Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY‐876
Open accessAbstract
Despite the long‐known fact that the facilitative glucose transporter GLUT1 is one of the key players safeguarding the increase in glucose consumption of many tumor entities even under conditions of normal oxygen supply (known as the Warburg effect), only few endeavors have been undertaken to find a GLUT1‐selective small‐molecule inhibitor. Because other transporters of the GLUT1 family are involved in crucial processes, these transporters should not be addressed by such an inhibitor. A high‐throughput screen against a library of ∼3 million compounds was performed to find a small molecule with this challenging potency and selectivity profile. The N ‐(1 H ‐pyrazol‐4‐yl)quinoline‐4‐carboxamides were identified as an excellent starting point for further compound optimization. After extensive structure–activity relationship explorations, single‐digit nanomolar inhibitors with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4 were obtained. The most promising compound, BAY‐876 [ N 4 ‐[1‐(4‐cyanobenzyl)‐5‐methyl‐3‐(trifluoromethyl)‐1 H ‐pyrazol‐4‐yl]‐7‐fluoroquinoline‐2,4‐dicarboxamide], showed good metabolic stability in vitro and high oral bioavailability in vivo.
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BAY-876, a potent GLUT1 inhibitor, was effective in preclinical settings.
“BAY-876, a potent GLUT1 inhibitor49, was separately shown as an effective candidate in pre-clinical setting 50.”
From The metabolic landscape of RAS-driven cancers from biology to therapy (2021) · cites this paper as [49]
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Development of a Novel Class of Glucose Transporter Inhibitors
Wang, D.-S., Chu, P., Yang, C., Yan, R., Chuang, Y.-C., Kulp, S. K., & Chen, C. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300015m · Cited by 42 · see citing works
RetractedUnderstanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation
Vander Heiden, M. G., Cantley, L. C., & Thompson, C. B. (2009) · Science · doi:10.1126/science.1160809 · Cited by 16,197 · see citing works
Warburg, O. (1956) · Science · doi:10.1126/science.123.3191.309 · Cited by 13,425 · see citing works
On Respiratory Impairment in Cancer Cells
Warburg, O. H. (1956) · Science · doi:10.1126/science.124.3215.269 · Cited by 3,472 · see citing works
Otto Warburg's contributions to current concepts of cancer metabolism
Koppenol, W. H., Bounds, P. L., & Dang, C. V. (2011) · Nature Reviews Cancer · doi:10.1038/nrc3038 · Cited by 3,427 · see citing works
1-Hydroxy-7-azabenzotriazole. An efficient peptide coupling additive
Carpino, L. A. (1993) · Journal of the American Chemical Society · doi:10.1021/ja00063a082 · Cited by 1,494 · see citing works
Cancer's Molecular Sweet Tooth and the Warburg Effect
Kim, J., & Dang, C. V. (2006) · Cancer Research · doi:10.1158/0008-5472.can-06-1501 · Cited by 1,217 · see citing works
Regulated transport of the glucose transporter GLUT4
Bryant, N. J., Govers, R., & James, D. E. (2002) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm782 · Cited by 1,183 · see citing works
Deregulation of Glucose Transporter 1 and Glycolytic Gene Expression by c-Myc
Osthus, R. C., Shim, H., Kim, S., Li, Q., Reddy, R., Mukherjee, M., Xu, Y., Wonsey, D. R., Lee, L. A., & Dang, C. V. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.c000023200 · Cited by 876 · see citing works
Regulation of glucose transport by insulin: traffic control of GLUT4
Leto, D., & Saltiel, A. R. (2012) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3351 · Cited by 848 · see citing works
The Tumor Suppressor p53 Down-Regulates Glucose Transporters GLUT1 and GLUT4 Gene Expression
Bar‐Yoseph, F., Armoni, M., & Karnieli, E. (2004) · Cancer Research · doi:10.1158/0008-5472.can-03-0846 · Cited by 728 · see citing works
Causes and Consequences of Increased Glucose Metabolism of Cancers
Gillies, R. J., Robey, I., & Gatenby, R. A. (2008) · Journal of Nuclear Medicine · doi:10.2967/jnumed.107.047258 · Cited by 617 · see citing works
Targeting GLUT1 and the Warburg Effect in Renal Cell Carcinoma by Chemical Synthetic Lethality
Chan, D. A., Sutphin, P. D., Nguyen, P., Turcotte, S., Lai, E. W., Banh, A., Reynolds, G. E., Chi, J., Wu, J. J., Solow-Cordero, D. E., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002394 · Cited by 563 · see citing works
Liu, Y., Cao, Y., Zhang, W., Bergmeier, S. C., Qian, Y., Akbar, H., Colvin, R. A., Ding, J., Tong, L., Wu, S., et al. (2012) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-0131 · Cited by 563 · see citing works
Glucose transporters: expression, regulation and cancer
MEDINA, R. A., & OWEN, G. I. (2002) · Biological Research · doi:10.4067/s0716-97602002000100004 · Cited by 472 · see citing works
Facilitative glucose transporters: Implications for cancer detection, prognosis and treatment
Barron, C. C., Bilan, P. J., Tsakiridis, T. K., & Tsiani, E. (2015) · Metabolism · doi:10.1016/j.metabol.2015.10.007 · Cited by 441 · see citing works
Glycolysis in cancer: A potential target for therapy
Gatenby, R. A., & Gillies, R. J. (2007) · The International Journal of Biochemistry & Cell Biology · doi:10.1016/j.biocel.2007.03.021 · Cited by 305 · see citing works
Expression of GLUT1 and GLUT3 Glucose Transporters in Endometrial and Breast Cancers
Krześlak, A., Wójcik‐Krowiranda, K., Forma, E., Jóźwiak, P., Romanowicz, H., Bieńkiewicz, A., & Bryś, M. (2012) · Pathology & Oncology Research · doi:10.1007/s12253-012-9500-5 · Cited by 280 · see citing works
Kapoor, K., Finer-Moore, J. S., Pedersen, B. P., Caboni, L., Waight, A. B., Hillig, R. C., Bringmann, P., Heisler, I., Müller, T. M., Siebeneicher, H., et al. (2016) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1603735113 · Cited by 216 · see citing works
Self-citationGLUT1 as a therapeutic target in hepatocellular carcinoma
Amann, T., & Hellerbrand, C. (2009) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728220903307509 · Cited by 205 · see citing works
Distribution of the glucose transporters in human brain tumors.
