoglycerate DehydrogenaseXiaoyu Qing, Qian Wang, Hanyu Xu, Pei Liu, Luhua Lai · 2023 · Molecules
- ICBS 2017 in Shanghai—Illuminating Life with Chemical InnovationQi Zhang, Lixin Zhang, Evripidis Gavathiotis · 2018 · ACS Chemical Biology
- Targeting serine metabolism vulnerability in omipalisib-resistant acute myeloid leukemia with phosphoglycerate dehydrogenase inhibitorsChi-Yang Tseng, Yu-Hsuan Fu, Da‐Liang Ou, Hsin‐An Hou, Hsiung–Fei Chien, Liang‐In Lin · 2025 · Biomedicine & Pharmacotherapy
- Structure‐Based Computational Approach in Search of the Potent Molecules Targeting Phosphoglycerate Dehydrogenase (PHGDH) Enzyme for Cancer TreatmentPriyanka Solanki, Anu Manhas, Dhaval Patel, Prakash Chandra Jha · 2024 · ChemistrySelect
- The role of one-carbon amino acids in tumor-immune metabolism: From oncogenesis to therapySuchandrima Saha, Monisankar Ghosh · 2024 · Elsevier eBooks
- Establishment of inhibitor screening and validation system for tryptophanyl tRNA synthetase using surface plasmon resonanceQian Wang, Guiwang Zhu, Zhenming Liu · 2021 · Analytical Biochemistry
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- Tumor metabolic adaptation induced by L-asparaginase reveals a vulnerability to PARP1/2 inhibitor in B-cell lymphomasAussel Anaïs, Ivan Nemazanyy, Ashaina Vandenberghe, Pauline Meola, Dorat Noémie, Rachel Paul, Lama Habbouche, Laurie Exposito, Nicolas Nottet, Virginie Pétrilli et al. · 2026 · Nature Communications
- The Role of One‐Carbon Metabolism in Cancer and Its Therapeutic SignificanceYuting Jiang, Guoliang Zhou, Qian Zhang, Shengtao Zhou · 2026 · MedComm – Oncology
- Surface plasmon resonance in drug discovery: advances in protein-protein interaction and its kinetic analysisDiwakar Kumar Singh, Sameer Tiwari, Kumari Kripalata · 2026 · Discover Chemistry.
- L-asparaginase treatment induces a tumor metabolic plasticity and reveals a vulnerability to PARP1/2 inhibitor Olaparib, in B-cell lymphomasAussel Anaïs, Ivan Nemazanyy, Ashaina Vandenberghe, Pauline Meola, Dorat Noémie, Rachel Paul, Lama Habbouche, Laurie Exposito, Nicolas Nottet, Virginie Pétrilli et al. · 2025 · bioRxiv (Cold Spring Harbor Laboratory)
- Targeting Antioxidant Systems to Treat Pancreatic CancerFrancesco Gabriele Tatangelo Fazzari · 2018 · TSpace (University of Toronto)
- Faculty Opinions recommendation of Serine synthesis through PHGDH coordinates nucleotide levels by maintaining central carbon metabolism.Hans van Beek · 2019 · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature
- Mechanism Reveals a Novel Site for Allosteric Inhibition of Carcinogenic Activity of Human 3-Phosphoglycerate DehydrogenaseAnkita Tripathi, Qinghua Liao, Kshatresh Dutta Dubey · 2023 · ChemRxiv
- Additional file 6 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Min Liu, Paloma González‐Sánchez, Bo-Hyun Choi, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Additional file 7 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Min Liu, Paloma González‐Sánchez, Bo-Hyun Choi, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Additional file 5 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Min Liu, Paloma González‐Sánchez, Bo-Hyun Choi, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Additional file 8 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Min Liu, Paloma González‐Sánchez, Bo-Hyun Choi, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Prognostic value of serum phosphoglycerate dehydrogenase and glycine levels in breast cancerHussam Abd Jassem, Anwar Jasib Thaaban · 2024 · Menopause Review/Przegląd Menopauzalny
