#METABOLOMICS WORKBENCH wanglgene_20241206_112213 DATATRACK_ID:5437 STUDY_ID:ST003624 ANALYSIS_ID:AN005954 PROJECT_ID:PR002208 VERSION 1 CREATED_ON December 12, 2024, 6:32 pm #PROJECT PR:PROJECT_TITLE NRF2 supports non-small cell lung cancer growth independently of PR:PROJECT_TITLE CBP/p300-enhanced glutathione synthesis PR:PROJECT_TYPE MS quantitative analysis PR:PROJECT_SUMMARY Nuclear factor erythroid 2-related factor 2 (NRF2) is a stress responsive PR:PROJECT_SUMMARY transcription factor that is mutationally activated in a subset (~25%) of PR:PROJECT_SUMMARY clinically-aggressive non-small cell lung cancers (NSCLC). Mechanistic insight PR:PROJECT_SUMMARY into drivers of the NRF2 dependency remains poorly understood. Here, we defined PR:PROJECT_SUMMARY a novel NRF2 target gene set linked to NRF2-dependency in cancer cell lines, and PR:PROJECT_SUMMARY observed that a significant portion of these genes is devoid of PR:PROJECT_SUMMARY promoter-proximal NRF2. Using integrated genomic analyses, we characterized PR:PROJECT_SUMMARY extensive NRF2-dependent enhancer RNA (eRNA) synthesis and NRF2-mediated H3K27ac PR:PROJECT_SUMMARY deposition at proximal and distal enhancer regions regulating these genes. While PR:PROJECT_SUMMARY CBP/p300 is a well-validated direct interaction partner of NRF2 with prominent PR:PROJECT_SUMMARY functions at enhancers, we report that this interaction is not required for PR:PROJECT_SUMMARY NRF2-dependent NSCLC cell growth, indicating that NRF2 can sustain sufficient PR:PROJECT_SUMMARY transcriptional activity in the absence of CBP/p300 coactivation. Broad PR:PROJECT_SUMMARY metabolic profiling established a primary role for CBP/p300 in NRF2-dependent PR:PROJECT_SUMMARY accumulation of glutathione and glutathione-related metabolites. While redox PR:PROJECT_SUMMARY homeostasis via enhanced glutathione production is commonly associated with the PR:PROJECT_SUMMARY normal physiological role of NRF2, collectively our results suggest that PR:PROJECT_SUMMARY NRF2-dependent cancer cell growth does not require this enhanced glutathione PR:PROJECT_SUMMARY production. PR:INSTITUTE Genentech Inc. PR:LAST_NAME Wang PR:FIRST_NAME Mike Lingjue PR:ADDRESS 1 DNA Way, South San Francisco, CA 94404 PR:EMAIL wang.mike@gene.com PR:PHONE 650-245-7991 PR:CONTRIBUTORS Ryan J. Conrad, James A. Mondo, Mike Lingjue Wang, Peter S. Liu, Zijuan Lai, PR:CONTRIBUTORS Feroza K Choudhury, Qingling Li, Weng Ruh Wong, James Lee, Frances Shanahan, Eva PR:CONTRIBUTORS Lin, Scott Martin, Joachim Rudolph, John G. Moffat, Dewakar Sangaraju, Wendy PR:CONTRIBUTORS Sandoval, Timothy Sterne-Weiler, Scott A. Foster #STUDY ST:STUDY_TITLE NRF2 supports non-small cell lung cancer growth independently of ST:STUDY_TITLE CBP/p300-enhanced glutathione synthesis: Absolute Quantification of NADP+ and ST:STUDY_TITLE NADPH in A549 cells (Part 2 of 3) ST:STUDY_SUMMARY This study aims at directly quantifying NADPH, NADP+, and ratios of NADPH/NADP+ ST:STUDY_SUMMARY and its association with NRF2 to reveal NRF2 function in redox homeostasis. ST:STUDY_SUMMARY Briefly, cells were extracted by using acidified ACN/MeOH/water mixture with ST:STUDY_SUMMARY 15N-labeled ADP followed by adjusting pH to 8. Standard curve was established to ST:STUDY_SUMMARY quantify NADPH and NADP+ by using LC-HRMS. The result shows that when NRF2 is ST:STUDY_SUMMARY absent, both NADPH and NADP+ levels decrease. ST:INSTITUTE Genentech Inc. ST:LAST_NAME Wang ST:FIRST_NAME Mike ST:ADDRESS 1 DNA Way, South San Francisco, CA 94080, USA ST:EMAIL wang.mike@gene.com ST:PHONE 6502457991 #SUBJECT SU:SUBJECT_TYPE Cultured cells SU:SUBJECT_SPECIES Homo sapiens SU:TAXONOMY_ID 9606 SU:CELL_STRAIN_DETAILS A549 SU:SPECIES_GROUP Mammals #FACTORS #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 - Sample01 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Cell count (1E6)=23.23; RAW_FILE_NAME(Raw data)=20231005_017_neg_LunaNH2_CellG2_r2 SUBJECT_SAMPLE_FACTORS - Sample02 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Cell count (1E6)=23.23; RAW_FILE_NAME(Raw data)=20231005_024_neg_LunaNH2_CellG2_r3 SUBJECT_SAMPLE_FACTORS - Sample03 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Cell count (1E6)=23.23; RAW_FILE_NAME(Raw data)=20231005_031_neg_LunaNH2_CellG2_r4 SUBJECT_SAMPLE_FACTORS - Sample04 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Cell count (1E6)=23.23; RAW_FILE_NAME(Raw data)=20231005_038_neg_LunaNH2_CellG2_r5 SUBJECT_SAMPLE_FACTORS - Sample05 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Cell count (1E6)=23.23; RAW_FILE_NAME(Raw data)=20231005_045_neg_LunaNH2_CellG2_r1 SUBJECT_SAMPLE_FACTORS - Sample06 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Cell count (1E6)=28.5; RAW_FILE_NAME(Raw data)=20231005_020_neg_LunaNH2_CellG5_r5 SUBJECT_SAMPLE_FACTORS - Sample07 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Cell count (1E6)=28.5; RAW_FILE_NAME(Raw data)=20231005_027_neg_LunaNH2_CellG5_r1 SUBJECT_SAMPLE_FACTORS - Sample08 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Cell count (1E6)=28.5; RAW_FILE_NAME(Raw data)=20231005_034_neg_LunaNH2_CellG5_r2 SUBJECT_SAMPLE_FACTORS - Sample09 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Cell count (1E6)=28.5; RAW_FILE_NAME(Raw data)=20231005_041_neg_LunaNH2_CellG5_r3 SUBJECT_SAMPLE_FACTORS - Sample10 Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Cell count (1E6)=28.5; RAW_FILE_NAME(Raw data)=20231005_048_neg_LunaNH2_CellG5_r4 SUBJECT_SAMPLE_FACTORS - Sample11 Sample source:STD | Genotype:STD | Treatment:STD4 | Sample Label:39ng Cell count (1E6)=0; RAW_FILE_NAME(Raw data)=20231005_054_neg_LunaNH2_STD4_r2 SUBJECT_SAMPLE_FACTORS - Sample12 Sample source:STD | Genotype:STD | Treatment:STD5 | Sample Label:78ng Cell count (1E6)=0; RAW_FILE_NAME(Raw data)=20231005_055_neg_LunaNH2_STD5_r2 SUBJECT_SAMPLE_FACTORS - Sample13 Sample source:STD | Genotype:STD | Treatment:STD6 | Sample Label:156ng Cell count (1E6)=0; RAW_FILE_NAME(Raw data)=20231005_056_neg_LunaNH2_STD6_r2 SUBJECT_SAMPLE_FACTORS - Sample14 Sample source:STD | Genotype:STD | Treatment:STD7 | Sample Label:312ng Cell count (1E6)=0; RAW_FILE_NAME(Raw data)=20231005_057_neg_LunaNH2_STD7_r2 SUBJECT_SAMPLE_FACTORS - Sample15 Sample source:STD | Genotype:STD | Treatment:STD8 | Sample Label:625ng Cell count (1E6)=0; RAW_FILE_NAME(Raw data)=20231005_058_neg_LunaNH2_STD8_r2 SUBJECT_SAMPLE_FACTORS - Sample16 Sample source:STD | Genotype:STD | Treatment:STD9 | Sample Label:1250ng Cell count (1E6)=0; RAW_FILE_NAME(Raw data)=20231005_059_neg_LunaNH2_STD9_r2 #COLLECTION CO:COLLECTION_SUMMARY All cell lines were obtained from the Genentech cell bank (Yu et al, 2015) and CO:COLLECTION_SUMMARY grown in RPMI or DMEM supplemented with 10% FBS, 1% glutamine, and 1% CO:COLLECTION_SUMMARY penicillin-streptomycin at 37°C, 5% CO2. Cell lines were confirmed via STR CO:COLLECTION_SUMMARY profiling and were mycoplasma free. A549 and A549shNRF2-BIND rescue cell lines CO:COLLECTION_SUMMARY were generated using the Piggybac system. Donor constructs were co-transfected CO:COLLECTION_SUMMARY with transposase (Ding et al, 2005) at a 4:1 ratio using Lipofetamine 3000 CO:COLLECTION_SUMMARY (Thermo) according to manufacturer’s protocol. 