Nishioka, T., Oda, Y., Seino, Y., Yamamoto, T., Inagaki, N., Yano, H., Imura, H., Shigemoto, R., & Kikuchi, H. (1992) · PubMed · Cited by 182 · see citing works
Hughes, S., Quaade, C., Johnson, J. H., Ferber, S., & Newgard, C. B. (1993) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)82457-7 · Cited by 154 · see citing works
Brown, R. S., Leung, J. Y., Fisher, S. J., Frey, K. A., Ethier, S. P., & Wahl, R. L. (1996) · PubMed · Cited by 134 · see citing works
Jung, K., Lee, J. H., Quach, C. H. T., Paik, J.-Y., Oh, H., Park, J. W., Lee, E. J., Moon, S. H., & Lee, K.-H. (2013) · Journal of Nuclear Medicine · doi:10.2967/jnumed.112.115436 · Cited by 124 · see citing works
Cellular distribution of Glut‐1 and Glut‐5 in benign and malignant human prostate tissue
Reinicke, K., Sotomayor, P. C., Cisterna, P., Delgado, C., Nualart, F., & Godoy, A. (2011) · Journal of Cellular Biochemistry · doi:10.1002/jcb.23379 · Cited by 111 · see citing works
Nagase, Y., Takata, K., Moriyama, N., Aso, Y., Murakami, T., & Hirano, H. (1995) · The Journal of Urology · doi:10.1097/00005392-199503000-00077 · Cited by 107 · see citing works
Effert, P. J., Beniers, A. J. M. C., Tamimi, Y., Handt, S., & Jakse, G. (2004) · PubMed · Cited by 101 · see citing works
Synthesis enables identification of the cellular target of leucascandrolide A and neopeltolide
Ulanovskaya, O. A., Janjic, J. M., Suzuki, M., Sabharwal, S. S., Schumacker, P. T., Kron, S. J., & Kozmin, S. A. (2008) · Nature Chemical Biology · doi:10.1038/nchembio.94 · Cited by 96 · see citing works
Gnudi, L., Viberti, G., Raij, L. R., Rodriguez, V., Burt, D. J., Cortés, P., Hartley, B., Thomas, S., Maestrini, S., & Gruden, G. (2003) · Hypertension · doi:10.1161/01.hyp.0000075949.19968.ef · Cited by 86 · see citing works
Overexpression of GLUT1 correlates with Kras mutations in lung carcinomas
Sasaki, H. (2011) · Molecular Medicine Reports · doi:10.3892/mmr.2011.736 · Cited by 84 · see citing works
Nagase, Y., Takata, K., Moriyama, N., Aso, Y., Murakami, T., & Hirano, H. (1995) · The Journal of Urology · doi:10.1016/s0022-5347(01)67725-5 · Cited by 82 · see citing works
Martin, H.-J., Kornmann, F., & Fuhrmann, G. F. (2003) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2003.06.001 · Cited by 80 · see citing works
The rate-limiting step for tumor [18F]fluoro-2-deoxy-D-glucose (FDG) incorporation
Smith, T. (2001) · Nuclear Medicine and Biology · doi:10.1016/s0969-8051(00)00177-3 · Cited by 75 · see citing works
Membrane-permeable luciferin esters for assay of firefly luciferase in live intact cells
Craig, F. F., Simmonds, A. C., Watmore, D., McCapra, F., & White, M. (1991) · Biochemical Journal · doi:10.1042/bj2760637 · Cited by 70 · see citing works
Salas, M., Obando, P., Ojeda, L., Ojeda, P. G., Pérez, A., Vargas‐Uribe, M., Rivas, C. I., Vera, J. C., & Reyes, A. M. (2013) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00387.2012 · Cited by 52 · see citing works
Identification of novel GLUT inhibitors
Siebeneicher, H., Bauser, M., Buchmann, B., Heisler, I., Müller, T. H., Neuhaus, R., Rehwinkel, H., Telser, J., & Zorn, L. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.02.050 · Cited by 49 · see citing works
Self-citationOverexpression of GLUT1 in Colorectal Cancer is Independently Associated with Poor Prognosis
Shen, Y., Arbman, G., Olsson, B., & Sun, X. (2011) · The International Journal of Biological Markers · doi:10.5301/jbm.2011.8550 · Cited by 48 · see citing works
Mechanistic Study of Human Glucose Transport Mediated by GLUT1
Fu, X., Zhang, G., Liu, R., Wei, J., Zhang‐Negrerie, D., Jian, X., & Gao, Q. (2016) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.5b00597 · Cited by 48 · see citing works
