Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTCN76C1)

• DOT Name: Breakpoint cluster region protein (BCR)
• Synonyms: EC 2.7.11.1; Renal carcinoma antigen NY-REN-26
• Gene Name: BCR
• Related Disease:
  B-cell lymphoma
  Bipolar disorder
  Haematological malignancy
  Meningioma
  Small lymphocytic lymphoma
  Adult lymphoma
  Autoimmune disease
  Childhood myelodysplastic syndrome
  Chronic leukemia
  Classic Hodgkin lymphoma
  Colorectal carcinoma
  Follicular lymphoma
  Leukemia, myeloid, accelerated-phase
  Lymphoid leukemia
  Major depressive disorder
  Mantle cell lymphoma
  Mixed phenotype acute leukemia
  Myelodysplastic/myeloproliferative neoplasm
  Myeloid leukaemia
  Narcolepsy
  Non-hodgkin lymphoma
  Non-insulin dependent diabetes
  Pediatric lymphoma
  Plasma cell myeloma
  Primary myelofibrosis
  Promyelocytic leukaemia
  Rheumatoid arthritis
  T-cell acute lymphoblastic leukaemia
  Thrombocytopenia
  Thrombocytosis disease
  Abetalipoproteinemia
  Acute undifferentiated leukemia
  Chronic myelomonocytic leukaemia
  Immunodeficiency
  Lupus
  Myelofibrosis
  Prostate carcinoma
  T-cell leukaemia
  Wilms tumor
  Neoplasm
  Acute monocytic leukemia
  B-cell acute lymphoblastic leukaemia
  Burkitt lymphoma
  Prostate cancer
  Systemic lupus erythematosus
• UniProt ID: BCR_HUMAN
• PDB ID: 1K1F; 2AIN; 5N6R; 5N7E; 5OC7
• EC Number: 2.7.11.1
• Pfam ID: PF09036 ; PF00168 ; PF19057 ; PF00620 ; PF00621
• Sequence:
  MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQ
  TLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGE
  GSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNV
  EFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSC
  GVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQ
  STSEQEKRLTWPRRSYSPRSFEDCGGGYTPDCSSNENLTSSEEDFSSGQSSRVSPSPTTY
  RMFRDKSRSPSQNSQQSFDSSSPPTPQCHKRHRHCPVVVSEATIVGVRKTGQIWPNDGEG
  AFHGDADGSFGTPPGYGCAADRAEEQRRHQDGLPYIDDSPSSSPHLSSKGRGSRDALVSG
  ALESTKASELDLEKGLEMRKWVLSGILASEETYLSHLEALLLPMKPLKAAATTSQPVLTS
  QQIETIFFKVPELYEIHKEFYDGLFPRVQQWSHQQRVGDLFQKLASQLGVYRAFVDNYGV
  AMEMAEKCCQANAQFAEISENLRARSNKDAKDPTTKNSLETLLYKPVDRVTRSTLVLHDL
  LKHTPASHPDHPLLQDALRISQNFLSSINEEITPRRQSMTVKKGEHRQLLKDSFMVELVE
  GARKLRHVFLFTDLLLCTKLKKQSGGKTQQYDCKWYIPLTDLSFQMVDELEAVPNIPLVP
  DEELDALKIKISQIKNDIQREKRANKGSKATERLKKKLSEQESLLLLMSPSMAFRVHSRN
  GKSYTFLISSDYERAEWRENIREQQKKCFRSFSLTSVELQMLTNSCVKLQTVHSIPLTIN
  KEDDESPGLYGFLNVIVHSATGFKQSSNLYCTLEVDSFGYFVNKAKTRVYRDTAEPNWNE
  EFEIELEGSQTLRILCYEKCYNKTKIPKEDGESTDRLMGKGQVQLDPQALQDRDWQRTVI
  AMNGIEVKLSVKFNSREFSLKRMPSRKQTGVFGVKIAVVTKRERSKVPYIVRQCVEEIER
  RGMEEVGIYRVSGVATDIQALKAAFDVNNKDVSVMMSEMDVNAIAGTLKLYFRELPEPLF
  TDEFYPNFAEGIALSDPVAKESCMLNLLLSLPEANLLTFLFLLDHLKRVAEKEAVNKMSL
  HNLATVFGPTLLRPSEKESKLPANPSQPITMTDSWSLEVMSQVQVLLYFLQLEAIPAPDS
  KRQSILFSTEV
• Function: Protein with a unique structure having two opposing regulatory activities toward small GTP-binding proteins. The C-terminus is a GTPase-activating protein (GAP) domain which stimulates GTP hydrolysis by RAC1, RAC2 and CDC42. Accelerates the intrinsic rate of GTP hydrolysis of RAC1 or CDC42, leading to down-regulation of the active GTP-bound form. The central Dbl homology (DH) domain functions as guanine nucleotide exchange factor (GEF) that modulates the GTPases CDC42, RHOA and RAC1. Promotes the conversion of CDC42, RHOA and RAC1 from the GDP-bound to the GTP-bound form. The amino terminus contains an intrinsic kinase activity. Functions as an important negative regulator of neuronal RAC1 activity. Regulates macrophage functions such as CSF1-directed motility and phagocytosis through the modulation of RAC1 activity. Plays a major role as a RHOA GEF in keratinocytes being involved in focal adhesion formation and keratinocyte differentiation.
