#METABOLOMICS WORKBENCH lgafeira_20241119_065522 DATATRACK_ID:5383 STUDY_ID:ST003585 ANALYSIS_ID:AN005888 PROJECT_ID:PR002215 VERSION 1 CREATED_ON November 21, 2024, 6:33 pm #PROJECT PR:PROJECT_TITLE Glutaminase 1 (GLS1)-based therapy targets glutamine reliance in glioblastoma PR:PROJECT_TITLE (GBM) PR:PROJECT_SUMMARY Glioblastomas (GBMs) are the most lethal central nervous system (CNS) neoplasms, PR:PROJECT_SUMMARY accounting for this the inexistence of specific therapies. Glutamine plays a key PR:PROJECT_SUMMARY role in CNS physiology, and metabolic adjustments have been reported in GBM, PR:PROJECT_SUMMARY which are considered glutamine-addicted. Therefore, our goal was to affect GBM PR:PROJECT_SUMMARY cells by decreasing the systemic bioavailability of glutamine with a glutaminase PR:PROJECT_SUMMARY (GLS1)-based therapy. The in vitro results showed that the GBM cell lines were PR:PROJECT_SUMMARY indeed glutamine-dependent, triggering a metabolic remodeling upon the PR:PROJECT_SUMMARY presence/absence of glutamine. GLS1 treatment increased cell death, decreased PR:PROJECT_SUMMARY cell proliferation, and induced U-87MG invasion, due to glutamine scarcity. This PR:PROJECT_SUMMARY intervention triggered a metabolic shift, evident in altered gene expression and PR:PROJECT_SUMMARY metabolite profiles in cell extracts and conditioned media. Results from the in PR:PROJECT_SUMMARY vivo orthotopic xenograft mouse model of GBM showed an increase in overall PR:PROJECT_SUMMARY survival (OS) with the GLS1 treatment, along with lower cachexia. Moreover, PR:PROJECT_SUMMARY metabolomics’ multivariate analysis of serum collected during tumor induction PR:PROJECT_SUMMARY and the therapeutic course showed statistically different metabolic profiles of PR:PROJECT_SUMMARY GLS1-treated mice midst treatment, which could help monitor the therapy PR:PROJECT_SUMMARY response. PR:INSTITUTE ITQB NOVA PR:LAST_NAME Gonçalves PR:FIRST_NAME Luís PR:ADDRESS Avenida Republica, Oeiras, Not USCanada, 2780-157 Oeiras, Portugal PR:EMAIL lgafeira@itqb.unl.pt PR:PHONE 214469464 PR:CONTRIBUTORS Filipa Martins, Céline S. Gonçalves, Fernanda Silva2, David van der Kellen, PR:CONTRIBUTORS Eduarda P. Martins, Renata Arada, Saudade André, Lúcia Roque, Marta Pojo, PR:CONTRIBUTORS Luís G. Gonçalves, Bruno M. Costa, Jacinta Serpa #STUDY ST:STUDY_TITLE Glutaminase 1 (GLS1)-based therapy targets glutamine reliance in glioblastoma ST:STUDY_TITLE (GBM)- cell line assays supernants ST:STUDY_SUMMARY Glioblastomas (GBMs) are the most lethal central nervous system (CNS) neoplasms, ST:STUDY_SUMMARY accounting for this the inexistence of specific therapies. Glutamine plays a key ST:STUDY_SUMMARY role in CNS physiology, and metabolic adjustments have been reported in GBM, ST:STUDY_SUMMARY which are considered glutamine-addicted. Therefore, our goal was to affect GBM ST:STUDY_SUMMARY cells by decreasing the systemic