Reddy, P. V., Jensen, K. C., Mesecar, A. D., Fanwick, P. E., & Cushman, M. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm201251c · Cited by 45 · see citing works
Wincewicz, A., SULKOWSKA, M., Koda, M., & Sulkowski, S. (2007) · Pathology & Oncology Research · doi:10.1007/bf02893436 · Cited by 44 · see citing works
A Pairwise Chemical Genetic Screen Identifies New Inhibitors of Glucose Transport
Ulanovskaya, O. A., Cui, J., Kron, S. J., & Kozmin, S. A. (2011) · Chemistry & Biology · doi:10.1016/j.chembiol.2010.12.015 · Cited by 43 · see citing works
C-nucleoside studies. Part 14. A new synthesis of pyrazofurin
BUCHANAN, J. G., Stobie, A., & Wightman, R. H. (1981) · Journal of the Chemical Society Perkin Transactions 1 · doi:10.1039/p19810002374 · Cited by 38 · see citing works
Sheu, J. J., Guan, B., Tsai, F., Hsiao, E. Y.-T., Chen, C., Seruca, R., Wang, T., & Shih, I. (2012) · American Journal Of Pathology · doi:10.1016/j.ajpath.2011.11.026 · Cited by 36 · see citing works
Pfitzinger Reaction in the Synthesis of Bioactive Compounds - A Review
Sangshetti, J. N., Zambare, A. S., Gonjari, I. D., & Shinde, D. B. (2014) · Mini-Reviews in Organic Chemistry · doi:10.2174/1570193x113106660020 · Cited by 31 · see citing works
Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells
Granchi, C., Qian, Y., Lee, H. Y., Paterni, I., Pasero, C., Iegre, J., Carlson, K. E., Tuccinardi, T., Chen, X., Katzenellenbogen, J. A., et al. (2015) · ChemMedChem · doi:10.1002/cmdc.201500320 · Cited by 22 · see citing works
Expression of glucose transporter protein 1 and p63 in serous ovarian tumor
Cai, Y. C., Zhai, J., Feng, B., Duan, X., & He, X. (2014) · Journal of obstetrics and gynaecology research · doi:10.1111/jog.12447 · Cited by 18 · see citing works
The Preparation of Some Py-Amino Quinolines and Derivatives
Renshaw, R. R., & Friedman, H. L. (1939) · Journal of the American Chemical Society · doi:10.1021/ja01267a025 · Cited by 17 · see citing works
Xu, H., Li, B., Yu, W., Wang, H., Zhao, X., Yao, Y., & Huang, D. (2013) · Nuclear Medicine Communications · doi:10.1097/mnm.0b013e328364a9e2 · Cited by 13 · see citing works
The effect of rotenone on respiration and its point of attack.
Lindahl, P. E., & OBERG, K. E. (1961) · PubMed · doi:10.1016/0014-4827(61)90033-7
Glucose transporter proteins in brain: Delivery of glucose to neurons and glia
Vannucci, S. J., Maher, F., & Simpson, I. A. (1997) · Glia · doi:10.1002/(sici)1098-1136(199709)21:1
Flagged first, then by citations
Research works printed but not linked: 10
- [6]T. Nishioka, Y. Oda, Y. Seino, T. Yamamoto, N. Inagaki, H. Yano, H. Imura, R. Shigemoto, H. Kikuchi, Cancer Res. 1992, 52, 3972– 3979. 1617673
- H. E. Rashed, S. A. Ahmed, M. Abdelgawad, Life Sci. J. 2015, 12, 162– 169;
- P. Effert, A. J. Beniers, Y. Tamimi, S. Handt, G. Jakse, Anticancer Res. 2004, 24, 3057– 3063. 15517916
- R. S. Brown, J. Y. Leung, S. J. Fisher, K. A. Frey, S. P. Ethier, R. L. Wahl, J. Nucl. Med. 1996, 37, 1042– 1047. 8683298
- [31]K. Kapoora, J. S. Finer-Moorea, B. P. Pedersena, L. Cabonia, A. Waight, R. C. Hillig, P. Bringmann, I. Heisler, T. Mueller, H. Siebeneicher, R. M. Stroud, Proc. Natl. Acad. Sci. USA 2016, 113, 4711– 4716. 27078104 PMC4855560
- [34]P. Ciapetti, B. Giethlen in The Practice of Medicinal Chemistry, 4th ed (Eds.: C. G. Wermuth, D. Aldous, P. Raboisson, D. Rognan), Elsevier, London, 2015, pp. 181– 241.
- [36]J. G. Buchanan, A. Stobie, R. H. Wightman, J. Chem. Soc. Perkin Trans. 1 1981, 2374– 2378.
- [37]J. N. Sangshetti, A. S. Zambare, I. Gonjari, D. B. Shinde, Mini-Rev. Org. Chem. 2014, 11, 225– 250.
- R. R. Renshaw, H. L. Friedman, J. Am. Chem. Soc. 1939, 61, 3320– 3322;
- [39]L. A. Carpino, J. Am. Chem. Soc. 1993, 115, 4397– 4398.