• KEGG Pathway:
  Pathways in cancer (hsa05200)
  Chronic myeloid leukemia (hsa05220)
• Reactome Pathway:
  Signaling by FGFR1 in disease (R-HSA-5655302)
  RHOA GTPase cycle (R-HSA-8980692)
  RHOB GTPase cycle (R-HSA-9013026)
  RHOC GTPase cycle (R-HSA-9013106)
  CDC42 GTPase cycle (R-HSA-9013148)
  RAC1 GTPase cycle (R-HSA-9013149)
  RAC2 GTPase cycle (R-HSA-9013404)
  RAC3 GTPase cycle (R-HSA-9013423)
  Signaling by cytosolic FGFR1 fusion mutants (R-HSA-1839117)

Molecular Interaction Atlas (MIA) of This DOT

45 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
B-cell lymphoma	DISIH1YQ	Definitive	Biomarker	[1]
Bipolar disorder	DISAM7J2	Definitive	Genetic Variation	[2]
Haematological malignancy	DISCDP7W	Definitive	Biomarker	[3]
Meningioma	DISPT4TG	Definitive	Biomarker	[4]
Small lymphocytic lymphoma	DIS30POX	Definitive	Biomarker	[5]
Adult lymphoma	DISK8IZR	Strong	Biomarker	[6]
Autoimmune disease	DISORMTM	Strong	Biomarker	[7]
Childhood myelodysplastic syndrome	DISMN80I	Strong	Biomarker	[8]
Chronic leukemia	DIS0C4XI	Strong	Biomarker	[9]
Classic Hodgkin lymphoma	DISV1LU6	Strong	Genetic Variation	[10]
Colorectal carcinoma	DIS5PYL0	Strong	Biomarker	[11]
Follicular lymphoma	DISVEUR6	Strong	Biomarker	[12]
Leukemia, myeloid, accelerated-phase	DISNDQL5	Strong	Altered Expression	[13]
Lymphoid leukemia	DIS65TYQ	Strong	Genetic Variation	[14]
Major depressive disorder	DIS4CL3X	Strong	Biomarker	[15]
Mantle cell lymphoma	DISFREOV	Strong	Biomarker	[16]
Mixed phenotype acute leukemia	DISNCHV9	Strong	Biomarker	[17]
Myelodysplastic/myeloproliferative neoplasm	DISDHXQ4	Strong	Biomarker	[18]
Myeloid leukaemia	DISMN944	Strong	Altered Expression	[19]
Narcolepsy	DISLCNLI	Strong	Genetic Variation	[20]
Non-hodgkin lymphoma	DISS2Y8A	Strong	Biomarker	[8]
Non-insulin dependent diabetes	DISK1O5Z	Strong	Biomarker	[21]
Pediatric lymphoma	DIS51BK2	Strong	Biomarker	[6]
Plasma cell myeloma	DIS0DFZ0	Strong	Genetic Variation	[6]
Primary myelofibrosis	DIS6L0CN	Strong	Genetic Variation	[22]
Promyelocytic leukaemia	DISYGG13	Strong	Biomarker	[23]
Rheumatoid arthritis	DISTSB4J	Strong	Biomarker	[24]
T-cell acute lymphoblastic leukaemia	DIS17AI2	Strong	Genetic Variation	[25]
Thrombocytopenia	DISU61YW	Strong	Biomarker	[26]
Thrombocytosis disease	DISNG0P4	Strong	Biomarker	[27]
Abetalipoproteinemia	DISMSS7T	moderate	Biomarker	[28]
Acute undifferentiated leukemia	DISJ4SSG	moderate	Biomarker	[29]
Chronic myelomonocytic leukaemia	DISDN5P7	moderate	Biomarker	[30]
Immunodeficiency	DIS093I0	moderate	Altered Expression	[31]
Lupus	DISOKJWA	moderate	Altered Expression	[32]
Myelofibrosis	DISIMP21	moderate	Biomarker	[33]
Prostate carcinoma	DISMJPLE	moderate	Biomarker	[34]
T-cell leukaemia	DISJ6YIF	moderate	Genetic Variation	[35]
Wilms tumor	DISB6T16	moderate	Biomarker	[36]
Neoplasm	DISZKGEW	Disputed	Biomarker	[37]
Acute monocytic leukemia	DIS28NEL	Limited	Biomarker	[38]
B-cell acute lymphoblastic leukaemia	DISKLOKC	Limited	Biomarker	[39]
Burkitt lymphoma	DIS9D5XU	Limited	Biomarker	[40]
Prostate cancer	DISF190Y	Limited	Biomarker	[34]
Systemic lupus erythematosus	DISI1SZ7	Limited	Biomarker	[41]