bioavailability of glutamine with a glutaminase ST:STUDY_SUMMARY (GLS1)-based therapy. In order to understand how Glutaminase treatment affects ST:STUDY_SUMMARY the metabolism of GBM cell lines (U251 and U-87MG), we exposed these cell lines ST:STUDY_SUMMARY to GLS1 for 24 h and the conditioned media (supernatants) and cell extracts ST:STUDY_SUMMARY (aqueous and organic phase) were further analyzed by 1H-NMR. The in vitro ST:STUDY_SUMMARY results showed that the GBM cell lines were indeed glutamine-dependent, ST:STUDY_SUMMARY triggering a metabolic remodeling upon the presence/absence of glutamine. GLS1 ST:STUDY_SUMMARY treatment increased cell death, decreased cell proliferation, and induced U-87MG ST:STUDY_SUMMARY invasion, due to glutamine scarcity. This intervention triggered a metabolic ST:STUDY_SUMMARY shift, evident in altered gene expression and metabolite profiles in cell ST:STUDY_SUMMARY extracts and conditioned media. Results from the in vivo orthotopic xenograft ST:STUDY_SUMMARY mouse model of GBM showed an increase in overall survival (OS) with the GLS1 ST:STUDY_SUMMARY treatment, along with lower cachexia. Moreover, metabolomics’ multivariate ST:STUDY_SUMMARY analysis of serum collected during tumor induction and the therapeutic course ST:STUDY_SUMMARY showed statistically different metabolic profiles of GLS1-treated mice midst ST:STUDY_SUMMARY treatment, which could help monitor the therapy response. ST:INSTITUTE ITQB NOVA ST:LAST_NAME Gonçalves ST:FIRST_NAME Luís ST:ADDRESS Avenida Republica, Oeiras, Not USCanada, 2780-157 Oeiras, Portugal ST:EMAIL lgafeira@itqb.unl.pt ST:PHONE 214469464 #SUBJECT SU:SUBJECT_TYPE Cultured cells SU:SUBJECT_SPECIES Homo sapiens SU:TAXONOMY_ID 9606 #SUBJECT_SAMPLE_FACTORS: SUBJECT(optional)[tab]SAMPLE[tab]FACTORS(NAME:VALUE pairs separated by |)[tab]Raw file names and additional sample data SUBJECT_SAMPLE_FACTORS - C_U_ 1 Condition:Control | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super1_210113 SUBJECT_SAMPLE_FACTORS - C_U_ 2 Condition:Control | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super2_210113 SUBJECT_SAMPLE_FACTORS - C_U_ 3 Condition:Control | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super201_210519 SUBJECT_SAMPLE_FACTORS - C_U_ 4 Condition:Control | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super202_210519a SUBJECT_SAMPLE_FACTORS - Gln_U_1 Condition:Glutamine | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super5_210113 SUBJECT_SAMPLE_FACTORS - Gln_U_2 Condition:Glutamine | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super6_210113 SUBJECT_SAMPLE_FACTORS - Gln_U_3 Condition:Glutamine | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super237_210519 SUBJECT_SAMPLE_FACTORS - Gln_U_4 Condition:Glutamine | Sample source:U251 brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super238_210519 SUBJECT_SAMPLE_FACTORS - C_MG_1 Condition:Control | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super9_210113 SUBJECT_SAMPLE_FACTORS - C_MG_2 Condition:Control | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super10_210113 SUBJECT_SAMPLE_FACTORS - C_MG_3 Condition:Control | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super215_210519 SUBJECT_SAMPLE_FACTORS - C_MG_4 Condition:Control | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super216_210519 SUBJECT_SAMPLE_FACTORS - Gln_MG_1 Condition:Glutamine | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super13_210113 SUBJECT_SAMPLE_FACTORS - Gln_MG_2 Condition:Glutamine | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super14_210113 SUBJECT_SAMPLE_FACTORS - Gln_MG_3 Condition:Glutamine | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super229_210519 SUBJECT_SAMPLE_FACTORS - Gln_MG_4 Condition:Glutamine | Sample source:U-87MG brain cancer cells RAW_FILE_NAME(Spectra)=FM_Super230_210519 #COLLECTION CO:COLLECTION_SUMMARY Two commercial GBM cell lines, U-87 MG (HTB-14, American Type Culture Collection CO:COLLECTION_SUMMARY – ATCC) and U251 (09063001, European Collection of Authenticated Cell Cultures CO:COLLECTION_SUMMARY – ECACC) were cultured in Dulbecco’s modified Eagle medium F-12 (DMEM/F-12; CO:COLLECTION_SUMMARY 11330-032, Gibco, Life Technologies), supplemented with 10% fetal bovine serum CO:COLLECTION_SUMMARY (FBS; P40-37500, PAN Biotech), 1% Antibiotic-Antimycotic (AA; P06-07300, PAN CO:COLLECTION_SUMMARY Biotech) and 50 µg/mL gentamicin (15750-060, Gibco, Life Technologies). Cells CO:COLLECTION_SUMMARY (2.6 x 10^7 cells/flask) were seeded in 175 cm2 culture flasks. After exposure CO:COLLECTION_SUMMARY to the experimental conditions, supernatants were collected and stored at CO:COLLECTION_SUMMARY -80ºC. CO:COLLECTION_PROTOCOL_FILENAME Glutamine_Protocols.pdf CO:SAMPLE_TYPE Culture Media CO:STORAGE_CONDITIONS -80℃ #TREATMENT TR:TREATMENT_SUMMARY Cells were grown in presence of 6 mM L-glutamine (25030-024, Gibco) or in TR:TREATMENT_SUMMARY absence #SAMPLEPREP SP:SAMPLEPREP_SUMMARY 60 µL solution of 0.35 mM KPi (pH 7.4) and 0.16 mM in D2O was added to 540 µL SP:SAMPLEPREP_SUMMARY of supernatants SP:PROCESSING_STORAGE_CONDITIONS -80℃ #ANALYSIS AN:ANALYSIS_PROTOCOL_FILE Glutamine_Protocols.pdf #NMR NM:INSTRUMENT_NAME Bruker Avance II+ 800 MHz NM:INSTRUMENT_TYPE FT-NMR NM:NMR_EXPERIMENT_TYPE 1D-1H NM:SPECTROMETER_FREQUENCY 800 NM:NMR_PROBE 5 mm TCI cryoprobe NM:NMR_SOLVENT 10 % D2O/ 90 % H20 NM:NMR_TUBE_SIZE 5 mm NM:PULSE_SEQUENCE noesygppr1d #NMR_METABOLITE_DATA NMR_METABOLITE_DATA:UNITS mM NMR_METABOLITE_DATA_START Samples C_U_ 1 C_U_ 2 C_U_ 3 C_U_ 4 Gln_U_1 Gln_U_2 Gln_U_3 Gln_U_4 C_MG_1 C_MG_2 C_MG_3 C_MG_4 Gln_MG_1 Gln_MG_2 Gln_MG_3 Gln_MG_4 Factors Condition:Control | Sample source:U251 brain cancer cells Condition:Control | Sample source:U251 brain cancer cells Condition:Control | Sample source:U251 brain cancer cells Condition:Control | Sample source:U251 brain cancer cells Condition:Glutamine | Sample source:U251 brain cancer cells Condition:Glutamine | Sample source:U251 brain cancer cells Condition:Glutamine | Sample source:U251 brain cancer cells Condition:Glutamine | Sample source:U251 brain cancer cells Condition:Control | Sample source:U-87MG brain cancer cells Condition:Control | Sample source:U-87MG brain cancer cells Condition:Control | Sample source:U-87MG brain cancer cells Condition:Control | Sample source:U-87MG brain cancer cells Condition:Glutamine | Sample source:U-87MG brain cancer cells Condition:Glutamine | Sample source:U-87MG brain cancer cells Condition:Glutamine | Sample source:U-87MG brain cancer cells Condition:Glutamine | Sample source:U-87MG brain cancer cells 1-Methylnicotinamide 2.7 3.4 13 11.7 3.6 3.3 9.4 9.5 2-Hydroxybutyrate 90.7 111.4 91.3 72 25.4 32.3 28.7 30.1 37 29.5 38.5 27.2 26.7 23.1 23.9 24.3 2-Oxoisocaproate 53.5 68.4 66 65.2 8.6 10.8 12.8 11.6 11.8 17.9 9.7 10 7.8 12.3 13.4 3-Hydroxyisobutyrate 55.2 49.5 18 51.4 Acetate 86.1 42 78.7 35.8 60.2 63.2 30.1 121 170.4 152.3 203.5 162.3 99.2 147.2 157.1 Alanine 26.5 26.4 9.6 9.6 234.2 349.3 313.5 298.8 72.2 69.2 88.7 76.4 123.3 100.7 83.3 88.1 Arginine 250.9 180.8 240.9 285.6 244.9 209.3 294.6 195.2 479.7 516.3 362.7 408.7 455 507.2 480 623.9 Asparagine 152.4 312.6 Aspartate 267.9 91.9 165.8 220.4 49 84.7 51.3 57.6 84.6 79.6 45 66.4 Choline 46.8 28.9 28.2 22.5 42 36.7 78.7 44 61 64.3 61.8 68.2 62.6 57.4 65.5 68.1 Citrate 10.6 31.8 36.5 29.4 50.9 17.2 14.9 22.5 17.1 Ethanol 104.5 132.2 230.2 185.3 72.7 140 176.7 205.2 199 213.7 410.6 217.9 170.9 346.5 351.8 Formate 197.9 227.9 579.9 406.6 195.4 189.9 316.4 303 126.2 90.2 125.2 80.7 92.9 76 53.6 55.6 Fumarate 2.9 2.3 4.9 5.3 Glucose 121.8 273.8 968.3 337.7 123.5 151.6 322.1 299.6 Glutamate 75.8 495.2 314.7 423.4 419.3 229.6 118.9 Glutamine 1438.5 1965.3 1694.1 1664.3 3677.3 3244.7 3168.2 3212.2 Glycine 221.2 220.7 553 392.2 169.3 185.2 296 281.6 292 298.3 295.6 282.8 267.6 241.6 236.8 245.4 Histidine 81.8 92 26.5 60.1 44 82 56.6 56.1 35.9 80.3 61.8 104.7 29.2 49.4 37.9 36.2 Hypoxanthine 16.6 5.6 12.3 7.9 7.8 4.5 3.1 3.7 9.9 12.2 11.1 15.2 8.9 8 11.4 12.1 Isobutyrate 31.2 46.9 39.7 38.9 6.7 9.8 8.2 9.5 12.4 7.7 13.5 7.2 6.3 5.6 4.1 222.7 Isoleucine 211.5 86 146.6 125.7 216.7 212.9 212.2 295.9 309.2 351.8 291.5 346.8 332.3 280.4 327.6 280.7 Lactate 336.4 444.4 164.8 279.1 319.8 816.3 484.1 401.9 2223.9 2012.5 3005.1 1427 2051 2223 1234.3 1545 Leucine 204.8 130.3 131.5 124.2 246.9 219.7 210.8 205.2 304.3 342 298.8 339.2 329.4 301 337.4 353.3 Lysine 384.6 344 335.4 303 263.1 358.4 346.2 298.6 396.8 393.1 420.5 358.4 608.4 319.5 421.4 530.1 Methionine 76.7 64.2 71.2 72.4 62.2 56.2 57.9 63.7 92.7 95.8 75.6 79.4 96.5 87.7 95.5 96.2 Nicotinate 11.3 9.8 4.9 5.1 10 9.5 3.6 4.6 16.9 15.4 17.3 16.2 15.9 12.6 16.2 14.7 Ornithine 157.4 201.5 99.4 80.4 255.1 272.7 175.6 