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)

Items 101–156 of 156

  1. Discovery of novel inhibitors of human phosphoglycerate dehydrogenase by activity-directed combinatorial chemical synthesis strategy
    Xia Zhou, Yuping Tan, Kun Gou, Lei Tao, Yuan Luo, Yue Zhou, Zeping Zuo, Qingxiang Sun, Youfu Luo, Yinglan Zhao · 2021 · Bioorganic Chemistry
  2. Correlation Between Allosteric and Orthosteric Sites
    Weilin Zhang, Juan Xie, Luhua Lai · 2019 · Advances in experimental medicine and biology
  3. Targeting metabolic pathway enhance CAR-T potency for solid tumor
    Wenying Li, Jiannan Chen, Zhigang Guo · 2024 · International Immunopharmacology
  4. Dynamic remodeling of amino acid metabolism in tumor-associated macrophages: Fueling immunosuppression, reshaping tumor niches, and unlocking metabolic checkpoints
    Beibei Ran, Lingjun Xiao, Yan Liu, Chenglin Zhang, Lingkai Kong, Yuxin Zhang, Xiaosong Gu, Chunping Jiang, Junhua Wu · 2025 · Journal of Advanced Research
  5. The “serine code” of metabolic reprogramming: multidimensional roles of the serine synthesis pathway in tumors and novel breakthroughs for targeted therapy
    Peng Su, Ying Yang, Hong Zheng · 2026 · Frontiers in Immunology
  6. Parkin on serine: a Parkinson disease gene suppresses serine synthesis in cancer
    William Brian Dalton · 2020 · Journal of Clinical Investigation
  7. Cancer Metabolism
    Michael A. Reid, Sydney M. Sanderson, Jason W. Locasale · 2020 · Elsevier eBooks
  8. Efficient Inhibition of SmNACE by Coordination Complexes Is Abolished by S. mansoni Sequestration of Metal
    Hélène 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
  9. Modifying dietary amino acids in cancer patients
    Josephine Connolly-Schoonen, Steven F. Biamonte, Lorraine Danowski, David C. Montrose · 2022 · International review of cytology
  10. Integrated Metabolomics and Transcriptomics Analysis of Anacardic Acid Inhibition of Breast Cancer Cell Viability
    Kellianne M. Piell, Claire C. Poulton, Christian G. Stanley, David J. Schultz, Carolyn M. Klinge · 2024 · International Journal of Molecular Sciences
  11. Discovery of pyrazole‐carbohydrazide with indole moiety as tubulin polymerization inhibitors and anti‐tumor candidates
    Ruo‐Jun Man, Tian Lu, Chi‐Chong Zheng, Tong Li, Meng‐Ke Wu, Dong‐Dong Li, Xuemei He · 2022 · Drug Development Research
  12. Towards multi-target glioblastoma therapy: Structural, distribution, and functional insights into protein target candidates
    Emily Anas, Emma Hoover, Anetta L. Ille, Alexander M. Ille, Stacy A. Amico-Ruvio · 2023 · Brain Research
  13. Serine synthesis pathway upregulated by E-cadherin is essential for the proliferation and metastasis of breast cancers
    Geonhui 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)
  14. Reprogramming of amino acid metabolism in breast cancer
    Meijin Wang, Yunlu Zhang, Zhenhua Li, Li Fu · 2025 · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer
  15. Emerging roles for methionine metabolism in immune cell fate and function
    Shaojuan Liu, Xiao‐Tian Tang, Min Huang, Jianian Tang, Yiwen Yang · 2025 · Frontiers in Immunology
  16. Synthesis and biological evaluation of innovative thiourea derivatives as PHGDH inhibitors
    Jiawei Xiang, Lei Tao, Yue Zhou, Yuping Tan, Zicheng Li, Yinglan Zhao, Qingxiang Sun, Youfu Luo · 2020 · Chemical Papers
  17. Expression of Glucose Metabolism-Related Proteins in Adrenal Neoplasms
    Eun‐Kyung Kim, Hye Min Kim, Ja Seung Koo · 2021 · Pathobiology
  18. Designing Cyclic-Constrained Peptides to Inhibit Human Phosphoglycerate Dehydrogenase
    Xiaoyu Qing, Qian Wang, Hanyu Xu, Pei Liu, Luhua Lai · 2023 · Molecules
  19. ICBS 2017 in Shanghai—Illuminating Life with Chemical Innovation
    Qi Zhang, Lixin Zhang, Evripidis Gavathiotis · 2018 · ACS Chemical Biology
  20. Targeting serine metabolism vulnerability in omipalisib-resistant acute myeloid leukemia with phosphoglycerate dehydrogenase inhibitors
    Chi-Yang Tseng, Yu-Hsuan Fu, Da‐Liang Ou, Hsin‐An Hou, Hsiung–Fei Chien, Liang‐In Lin · 2025 · Biomedicine & Pharmacotherapy
  21. Structure‐Based Computational Approach in Search of the Potent Molecules Targeting Phosphoglycerate Dehydrogenase (PHGDH) Enzyme for Cancer Treatment
    Priyanka Solanki, Anu Manhas, Dhaval Patel, Prakash Chandra Jha · 2024 · ChemistrySelect
  22. The role of one-carbon amino acids in tumor-immune metabolism: From oncogenesis to therapy
    Suchandrima Saha, Monisankar Ghosh · 2024 · Elsevier eBooks
  23. Establishment of inhibitor screening and validation system for tryptophanyl tRNA synthetase using surface plasmon resonance
    Qian Wang, Guiwang Zhu, Zhenming Liu · 2021 · Analytical Biochemistry
  24. Developing chemical reprogramming strategies of non-hepatocytes for liver regeneration
    Dong-Xue Ge, Wan-Qi Yang, Hao-Zhen Ren, Jing-Lin Wang · 2025 · Journal of Advanced Research
  25. Tumor metabolic adaptation induced by L-asparaginase reveals a vulnerability to PARP1/2 inhibitor in B-cell lymphomas
    Aussel Anaïs, Ivan Nemazanyy, Ashaina Vandenberghe, Pauline Meola, Dorat Noémie, Rachel Paul, Lama Habbouche, Laurie Exposito, Nicolas Nottet, Virginie Pétrilli et al. · 2026 · Nature Communications
  26. The Role of One‐Carbon Metabolism in Cancer and Its Therapeutic Significance
    Yuting Jiang, Guoliang Zhou, Qian Zhang, Shengtao Zhou · 2026 · MedComm – Oncology
  27. Surface plasmon resonance in drug discovery: advances in protein-protein interaction and its kinetic analysis
    Diwakar Kumar Singh, Sameer Tiwari, Kumari Kripalata · 2026 · Discover Chemistry.