17 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the expression of Breakpoint cluster region protein (BCR).	[42]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Breakpoint cluster region protein (BCR).	[43]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate decreases the expression of Breakpoint cluster region protein (BCR).	[44]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of Breakpoint cluster region protein (BCR).	[45]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of Breakpoint cluster region protein (BCR).	[46]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Breakpoint cluster region protein (BCR).	[47]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Breakpoint cluster region protein (BCR).	[48]
Folic acid	DMEMBJC	Approved	Folic acid decreases the expression of Breakpoint cluster region protein (BCR).	[49]
Bortezomib	DMNO38U	Approved	Bortezomib decreases the expression of Breakpoint cluster region protein (BCR).	[50]
Irinotecan	DMP6SC2	Approved	Irinotecan decreases the expression of Breakpoint cluster region protein (BCR).	[51]
Dasatinib	DMJV2EK	Approved	Dasatinib decreases the activity of Breakpoint cluster region protein (BCR).	[52]
Sorafenib	DMS8IFC	Approved	Sorafenib decreases the activity of Breakpoint cluster region protein (BCR).	[53]
Imatinib	DM7RJXL	Approved	Imatinib decreases the activity of Breakpoint cluster region protein (BCR).	[54]
PMID28870136-Compound-48	DMPIM9L	Patented	PMID28870136-Compound-48 increases the expression of Breakpoint cluster region protein (BCR).	[58]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Breakpoint cluster region protein (BCR).	[60]
Chlorpyrifos	DMKPUI6	Investigative	Chlorpyrifos increases the expression of Breakpoint cluster region protein (BCR).	[61]
Rutin	DMEHRAJ	Investigative	Rutin decreases the expression of Breakpoint cluster region protein (BCR).	[62]

6 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Nilotinib	DM7HXWT	Approved	Nilotinib decreases the phosphorylation of Breakpoint cluster region protein (BCR).	[55]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the methylation of Breakpoint cluster region protein (BCR).	[56]
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 decreases the phosphorylation of Breakpoint cluster region protein (BCR).	[57]
PMID25656651-Compound-5	DMAI95U	Patented	PMID25656651-Compound-5 decreases the phosphorylation of Breakpoint cluster region protein (BCR).	[55]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A increases the methylation of Breakpoint cluster region protein (BCR).	[59]
Coumarin	DM0N8ZM	Investigative	Coumarin decreases the phosphorylation of Breakpoint cluster region protein (BCR).	[57]

References

• [1] Diffuse large B-cell lymphoma in Southeast Asian cohort: expression patterns of B-cell receptor (BCR) repertoire and its linkage with molecular subtypes and response to R-CHOP therapy.J Clin Pathol. 2019 Sep;72(9):630-635. doi: 10.1136/jclinpath-2019-205837. Epub 2019 Jun 12.
• [2] A possible association between missense polymorphism of the breakpoint cluster region gene and lithium prophylaxis in bipolar disorder.Prog Neuropsychopharmacol Biol Psychiatry. 2008 Jan 1;32(1):204-8. doi: 10.1016/j.pnpbp.2007.08.010. Epub 2007 Aug 19.
• [3] BCR: a promiscuous fusion partner in hematopoietic disorders.Oncotarget. 2019 Apr 12;10(28):2738-2754. doi: 10.18632/oncotarget.26837. eCollection 2019 Apr 12.