Cited by
Sorted by citations
Targeting cancer metabolism in the era of precision oncology
Stine, Z. E., Schug, Z. T., Salvino, J. M., & Dang, C. V. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00339-6 · Cited by 1,189 · see citing works
Actin cytoskeleton vulnerability to disulfide stress mediates disulfidptosis
Liu, X., Nie, L., Zhang, Y., Yan, Y., Wang, C., Colic, M., Olszewski, K. L., Horbath, A. D., Chen, X., Lei, G., et al. (2023) · Nature Cell Biology · doi:10.1038/s41556-023-01091-2 · Cited by 1,155 · see citing works
Tumor biomarkers for diagnosis, prognosis and targeted therapy
Zhou, Y., Tao, L., Qiu, J., Xu, J., Yang, X., Zhang, Y., Tian, X., Guan, X., Cen, X., & Zhao, Y. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01823-2 · Cited by 772 · see citing works
Nunes, A. S., Barros, A. S., Costa, E. C., Moreira, A. F., & Correia, I. J. (2019) · Biotechnology and Bioengineering · doi:10.1002/bit.26845 · Cited by 721 · see citing works
Liu, X., Olszewski, K. L., Zhang, Y., Lim, E. W., Shi, J., Zhang, X., Zhang, J., Lee, H., Koppula, P., Lei, G., et al. (2020) · Nature Cell Biology · doi:10.1038/s41556-020-0496-x · Cited by 599 · see citing works
Glucose transporters in cancer – from tumor cells to the tumor microenvironment
Ancey, P., Contat, C., & Meylan, E. (2018) · FEBS Journal · doi:10.1111/febs.14577 · Cited by 516 · see citing works
Changes in Nutritional Status Impact Immune Cell Metabolism and Function
Alwarawrah, Y., Kiernan, K., & MacIver, N. J. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2018.01055 · Cited by 519 · see citing works
Energy metabolism in health and diseases
Liu, H., Wang, S., Wang, J., Guo, X., Song, Y., Fu, K., Gao, Z., Liu, D., He, W., & Yang, L. (2025) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-025-02141-x · Cited by 438 · see citing works
The metabolic landscape of RAS-driven cancers from biology to therapy
Mukhopadhyay, S., Vander Heiden, M. G., & McCormick, F. (2021) · Nature Cancer · doi:10.1038/s43018-021-00184-x · Cited by 315 · see citing works
Fluorinated Pyrazoles: From Synthesis to Applications
Mykhailiuk, P. K. (2020) · Chemical Reviews · doi:10.1021/acs.chemrev.0c01015 · Cited by 299 · see citing works
Wu, L., Jin, Y., Zhao, X., Tang, K., Zhao, Y., Tong, L., Yu, X., Xiong, K., Luo, C., Zhu, J., et al. (2023) · Cell Metabolism · doi:10.1016/j.cmet.2023.07.001 · Cited by 292 · see citing works
Liao, M., Yao, D., Wu, L., Luo, C., Wang, Z., Zhang, J., & Liu, B. (2023) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2023.12.003 · Cited by 280 · see citing works
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Xiao, Y., Yu, T., Xu, Y., Ding, R., Wang, Y.-P., Jiang, Y., & Shao, Z. (2023) · Cell Metabolism · doi:10.1016/j.cmet.2023.07.006 · Cited by 266 · see citing works
Veys, K., Fan, Z., Ghobrial, M., Bouché, A., García‐Caballero, M., Vriens, K., Conchinha, N. V., Seuwen, A., Schlegel, F., Gorski, T., et al. (2020) · Circulation Research · doi:10.1161/circresaha.119.316463 · Cited by 246 · see citing works
Structure, function and regulation of mammalian glucose transporters of the SLC2 family
Holman, G. D. (2020) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/s00424-020-02411-3 · Cited by 232 · see citing works
Glucose Transporters as a Target for Anticancer Therapy
Pliszka, M., & Szablewski, L. (2021) · Cancers · doi:10.3390/cancers13164184 · Cited by 208 · see citing works
Liu, X., Zhang, Y., Zhuang, L., Olszewski, K. L., & Gan, B. (2020) · Genes & Diseases · doi:10.1016/j.gendis.2020.11.010 · Cited by 184 · see citing works
Inhibition of Glucose Transporters and Glutaminase Synergistically Impairs Tumor Cell Growth
Reckzeh, E. S., Karageorgis, G., Schwalfenberg, M., Ceballos, J., Nowacki, J., Stroet, M. C. M., Binici, A., Knauer, L., Brand, S., Choidas, A., et al. (2019) · Cell chemical biology · doi:10.1016/j.chembiol.2019.06.005 · Cited by 162 · see citing works
Ma, Y., Wang, W., Idowu, M. O., Oh, U., Wang, X.-Y., Temkin, S. M., & Fang, X. (2018) · Cancers · doi:10.3390/cancers11010033 · Cited by 145 · see citing works
Targeting glucose metabolism enzymes in cancer treatment: current and emerging strategies
Zhang, Y., Li, Q., Huang, Z., Li, B., Nice, E. C., Huang, C., Wei, L., & Zou, B. (2022) · Cancers · doi:10.3390/cancers14194568 · Cited by 144 · see citing works
Barbosa, A. M., & Martel, F. (2020) · Cancers · doi:10.3390/cancers12010154 · Cited by 137 · see citing works
