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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, Labadie SS, Lai KW, Liu W, Liu Y, Li C, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhang H, Zhou A
ACS Med Chem Lett 7 896-901 (2016)
Cited: 21 times
EuropePMC logo PMID: 27774125

Abstract

A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with <10 μM lactate IC50 in a MiaPaca2 cell line. Optimization of the series led to

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  1. Three-Dimensional Analysis of the Interactions between hLDH5 and Its Inhibitors. Poli G, Granchi C, Aissaoui M, Minutolo F, Tuccinardi T. Molecules 22 E2217 (2017)

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  1. The Metabolic Landscape of Lung Cancer: New Insights in a Disturbed Glucose Metabolism. Vanhove K, Graulus GJ, Mesotten L, Thomeer M, Derveaux E, Noben JP, Guedens W, Adriaensens P. Front Oncol 9 1215 (2019)
  2. Lactate in the Tumor Microenvironment: An Essential Molecule in Cancer Progression and Treatment. Pérez-Tomás R, Pérez-Guillén I. Cancers (Basel) 12 E3244 (2020)
  3. Ribosomal Protein S6: A Potential Therapeutic Target against Cancer? Yi YW, You KS, Park JS, Lee SG, Seong YS. Int J Mol Sci 23 48 (2021)
  4. The multiple roles of LDH in cancer. Claps G, Faouzi S, Quidville V, Chehade F, Shen S, Vagner S, Robert C. Nat Rev Clin Oncol 19 749-762 (2022)
  5. Small Molecule-Based Enzyme Inhibitors in the Treatment of Primary Hyperoxalurias. Moya-Garzon MD, Gomez-Vidal JA, Alejo-Armijo A, Altarejos J, Rodriguez-Madoz JR, Fernandes MX, Salido E, Salido S, Diaz-Gavilan M. J Pers Med 11 74 (2021)
  6. Conformational control in structure-based drug design. Zheng Y, Tice CM, Singh SB. Bioorg Med Chem Lett 27 2825-2837 (2017)
  7. MYCN and Metabolic Reprogramming in Neuroblastoma. Bansal M, Gupta A, Ding HF. Cancers (Basel) 14 4113 (2022)
  8. Non-coding RNAs: emerging regulators of glucose metabolism in hepatocellular carcinoma. Lai Y, Huang H, Abudoureyimu M, Lin X, Tian C, Wang T, Chu X, Wang R. Am J Cancer Res 10 4066-4084 (2020)
  9. Targeting cancer-specific metabolic pathways for developing novel cancer therapeutics. Pal S, Sharma A, Mathew SP, Jaganathan BG. Front Immunol 13 955476 (2022)

Articles citing this publication (9)



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