• [4] Pathological classification and molecular genetics of meningiomas.J Neurooncol. 2010 Sep;99(3):379-91. doi: 10.1007/s11060-010-0342-2. Epub 2010 Sep 1.
• [5] Overexpression of SH2-Containing Inositol Phosphatase Contributes to Chronic Lymphocytic Leukemia Survival.J Immunol. 2020 Jan 15;204(2):360-374. doi: 10.4049/jimmunol.1900153. Epub 2019 Dec 13.
• [6] Body size and obesity during adulthood, and risk of lympho-haematopoietic cancers: an update of the WCRF-AICR systematic review of published prospective studies.Ann Oncol. 2019 Apr 1;30(4):528-541. doi: 10.1093/annonc/mdz045.
• [7] Identification and Characterization of Post-activated B Cells in Systemic Autoimmune Diseases.Front Immunol. 2019 Sep 24;10:2136. doi: 10.3389/fimmu.2019.02136. eCollection 2019.
• [8] Leukopenia and lack of ribavirin predict poor outcomes in patients with haematological malignancies and respiratory syncytial virus infection.J Antimicrob Chemother. 2018 Nov 1;73(11):3162-3169. doi: 10.1093/jac/dky311.
• [9] NF-B pathways in hematological malignancies.Cell Mol Life Sci. 2014 Jun;71(11):2083-102. doi: 10.1007/s00018-013-1545-4. Epub 2014 Jan 14.
• [10] Chronic Myeloid Leukemia as Secondary Malignancy Following the Treatment of Hodgkin Lymphoma: A Case Series.Anticancer Res. 2019 Aug;39(8):4333-4335. doi: 10.21873/anticanres.13600.
• [11] No evidence for PML-RARa bcr1 fusion gene in colorectal cancer.Mol Biol Rep. 2012 May;39(5):5387-91. doi: 10.1007/s11033-011-1337-6. Epub 2011 Dec 14.
• [12] Follicular lymphoma (FL): Immunological tolerance theory in FL.Hum Immunol. 2017 Feb;78(2):138-145. doi: 10.1016/j.humimm.2016.09.010. Epub 2016 Sep 30.
• [13] Gadd45a deficiency accelerates BCR-ABL driven chronic myelogenous leukemia.Oncotarget. 2017 Feb 14;8(7):10809-10821. doi: 10.18632/oncotarget.14580.
• [14] A near-haploid clone harboring a BCR/ABL1 gene fusion in an adult patient with newly diagnosed B-lymphoblastic leukemia.Genes Chromosomes Cancer. 2019 Sep;58(9):665-668. doi: 10.1002/gcc.22744. Epub 2019 Mar 18.
• [15] The breakpoint cluster region gene on chromosome 22q11 is associated with bipolar disorder.Biol Psychiatry. 2005 May 15;57(10):1097-102. doi: 10.1016/j.biopsych.2005.02.019.
• [16] Pleiotropic Action of Novel Bruton's Tyrosine Kinase Inhibitor BGB-3111 in Mantle Cell Lymphoma.Mol Cancer Ther. 2019 Feb;18(2):267-277. doi: 10.1158/1535-7163.MCT-18-0478. Epub 2018 Nov 9.
• [17] Mixed-phenotype acute leukemia characteristics: first report from Iran.Clin Exp Med. 2018 Nov;18(4):513-521. doi: 10.1007/s10238-018-0520-7. Epub 2018 Jul 17.
• [18] Atypical neutrophilic panniculitis as presentation of BCR-ABL1-negative chronic myeloid leukaemia.BMJ Case Rep. 2019 Oct 8;12(10):e232005. doi: 10.1136/bcr-2019-232005.
• [19] Expression of BCR/ABL and BCL-2 in myeloid progenitors leads to myeloid leukemias.Proc Natl Acad Sci U S A. 2003 Aug 19;100(17):10002-7. doi: 10.1073/pnas.1633833100. Epub 2003 Jul 30.
• [20] Genome-wide association database developed in the Japanese Integrated Database Project.J Hum Genet. 2009 Sep;54(9):543-6. doi: 10.1038/jhg.2009.68. Epub 2009 Jul 24.
• [21] The LepR(db/db) mice model for studying glycation in the context of diabetes.Diabetes Metab Res Rev. 2019 Feb;35(2):e3103. doi: 10.1002/dmrr.3103. Epub 2019 Jan 7.