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Wu, Q., Heidenreich, D. J., Zhou, S., Ackloo, S. Z., Krämer, A., Nakka, K. K., Lima‐Fernandes, E., Deblois, G., Duan, S., Vellanki, R. N., et al. (2019) · Nature Communications · doi:10.1038/s41467-019-09672-2 · Cited by 120 · see citing works
Yin, F., Feng, F., Wang, L., Wang, X., Li, Z., & Cao, Y. W. (2019) · Cell Death and Disease · doi:10.1038/s41419-019-1884-7 · Cited by 121 · see citing works
Karageorgis, G., Reckzeh, E. S., Ceballos, J., Schwalfenberg, M., Sievers, S., Ostermann, C., Pahl, A., Ziegler, S., & Waldmann, H. (2018) · Nature Chemistry · doi:10.1038/s41557-018-0132-6 · Cited by 118 · see citing works
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Quanz, M., Bender, E., Kopitz, C., Grünewald, S., Schlicker, A., Schwede, W., Eheim, A. L., Toschi, L., Neuhaus, R., Richter, C., et al. (2018) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-17-1253 · Cited by 117 · see citing works
Self-citationCommander, R., Wei, C., Sharma, A., Mouw, J. K., Burton, L. J., Summerbell, E. R., Mahboubi, D., Peterson, R. J., Konen, J. M., Zhou, W., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-15219-7 · Cited by 111 · see citing works
Donated chemical probes for open science
Müller, S., Ackloo, S. Z., Arrowsmith, C. H., Bauser, M., Baryza, J. L., Blagg, J., Böttcher, J., Bountra, C., Brown, P. J., Bunnage, M. E., et al. (2018) · eLife · doi:10.7554/elife.34311 · Cited by 107 · see citing works
Self-citationThe Druggability of Solute Carriers
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Yao, C.-C., Sun, R.-M., Yang, Y., Zhou, H., Meng, Z., Chi, R., Xia, L., Ji, P., Chen, Y., Zhang, G., et al. (2023) · Cell Reports · doi:10.1016/j.celrep.2023.112186 · Cited by 97 · see citing works
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Meng, Y., Xu, X. J., Luan, H., Li, L., Dai, W., Li, Z., & Bian, J. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0052 · Cited by 82 · see citing works
Quercetin inhibits glucose transport by binding to an exofacial site on GLUT1
Hamilton, K. E., Rekman, J. F., Gunnink, L. K., Busscher, B. M., Scott, J. L., Tidball, A. M., Stehouwer, N. R., Johnecheck, G. N., Looyenga, B. D., & Louters, L. L. (2018) · Biochimie · doi:10.1016/j.biochi.2018.05.012 · Cited by 84 · see citing works
Highlighting membrane protein structure and function: A celebration of the Protein Data Bank
Li, F., Egea, P. F., Vecchio, A. J., Asial, I., Gupta, M., Paulino, J., Bajaj, R., Dickinson, M. S., Ferguson-Miller, S. M., Monk, B. C., et al. (2021) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2021.100557 · Cited by 81 · see citing works
Glucose transporter 1 regulates the proliferation and cisplatin sensitivity of esophageal cancer
Sawayama, H., Ogata, Y., Ishimoto, T., Mima, K., Hiyoshi, Y., Iwatsuki, M., Baba, Y., Miyamoto, Y., Yoshida, N., & Baba, H. (2019) · Cancer Science · doi:10.1111/cas.13995 · Cited by 81 · see citing works
Targeting lactate metabolism for cancer immunotherapy - a matter of precision
Heuser-Loy, C., Renner, K., Kreutz, M. P., & Gattinoni, L. (2022) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2022.12.001 · Cited by 76 · see citing works
Ma, Y., Wang, W., Devarakonda, T., Zhou, H., Wang, X., Salloum, F. N., Spiegel, S., & Fang, X. (2020) · Scientific Reports · doi:10.1038/s41598-020-58334-7 · Cited by 74 · see citing works
Olszewski, K. L., Barsotti, A. M., Feng, X., Momcilovic, M., Liu, K. G., Kim, J., Morris, K., Lamarque, C., Gaffney, J., Yu, X., et al. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.10.007 · Cited by 76 · see citing works
Yao, J., Tang, S., Shi, C., Lin, Y., Ge, L., Chen, Q., Ou, B., Liu, D., Miao, Y., Xie, Q., et al. (2022) · Autophagy · doi:10.1080/15548627.2022.2119353 · Cited by 69 · see citing works
The glucose transporter GLUT1 is required for ErbB2-induced mammary tumorigenesis
Wellberg, E. A., Johnson, S. J., Finlay-Schultz, J., Lewis, A. S., Terrell, K. L., Sartorius, C. A., Abel, E. D., Muller, W. J., & Anderson, S. M. (2016) · Breast Cancer Research · doi:10.1186/s13058-016-0795-0 · Cited by 65 · see citing works
Richter, E. A., Bilan, P. J., & Klip, A. (2025) · Physiological Reviews · doi:10.1152/physrev.00033.2024 · Cited by 64 · see citing works
Targeting metabolism to enhance immunotherapy within tumor microenvironment
Liang, X., Chen, X., Yan, Y., Cheng, A.-Y., Lin, J.-Y., Jiang, Y.-X., Chen, H., Jin, J., & Luan, X. (2024) · Acta Pharmacologica Sinica · doi:10.1038/s41401-024-01304-w · Cited by 68 · see citing works