237.6 21.7 38.6 102.9 85 61.3 46.6 Phenylalanine 157.1 206.6 160.9 162.1 134.3 177.9 130 151.2 189.7 176.3 174.7 154.4 133 141.1 156.7 177.1 Proline 118.8 139.9 169.7 132.4 235.8 205.9 220.3 243 142.1 146.5 179.4 142.3 149.4 175.2 230.7 134.7 Pyroglutamate 104.7 201.7 195.4 189.7 466.5 500.9 464.9 416.9 104.2 94.4 127 108.8 407.7 456.7 424.6 441.6 Pyruvate 8.8 12.9 3.7 15.4 12.5 38.5 25 179.4 243.8 296.6 411.7 162.3 158 387 416.8 Serine 107.4 90.3 87.1 83.5 250.9 144.7 202.9 181.9 148.9 178.8 193.8 169.2 170.8 157 193.4 188.3 Threonine 324.3 274.9 338.4 297.3 268.2 272.8 302.1 266.9 325.3 362.3 351.8 371.6 341.2 310.9 246.7 328.4 Tryptophan 31.1 22.8 22.6 17.5 25.8 23.3 22.2 24.6 28.5 27.3 11.6 28.4 27.9 27.8 12.2 26.7 Tyrosine 161.2 130.5 143.2 134.8 149.9 136.7 137.3 161.4 154.7 134 162 162 172.8 157.2 170.4 179.4 Uracil 19.8 10.3 28.8 18 11.8 6.8 19.6 20.7 Valine 232.2 180.6 203.4 189.7 250.6 226.7 252.1 244.4 305.9 366 342.4 354.9 305 339 325.2 341 myo-Inositol 53.4 51.1 69.6 62 56.2 48.7 61.8 62.6 62.3 58.8 74.6 69.1 62.9 59 74.7 91 NMR_METABOLITE_DATA_END #METABOLITES METABOLITES_START metabolite_name HMDB PubChem ChEBI KEGG METLIN 1-Methylnicotinamide HMDB0000699 457 16797 C02918 5667 2-Hydroxybutyrate HMDB0000008 440864 50613 C05984 3783 2-Oxoisocaproate HMDB0000695 70 48430 C00233 5663 3-Hydroxyisobutyrate HMDB0000023 440873 37373 C06001 483 Acetate HMDB0000042 176 15366 C00033 3206 Alanine HMDB0000161 5950 16977 C00041 NA Arginine HMDB0000517 6322 16467 C00062 5502 Asparagine HMDB0000168 6267 17196 C00152 14 Aspartate HMDB0000191 5960 17053 C00049 5206 Choline HMDB0000097 305 15354 C00114 56 Citrate HMDB0000094 311 30769 C00158 124 Ethanol HMDB0000108 702 16236 C00469 3203 Formate HMDB0304356 283 15740 NA NA Fumarate HMDB0000134 444972 18012 C00122 3242 Glucose HMDB0000122 5793 15903 C00031 133 Glutamate HMDB0000148 33032 16015 C00025 5174 Glutamine HMDB0000641 5961 18050 C00064 5614 Glycine HMDB0000123 750 15428 C00037 20 Histidine HMDB0000177 6274 15971 C00135 21 Hypoxanthine HMDB0000157 790 17368 C00262 83 Isobutyrate HMDB0001873 6590 16135 C02632 106 Isoleucine HMDB0000172 6306 17191 C00407 5193 Lactate HMDB0000190 107689 422 C00186 5205 Leucine HMDB0000687 6106 15603 C00123 24 Lysine HMDB0000182 5962 18019 C00047 5200 Methionine HMDB0000696 6137 16643 C00073 5664 Nicotinate HMDB0001488 938 15940 C00253 6272 Ornithine HMDB0000214 6262 15729 C00077 27 Phenylalanine HMDB0000159 6140 17295 C00079 28 Proline HMDB0000162 145742 17203 C00148 29 Pyroglutamate HMDB0000267 7405 18183 C01879 3251 Pyruvate HMDB0000243 1060 32816 C00022 117 Serine HMDB0000187 5951 17115 C00065 5203 Threonine HMDB0000167 6288 16857 C00188 32 Tryptophan HMDB0000929 6305 16828 C00078 5879 Tyrosine HMDB0000158 6057 17895 C00082 34 Uracil HMDB0000300 1174 17568 C00106 258 Valine HMDB0000883 6287 16414 C00183 5842 myo-Inositol HMDB0000211 NA 17268 C00137 5221 METABOLITES_END #END