• [22] Systematization of analytical studies of polycythemia vera, essential thrombocythemia and primary myelofibrosis, and a meta-analysis of the frequency of JAK2, CALR and MPL mutations: 2000-2018.BMC Cancer. 2019 Jun 17;19(1):590. doi: 10.1186/s12885-019-5764-4.
• [23] Driving Toward Precision Medicine for Acute Leukemias: Are We There Yet?.Pharmacotherapy. 2017 Sep;37(9):1052-1072. doi: 10.1002/phar.1977. Epub 2017 Jul 31.
• [24] Effective quantification of 11 tyrosine kinase inhibitors and caffeine in human plasma by validated LC-MS/MS method with potent phospholipids clean-up procedure. Application to therapeutic drug monitoring.Talanta. 2020 Feb 1;208:120450. doi: 10.1016/j.talanta.2019.120450. Epub 2019 Oct 11.
• [25] Multidisciplinary analysis of pediatric T-ALL: 9q34 gene fusions.Cancer Genet. 2019 Feb;231-232:1-13. doi: 10.1016/j.cancergen.2018.12.002. Epub 2018 Dec 12.
• [26] Nilotinib first-line therapy in patients with Philadelphia chromosome-negative/BCR-ABL-positive chronic myeloid leukemia in chronic phase: ENEST1st sub-analysis.J Cancer Res Clin Oncol. 2017 Jul;143(7):1225-1233. doi: 10.1007/s00432-017-2359-9. Epub 2017 Feb 21.
• [27] A Rare Case of Pediatric Chronic Myelogenous Leukemia Presenting With Severe Thrombocytosis Without Leukocytosis.Pediatr Dev Pathol. 2018 Jan-Feb;21(1):100-104. doi: 10.1177/1093526617698601. Epub 2017 Mar 20.
• [28] A novel tricolor, dual-fusion fluorescence in situ hybridization method to detect BCR/ABL fusion in cells with t(9;22)(q34;q11.2) associated with deletion of DNA on the derivative chromosome 9 in chronic myelocytic leukemia.Cancer Genet Cytogenet. 2004 Jan 1;148(1):1-6. doi: 10.1016/s0165-4608(03)00202-4.
• [29] Spectrum and Immunophenotypic Profile of Acute Leukemia: A Tertiary Center Flow Cytometry Experience.Mediterr J Hematol Infect Dis. 2019 Mar 1;11(1):e2019017. doi: 10.4084/MJHID.2019.017. eCollection 2019.
• [30] Postallogeneic monitoring with molecular markers detected by pretransplant next-generation or Sanger sequencing predicts clinical relapse in patients with myelodysplastic/myeloproliferative neoplasms.Eur J Haematol. 2014 Mar;92(3):189-94. doi: 10.1111/ejh.12223. Epub 2013 Nov 21.
• [31] Transgenic expression of human cytokines in immunodeficient mice does not facilitate myeloid expansion of BCR-ABL1 transduced human cord blood cells.PLoS One. 2017 Oct 12;12(10):e0186035. doi: 10.1371/journal.pone.0186035. eCollection 2017.
• [32] Netting Neutrophils Activate Autoreactive B Cells in Lupus.J Immunol. 2018 May 15;200(10):3364-3371. doi: 10.4049/jimmunol.1700778. Epub 2018 Apr 9.
• [33] Understanding Splenomegaly in Myelofibrosis: Association with Molecular Pathogenesis.Int J Mol Sci. 2018 Mar 18;19(3):898. doi: 10.3390/ijms19030898.
• [34] Prediction nomogram for (68)Ga-PSMA-11 PET/CT in different clinical settings of PSA failure after radical treatment for prostate cancer.Eur J Nucl Med Mol Imaging. 2020 Jan;47(1):136-146. doi: 10.1007/s00259-019-04505-2. Epub 2019 Sep 6.
• [35] Expression of functional granulocyte colony-stimulating factor receptors on human B-lymphocytic leukemia cells.Ann Hematol. 2000 Mar;79(3):127-31. doi: 10.1007/s002770050567.
• [36] Deregulation of the Wilms' tumour gene 1 protein (WT1) by BCR/ABL1 mediates resistance to imatinib in human leukaemia cells.Leukemia. 2007 Dec;21(12):2485-94. doi: 10.1038/sj.leu.2404924. Epub 2007 Aug 30.