A New Spectral Shift-Based Method to Characterize Molecular Interactions
Langer, A., Lüdecke, A., Bartoschik, T., Cehlár, O., Duhr, S., Baaske, P., & Streicher, W. W. (2022) · Assay and Drug Development Technologies · doi:10.1089/adt.2021.133 · Cited by 59 · see citing works
Miller, Z. A., Muthuswami, S., Mueller, A., Ma, R. Z., Sywanycz, S. M., Naik, A., Huang, L., Brody, R. M., Diab, A., Carey, R. M., et al. (2024) · Cell Death Discovery · doi:10.1038/s41420-024-02106-z · Cited by 59 · see citing works
Development of Glucose Transporter (GLUT) Inhibitors
Reckzeh, E. S., & Waldmann, H. (2019) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201901353 · Cited by 56 · see citing works
Cellular effects and clinical implications of SLC2A3 copy number variation
Ziegler, G. C., Álmos, P. Z., McNeill, R. V., Jansch, C., & Lesch, K. (2020) · Journal of Cellular Physiology · doi:10.1002/jcp.29753 · Cited by 57 · see citing works
Tyagi, K., Mandal, S., & Roy, A. (2021) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2021.188563 · Cited by 56 · see citing works
Henry, Ó. C., & O'Neill, L. A. J. (2025) · European Journal of Immunology · doi:10.1002/eji.202451381 · Cited by 56 · see citing works
Mamun, A. A., Hayashi, H., Yamamura, A., Nayeem, M. J., & Sato, M. (2020) · The Journal of Physiological Sciences · doi:10.1186/s12576-020-00773-y · Cited by 55 · see citing works
Metabolic gatekeepers to safeguard against autoimmunity and oncogenic B cell transformation
Müschen, M. (2019) · Nature reviews. Immunology · doi:10.1038/s41577-019-0154-3 · Cited by 55 · see citing works
Elevated UCP1 levels are sufficient to improve glucose uptake in human white adipocytes
Tews, D., Pula, T., Funcke, J., Jastroch, M., Keuper, M., Debatin, K., Wabitsch, M., & Fischer‐Posovszky, P. (2019) · Redox Biology · doi:10.1016/j.redox.2019.101286 · Cited by 52 · see citing works
Zhang, Y., Shi, J., Liu, X., Xiao, Z., Lei, G., Lee, H., Koppula, P., Cheng, W., Mao, C., Zhuang, L., et al. (2020) · Cancer Research · doi:10.1158/0008-5472.can-19-3580 · Cited by 51 · see citing works
Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor
Lefranc, J., Schulze, V., Hillig, R. C., Briem, H., Prinz, F., Mengel, A., Heinrich, T. K., Bálint, J., Rengachari, S., Irlbacher, H., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01460 · Cited by 51 · see citing works
Chemical biology probes of mammalian GLUT structure and function
Holman, G. D. (2018) · Biochemical Journal · doi:10.1042/bcj20170677 · Cited by 49 · see citing works
Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays
Guo, Z., Cheng, Z., Wang, J., Liu, W., Peng, H., Wang, Y., Rao, A., Li, R., Ying, X., Korangath, P. C., et al. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201905578 · Cited by 48 · see citing works
Exploiting metabolic cell death for cancer therapy
Mao, C., Jiang, D., Koong, A. C., & Gan, B. (2025) · Nature reviews. Cancer · doi:10.1038/s41568-025-00879-8 · Cited by 55 · see citing works
Hypoxia and its therapeutic possibilities in paediatric cancers
Bernauer, C., Man, Y. K. S., Chisholm, J., Lepicard, E. Y., Robinson, S. P., & SHIPLEY, J. M. (2020) · British Journal of Cancer · doi:10.1038/s41416-020-01107-w · Cited by 48 · see citing works
Hamilton, K. E., Bouwer, M. F., Louters, L. L., & Looyenga, B. D. (2021) · Biochimie · doi:10.1016/j.biochi.2021.06.017 · Cited by 46 · see citing works
Conformational Studies of Glucose Transporter 1 (GLUT1) as an Anticancer Drug Target
Almahmoud, S. A., Wang, X., Vennerstrom, J. L., & Zhong, H. A. (2019) · Molecules · doi:10.3390/molecules24112159 · Cited by 46 · see citing works
Pharmacological Targeting of GLUT1 to Control Autoreactive T Cell Responses
Dedda, C. D., Vignali, D., Piemonti, L., & Monti, P. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20194962 · Cited by 46 · see citing works
Na, K. J., Choi, H., Oh, H. R., Kim, Y. H., Lee, S. B., Jung, Y. J., Koh, J., Park, S., Lee, H. J., Jeon, Y. K., et al. (2020) · Theranostics · doi:10.7150/thno.48954 · Cited by 45 · see citing works
Targeted delivery of baicalein-p53 complex to smooth muscle cells reverses pulmonary hypertension
Teng, C., Li, B., Lin, C., Xing, X., Huang, F., Yang, Y., Li, Y., Azevedo, H. S., & He, W. (2021) · Journal of Controlled Release · doi:10.1016/j.jconrel.2021.12.006 · Cited by 45 · see citing works
Wang, J., Chen, J., Fan, K., Wang, M., Gao, M., Ren, Y., Wu, S., He, Q., Tu, K., Xu, Q., et al. (2024) · Advanced Science · doi:10.1002/advs.202408789 · Cited by 44 · see citing works