3-days post-transfection, CO:COLLECTION_SUMMARY puromycin selection (1µg/mL) was initiated and was performed for ~2 weeks prior CO:COLLECTION_SUMMARY to experimentation. A549shNRF2-BIND rescue cells represent polyclonal pools. CO:COLLECTION_SUMMARY Cell viability was measured using CellTiter-Glo® Luminescent Cell Viability CO:COLLECTION_SUMMARY Assay (Promega) using the Envision 2103 Plate Reader (Promega). Cell growth CO:COLLECTION_SUMMARY curves were generated using the IncuCyte System (Sartorius) according to the CO:COLLECTION_SUMMARY manufacturer’s protocol. Curve fits were performed in Prism. Clonogenic assays CO:COLLECTION_SUMMARY were performed by washing cells in PBS, staining with 0.5% crystal violet CO:COLLECTION_SUMMARY solution (Sigma HT90132) for 5 min, and washing 3x with PBS. Four replicates of CO:COLLECTION_SUMMARY 20-30 million A549shNRF2-BIND-luc, WT NRF2 or Neh4/5mut cells were treated with CO:COLLECTION_SUMMARY 2.5ng/mL dox for 48h. CO:SAMPLE_TYPE Cultured cells #TREATMENT TR:TREATMENT_SUMMARY No treatment was administered and this is a study based on genetic variants. #SAMPLEPREP SP:SAMPLEPREP_SUMMARY Briefly, cells were harvested by washing with PBS twice and quenched on dry-ice SP:SAMPLEPREP_SUMMARY by adding acidified 2:2:1 ACN/MeOH/water with spiked-in 15N5-ADP (Sigma, St. SP:SAMPLEPREP_SUMMARY Louis, MO, USA) as an internal standard. 2M ammonium bicarbonate was then added SP:SAMPLEPREP_SUMMARY to adjust the pH to 8 (22:3 v/v). The extract was freeze-thawed by liquid SP:SAMPLEPREP_SUMMARY nitrogen and sonicated three times and centrifuged at 15,000 rpm for 15 minutes. SP:SAMPLEPREP_SUMMARY The supernatant was transferred and subjected to LC-MS analysis. The extract was SP:SAMPLEPREP_SUMMARY kept on ice in all steps. #CHROMATOGRAPHY CH:CHROMATOGRAPHY_TYPE HILIC CH:INSTRUMENT_NAME Shimadzu Nexera HPLC CH:COLUMN_NAME Phenomenex Luna-NH2 (50 x 2.1mm x 3um, 100Å) CH:SOLVENT_A 5% acetonitrile/95% water; 20 mM ammonium acetate; 20 mM ammonium hydroxide CH:SOLVENT_B 95% acetonitrile/5% water CH:FLOW_GRADIENT 0-0.5 min 60% B, 3-10 min 0% B, 11.5 60% B CH:FLOW_RATE 0.4 mL/min CH:COLUMN_TEMPERATURE 25 #ANALYSIS AN:ANALYSIS_TYPE MS #MS MS:INSTRUMENT_NAME Thermo Q Exactive Plus Orbitrap MS:INSTRUMENT_TYPE Orbitrap MS:MS_TYPE ESI MS:ION_MODE NEGATIVE MS:MS_COMMENTS Samples were run in negative mode. The Q Exactive Plus Mass Spectrometer was MS:MS_COMMENTS operated with the following parameters: Sheath gas flow rate, 50 units; Aux gas MS:MS_COMMENTS flow rate, 13 units; Aux gas temperature, 425 °C; Capillary temperature, MS:MS_COMMENTS 263°C; Spray voltage, -2600V; Scan mode, MS2 scan with data-dependent MS/MS MS:MS_COMMENTS acquisition. In Full MS scan, scan range is 60-900 m/z; resolution is 70,000; MS:MS_COMMENTS AGC target, 1×e^6; Maximum IT, 100 ms. In ddMS2 scan, top 5 ions are selected MS:MS_COMMENTS with an isolation window of 1.5 m/z; resolution is 17,500; AGC target, 5×e^4; MS:MS_COMMENTS Maximum IT, 50 ms. #MS_METABOLITE_DATA MS_METABOLITE_DATA:UNITS ng/mL MS_METABOLITE_DATA_START Samples Sample01 Sample02 Sample03 Sample04 Sample05 Sample06 Sample07 Sample08 Sample09 Sample10 Factors Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox- | Sample Label:Ctrl Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox Sample source:A549 Cell | Genotype:shNRF2-Luciferase | Treatment:Dox+ | Sample Label:Dox NADP+ 16.64757804 15.78449946 14.7285253 18.05020452 14.46820237 23.81487719 32.68421053 23.40870175 22.06673684 21.65224561 NADPH 45.77395048 52.91354144 47.33024758 53.15044133 46.33860065 62.95550877 62.77238596 62.58550877 55.60164912 64.98252632 MS_METABOLITE_DATA_END #METABOLITES METABOLITES_START metabolite_name Ion Adduct Formula Exact mass Super class Main class Sub class NADP+ [M-H]- C21H28N7O17P3 743.0755 Nucleic acids Nicotinamides Nicotinamide dinucleotides NADPH [M-2H]2- C21H30N7O17P3 745.0911 Nucleic acids Nicotinamides Nicotinamide dinucleotides METABOLITES_END #END