• [37] Current and evolving understanding of atypical chronic myeloid leukemia.Blood Rev. 2019 Jan;33:74-81. doi: 10.1016/j.blre.2018.07.004. Epub 2018 Jul 29.
• [38] Relatively favorable outcome after allogeneic stem cell transplantation for BCR-ABL1-positive AML: A survey from the acute leukemia working party of the European Society for blood and marrow transplantation (EBMT).Am J Hematol. 2018 Jan;93(1):31-39. doi: 10.1002/ajh.24928. Epub 2017 Oct 31.
• [39] Genomic Landscape of Adult and Pediatric BCR-ABL1-Like B-Lymphoblastic Leukemia Using Parallel DNA and RNA Sequencing.Oncologist. 2019 Mar;24(3):372-374. doi: 10.1634/theoncologist.2018-0272. Epub 2018 Sep 4.
• [40] Detection of Chromosomal Translocation in Hematologic Malignancies by a Novel DNA-Based Looped Ligation Assay (LOLA).Clin Chem. 2017 Jul;63(7):1278-1287. doi: 10.1373/clinchem.2016.270140. Epub 2017 May 17.
• [41] Altered recruitment of Lyn, Syk and ZAP-70 into lipid rafts of activated B cells in Systemic Lupus Erythematosus.Cell Signal. 2019 Jun;58:9-19. doi: 10.1016/j.cellsig.2019.03.003. Epub 2019 Mar 3.
• [42] Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
• [43] Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
• [44] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [45] Genistein and bisphenol A exposure cause estrogen receptor 1 to bind thousands of sites in a cell type-specific manner. Genome Res. 2012 Nov;22(11):2153-62.
• [46] Inhibition of prostate cancer cell colony formation by the flavonoid quercetin correlates with modulation of specific regulatory genes. Clin Diagn Lab Immunol. 2004 Jan;11(1):63-9. doi: 10.1128/cdli.11.1.63-69.2004.
• [47] Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
• [48] Cotreatment with the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) enhances imatinib-induced apoptosis of Bcr-Abl-positive human acute leukemia cells. Blood. 2003 Apr 15;101(8):3236-9. doi: 10.1182/blood-2002-08-2675. Epub 2002 Nov 21.
• [49] Folic acid supplementation dysregulates gene expression in lymphoblastoid cells--implications in nutrition. Biochem Biophys Res Commun. 2011 Sep 9;412(4):688-92. doi: 10.1016/j.bbrc.2011.08.027. Epub 2011 Aug 16.
• [50] The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
• [51] Clinical determinants of response to irinotecan-based therapy derived from cell line models. Clin Cancer Res. 2008 Oct 15;14(20):6647-55.
• [52] Combined BCR-ABL inhibition with lentiviral-delivered shRNA and dasatinib augments induction of apoptosis in Philadelphia-positive cells. Exp Hematol. 2009 Feb;37(2):206-14. doi: 10.1016/j.exphem.2008.10.013. Epub 2008 Dec 18.
• [53] Sorafenib induces apoptosis specifically in cells expressing BCR/ABL by inhibiting its kinase activity to activate the intrinsic mitochondrial pathway. Cancer Res. 2009 May 1;69(9):3927-36. doi: 10.1158/0008-5472.CAN-08-2978. Epub 2009 Apr 14.
• [54] Sensitivity to imatinib therapy may be predicted by testing Wilms tumor gene expression and colony growth after a short in vitro incubation. Cancer. 2004 Sep 1;101(5):979-88. doi: 10.1002/cncr.20457.
• [55] AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028.
• [56] Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
• [57] Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.
• [58] Global expression profiling of theophylline response genes in macrophages: evidence of airway anti-inflammatory regulation. Respir Res. 2005 Aug 8;6(1):89. doi: 10.1186/1465-9921-6-89.
• [59] Global and region-specific post-transcriptional and post-translational modifications of bisphenol A in human prostate cancer cells. Environ Pollut. 2019 Dec;255(Pt 2):113318. doi: 10.1016/j.envpol.2019.113318. Epub 2019 Oct 2.
• [60] From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
• [61] The common insecticides cyfluthrin and chlorpyrifos alter the expression of a subset of genes with diverse functions in primary human astrocytes. Toxicol Sci. 2006 Sep;93(1):125-35. doi: 10.1093/toxsci/kfl046. Epub 2006 Jun 21.
• [62] Epicatechin and a cocoa polyphenolic extract modulate gene expression in human Caco-2 cells. J Nutr. 2004 Oct;134(10):2509-16.