AHR Regulates Metabolic Reprogramming to Promote SIRT1-Dependent Keratinocyte Differentiation
Sutter, T. R., Olesen, K. M., Bhuju, J., Guo, Z., & Sutter, T. R. (2018) · Journal of Investigative Dermatology · doi:10.1016/j.jid.2018.10.019 · Cited by 45 · see citing works
GLUT1 Biological Function and Inhibition: Research Advances
Cao, S., Chen, Y.-S., Ren, Y., Feng, Y., & Long, S. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0071 · Cited by 43 · see citing works
Temre, M. K., Kumar, A., & Singh, S. M. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.1035510 · Cited by 43 · see citing works
Glycometabolic Regulation of the Biogenesis of Small Extracellular Vesicles
Harada, Y., Nakajima, K., Suzuki, T., Fukushige, T., Kondo, K., Seino, J., Ohkawa, Y., Suzuki, T., Inoue, H., Kanekura, T., et al. (2020) · Cell Reports · doi:10.1016/j.celrep.2020.108261 · Cited by 42 · see citing works
Xu, Y., Hao, X., Ren, Y., Xu, Q., Liu, X., Song, S., & Wang, Y. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2022.1063423 · Cited by 43 · see citing works
Yu, J., Li, Q., Wei, Z., Fan, G., Wan, F., & Tian, L. (2023) · Acta Biomaterialia · doi:10.1016/j.actbio.2023.08.025 · Cited by 41 · see citing works
Role of Glucose Metabolic Reprogramming in Breast Cancer Progression and Drug Resistance
Lei, P., Wang, W., Sheldon, M., Sun, Y., Yao, F., & Ma, L. (2023) · Cancers · doi:10.3390/cancers15133390 · Cited by 40 · see citing works
Gauthier-Coles, G., Bröer, A., McLeod, M. D., George, A. J., Hannan, R. D., & Bröer, S. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.963066 · Cited by 38 · see citing works
Identification of Compounds That Decrease Glioblastoma Growth and Glucose Uptake in Vitro
Libby, C. J., Zhang, S., Benavides, G. A., Scott, S. E., Li, Y., Redmann, M., Tran, A. N., Otamias, A., Darley-Usmar, V. M., Напиерала, М., et al. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.8b00251 · Cited by 38 · see citing works
Tilekar, K. N., Upadhyay, N., Schweipert, M., Hess, J. D., Macias, L. G.-F., Mrówka, P., Meyer‐Almes, F., Aguilera, R. J., Iancu, C. V., Choe, J., et al. (2020) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2020.105512 · Cited by 38 · see citing works
Endothelial GLUTs and vascular biology
Wu, W., & Bai, Y. (2022) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2022.114151 · Cited by 38 · see citing works
Targeting RAS mutants in malignancies: successes, failures, and reasons for hope
Yang, H. S., Zhou, X., Fu, D., Le, C., Wang, J., Zhou, Q., Liu, X., Yuan, Y., Ding, K., & Xiao, Q. (2022) · 癌症:英文版 · doi:10.1002/cac2.12377 · Cited by 35 · see citing works
Bechard, M. E., Smalling, R., Hayashi, A., Zhong, Y., Word, A. E., Campbell, S. L., Tran, A. V., Weiss, V. L., Iacobuzio-Donahue, C., Wellen, K. E., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-17839-5 · Cited by 33 · see citing works
In what area of biology has a “new” type of cell death been discovered?
Wang, X., Lin, J., Li, Z., & Wang, M. (2023) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2023.188955 · Cited by 35 · see citing works
Inhibition of heme biosynthesis triggers cuproptosis in acute myeloid leukemia
Lewis, A. C., Gruber, E., Franich, R. L., Armstrong, J. M., Kelly, M. J., Opazo, C., Low, Y. C., Flippe, L., Wijanarko, K. J., Rowe, C. L., et al. (2025) · Cell · doi:10.1016/j.cell.2025.10.028 · Cited by 35 · see citing works
Huang, Y. C., Xian, L., Liu, Z., Wei, L., Qin, L., Xiong, Y., Hu, L., Zhou, S., Fu, Q., Li, B., et al. (2022) · Biochemical Pharmacology · doi:10.1016/j.bcp.2022.115198 · Cited by 35 · see citing works
Identification of a novel GLUT1 inhibitor with in vitro and in vivo anti-tumor activity
Chen, X., Zhao, Y., He, C., Gao, G., Li, J., Qiu, L., Wang, X., Gao, Y., Qi, Y., Sun, K., et al. (2022) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2022.07.123 · Cited by 34 · see citing works
Alanine supplementation exploits glutamine dependency induced by SMARCA4/2-loss
Zhu, X., Fu, Z., Chen, S. Y., Ong, D., Aceto, G., Ho, R., Steinberger, J., Monast, A., Pilon, V., Li, E., et al. (2023) · Nature Communications · doi:10.1038/s41467-023-38594-3 · Cited by 33 · see citing works
Bad neighbours: hypoxia and genomic instability in prostate cancer
Ashton, J., & Bristow, R. G. (2020) · British Journal of Radiology · doi:10.1259/bjr.20200087 · Cited by 32 · see citing works