  28. L-asparaginase treatment induces a tumor metabolic plasticity and reveals a vulnerability to PARP1/2 inhibitor Olaparib, in B-cell lymphomas
    Aussel 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)
  29. Targeting Antioxidant Systems to Treat Pancreatic Cancer
    Francesco Gabriele Tatangelo Fazzari · 2018 · TSpace (University of Toronto)
  30. 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
  31. Mechanism Reveals a Novel Site for Allosteric Inhibition of Carcinogenic Activity of Human 3-Phosphoglycerate Dehydrogenase
    Ankita Tripathi, Qinghua Liao, Kshatresh Dutta Dubey · 2023 · ChemRxiv
  32. Additional file 6 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  33. Additional file 7 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  34. Additional file 5 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  35. Additional file 8 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  36. Prognostic value of serum phosphoglycerate dehydrogenase and glycine levels in breast cancer
    Hussam Abd Jassem, Anwar Jasib Thaaban · 2024 · Menopause Review/Przegląd Menopauzalny
  37. Additional file 4 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  38. Additional file 1 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  39. Additional file 2 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  40. Additional file 3 of PHGDH supports liver ceramide synthesis and sustains lipid homeostasis
    Yun 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
  41. Physical–chemical approach to identify local structural determinants of molecular mechanisms: Case study of antimalarial drug pyronaridine and crystal-growth inhibition
    Angela Medvedeva, Ksenia Kolomeisky, Anatoly B. Kolomeisky · 2026 · The Journal of Chemical Physics
  42. PHGDH: a metabolic switch in tumor drug resistance and a therapeutic target
    Song-Song Shi, Si-Yi Chen, Wen Zhang, Guo-Wu Rao, Quan Zheng · 2026 · Drug Discovery Today
  43. Complexe SWI/SNF et cancer _ Altérations génétiques et anomalies métaboliques
    Julien Masliah‐Planchon · 2018 · theses.fr (ABES)
  44. Metabolic plasticity in the pancreatic cancer metastatic cascade
    Biwen Zhu, Yibing Guo, Yuhua Lu · 2026 · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer
  45. Structure-Based Design and Optimization of Novel PHGDH Inhibitors for Overcoming Erlotinib-Resistant Lung Cancer
    Xingmei 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
  46. Discovery of a Covalent Inhibitor Targeting the PHGDH Dimer Interface with Antitumor Efficacy
    Lei 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
  47. Tumoral Metabolism at the Intersection of Oncogene Signaling, Epigenetics and Immunology: Emerging Therapeutic Strategies in Cancer
    Bhoomendra 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
  48. Tumor-intrinsic PHGDH inhibition sensitizes colorectal cancer to PD-1 blockade via α-ketoglutarate–mediated macrophage reprogramming
    Jieping 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
  49. Immunometabolism and rheumatic disease—advancing targeted therapies
    Mark Robin Boothby · 2026 · EULAR Rheumatology Open
  50. BindingDB Entry 50022425: Applications of oxetanes in drug discovery and medicinal chemistry.
    BindingDB · 2025 · UC San Diego
  51. BindingDB Entry 50001186: Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.
    BindingDB · 2020 · UC San Diego
  52. BindingDB Entry 50019189: Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy.
    BindingDB · 2024 · UC San Diego
  53. BindingDB Entry 15: Efficient Inhibition of SmNACE by Coordination Complexes Is Abolished by S. mansoni Sequestration of Metal.
    BindingDB · 2018 · UC San Diego
  54. BindingDB Entry 50018393: A retrospective overview of PHGDH and its inhibitors for regulating cancer metabolism.
    BindingDB · 2024 · UC San Diego
  55. BindingDB Entry 50008414: Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor
    BindingDB · 2021 · UC San Diego
  56. The Role of D-3-Phosphoglycerate Dehydrogenase (PHGDH) in Chemoresistance in Ovarian Cancer: Molecular Insights and Therapeutic Potential
    Jesús 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