- Additional file 4 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Liu, Min, Paloma González‐Sánchez, Choi, Bo-Hyun, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Additional file 1 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Liu, Min, Paloma González‐Sánchez, Choi, Bo-Hyun, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Additional file 2 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Liu, Min, Paloma González‐Sánchez, Choi, Bo-Hyun, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Additional file 3 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasisYun Pyo Kang, Aimee Falzone, Liu, Min, Paloma González‐Sánchez, Choi, Bo-Hyun, Jonathan L. Coloff, James Joseph Saller, Florian A. Karreth, Gina M. DeNicola · 2020 · Figshare
- Physical–chemical approach to identify local structural determinants of molecular mechanisms: Case study of antimalarial drug pyronaridine and crystal-growth inhibitionAngela Medvedeva, Ksenia Kolomeisky, Anatoly B. Kolomeisky · 2026 · The Journal of Chemical Physics
- PHGDH: a metabolic switch in tumor drug resistance and a therapeutic targetSong-Song Shi, Si-Yi Chen, Wen Zhang, Guo-Wu Rao, Quan Zheng · 2026 · Drug Discovery Today
- Complexe SWI/SNF et cancer _ Altérations génétiques et anomalies métaboliquesJulien Masliah‐Planchon · 2018 · theses.fr (ABES)
- Metabolic plasticity in the pancreatic cancer metastatic cascadeBiwen Zhu, Yibing Guo, Yuhua Lu · 2026 · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer
- Structure-Based Design and Optimization of Novel PHGDH Inhibitors for Overcoming Erlotinib-Resistant Lung CancerXingmei Wu, Tang, Y Yan, Xinyu Cao, Yixin Cen, Xiaojing Lan, Y C Zhu, Da‐Yu Shi, Guo‐Qiang Lin, Ping Tian et al. · 2026 · Journal of Medicinal Chemistry
- Discovery of a Covalent Inhibitor Targeting the PHGDH Dimer Interface with Antitumor EfficacyLei Feng, Liu Y, Yiwei Zhang, Zhongjiao Fan, Xinyuan Wu, Xiancheng Yang, Leyi Liu, Zhibei Qu, Ye Shen, Xiaojie Lu et al. · 2026 · Journal of Medicinal Chemistry
- Tumoral Metabolism at the Intersection of Oncogene Signaling, Epigenetics and Immunology: Emerging Therapeutic Strategies in CancerBhoomendra A. Bhongade, Areeg Anwer Ali, Mohamed El‐Tanani, Shakta Mani Satyam, Sirajunisa Talath, Adil Farooq Wali, Syed Arman Rabbani, Walaa Ibraheem, Karolina Hoffmann, Авагимян Ашот Арманович et al. · 2026 · Current Issues in Molecular Biology
- Tumor-intrinsic PHGDH inhibition sensitizes colorectal cancer to PD-1 blockade via α-ketoglutarate–mediated macrophage reprogrammingJieping Qiu, Jingwen Wei, Jiaming Liu, Jing Bai, Keqin Tan, Yuhao Wei, Haorui Zhou, Lusi Feng, Qianlong Kang, Huan Tong et al. · 2026 · Drug Resistance Updates
- Immunometabolism and rheumatic disease—advancing targeted therapiesMark Robin Boothby · 2026 · EULAR Rheumatology Open
- BindingDB Entry 50022425: Applications of oxetanes in drug discovery and medicinal chemistry.BindingDB · 2025 · UC San Diego
- BindingDB Entry 50001186: Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50019189: Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy.BindingDB · 2024 · UC San Diego
- BindingDB Entry 15: Efficient Inhibition of SmNACE by Coordination Complexes Is Abolished by S. mansoni Sequestration of Metal.BindingDB · 2018 · UC San Diego
- BindingDB Entry 50018393: A retrospective overview of PHGDH and its inhibitors for regulating cancer metabolism.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50008414: Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) InhibitorBindingDB · 2021 · UC San Diego
- The Role of D-3-Phosphoglycerate Dehydrogenase (PHGDH) in Chemoresistance in Ovarian Cancer: Molecular Insights and Therapeutic PotentialJesús Omar Velázquez-Moreno, María de la Luz Mejía-Aguayo, Felix De Dios Padre Casarrubias-Jaimes, Marcela Angélica De la Fuente-Hernández, Daniel de Jesús Apolonio-Sánchez, Rodrigo Sosa-León, Rosa María Álvarez-Gómez, Marco Antonio Leyva‐Vázquez, Abraham Pedroza‐Torres, Olga Lilia Garibay‐Cerdenares · 2026 · International Journal of Molecular Sciences