Yang, H., Zhang, M.-Z.-H., Sun, H., Chai, Y., Li, X., Jiang, Q., & Hou, J. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.783194 · Cited by 33 · see citing works
García‐Cañaveras, J. C., & Lahoz, A. (2021) · Cancers · doi:10.3390/cancers13133230 · Cited by 32 · see citing works
Characterization of the effect of the GLUT-1 inhibitor BAY-876 on T cells and macrophages
Chen, Z., Vaeth, M., Eckstein, M., Delgobo, M., Ramos, G. C., Frantz, S., Hofmann, U., & Gladow, N. (2023) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2023.175552 · Cited by 31 · see citing works
Pharmacological inhibition of GLUT1 as a new immunotherapeutic approach after myocardial infarction
Chen, Z., Dudek, J., Maack, C., & Hofmann, U. (2021) · Biochemical Pharmacology · doi:10.1016/j.bcp.2021.114597 · Cited by 30 · see citing works
Zügner, E., Yang, H., Kotzbeck, P., Boulgaropoulos, B., Sourij, H., Hagvall, S., Elmore, C. S., ESTERLINE, R. L., Moosmang, S., Oscarsson, J., et al. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23147966 · Cited by 33 · see citing works
Discovery and Optimization of Glucose Uptake Inhibitors
Liu, K. G., Kim, J., Olszewski, K. L., Barsotti, A. M., Morris, K., Lamarque, C., Yu, X., Gaffney, J., Feng, X., Patel, J. P., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b02153 · Cited by 29 · see citing works
Burgart, Y. V., Agafonova, N. A., Shchegolkov, E. V., Красных, О. П., Kushch, S. O., Evstigneeva, N. P., Герасимова, Н. А., Владимировна, М. В., Триандафилова, Г. А., Solodnikov, S. Y., et al. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112768 · Cited by 29 · see citing works
Wortmann, L., Bräuer, N., Holton, S. J., Irlbacher, H., Weiske, J., Lechner, C., Meier, R., Karén, J., Sioberg, C., Pütter, V., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01245 · Cited by 28 · see citing works
Self-citationMiR-378a inhibits glucose metabolism by suppressing GLUT1 in prostate cancer
Cannistraci, A., Hascoët, P., Ali, A., Mundra, P. A., Clarke, N. W., Pavet, V., & Marais, R. (2022) · Oncogene · doi:10.1038/s41388-022-02178-0 · Cited by 28 · see citing works
Rodriguez‐Zabala, M., Ramakrishnan, R., Reinbach, K., Ghosh, S., Oburoglu, L., Falqués, T., Bellamkonda, K., Ehinger, M., Peña‐Martínez, P., Puente‐Moncada, N., et al. (2023) · Blood Advances · doi:10.1182/bloodadvances.2023009967 · Cited by 28 · see citing works
Molecular Tools for Facilitative Carbohydrate Transporters (Gluts)
Tanasova, M., & Fedie, J. R. (2017) · ChemBioChem · doi:10.1002/cbic.201700221 · Cited by 28 · see citing works
Guo, L., Zhang, W., Xie, Y., Chen, X., Olmstead, E. E., Lian, M., Zhang, B., Zaytseva, Y. Y., Evers, B. M., Spielmann, H. P., et al. (2022) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-0925 · Cited by 28 · see citing works
GLUT4 expression and glucose transport in human induced pluripotent stem cell-derived cardiomyocytes
Bowman, P. R. T., Smith, G. L., & Gould, G. W. (2019) · PLoS ONE · doi:10.1371/journal.pone.0217885 · Cited by 28 · see citing works
Heitmeier, M. R., Hresko, R. C., Edwards, R. L., Prinsen, M. J., Ilagan, M. X. G., John, A. R. O., & Hruz, P. W. (2019) · PLoS ONE · doi:10.1371/journal.pone.0216457 · Cited by 27 · see citing works
- Authors
- Siebeneicher, H., Cleve, A., Rehwinkel, H., Neuhaus, R., Heisler, I., Müller, T., Bauser, M., & Buchmann, B.
- Affiliations
- Bayer AG Drug Discovery 13353 Berlin Germany
- Bayer (Germany) (DE)
- Corresponding author
- Buchmann, Bernd
- ORCID
- Müller, Thomas
- Venue
- ChemMedChem
- Publisher
- Wiley
- Published
- 2016-08-23
- Volume
- 11
- Issue
- 20
- Pages
- 2261-2271
- ISSN
- 1860-7179 (ISSN-L)
- 1860-7187
- PMC
- PMC5095872
- OpenAlex
- W2517194940
- Cited by
- 294
- References
- 51
- Citations by year
- 2026: 38 · 2025: 38 · 2024: 41 · 2023: 34 · 2022: 34 · 2021: 32 · 2020: 31 · 2019: 29 · 2018: 14 · 2017: 2 · 2016: 1
- FWCI
- 6.40
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- ChemMedChem (publishedVersion, cc-by-nc-nd)
- PubMed Central (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Keywords
- GLUT1, glucose transporter inhibitors, BAY-876, pyrazolone derivatives, structure-activity relationship, high-throughput screening, Warburg effect, tumor glucose metabolism, metabolic stability, oral bioavailability
- MeSH terms
- Administration, Oral, Biological Availability, Humans, Pyrazoles, Quinolines, Structure-Activity Relationship, Molecular Structure, Glucose Transporter Type 1, High-Throughput Screening Assays
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