Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTZM3MJJ)

• DOT Name: Lysine-specific demethylase 6A (KDM6A)
• Synonyms: EC 1.14.11.68; Histone demethylase UTX; Ubiquitously-transcribed TPR protein on the X chromosome; Ubiquitously-transcribed X chromosome tetratricopeptide repeat protein; -trimethyl-L-lysine(27) demethylase 6A
• Gene Name: KDM6A
• Related Disease:
  Kabuki syndrome 2
  Neoplasm
  Acute myelogenous leukaemia
  Advanced cancer
  Autoimmune disease
  Benign neoplasm
  Bladder cancer
  Bone osteosarcoma
  Breast cancer
  Breast carcinoma
  Breast neoplasm
  Castration-resistant prostate carcinoma
  Chronic myelomonocytic leukemia
  Clear cell renal carcinoma
  Coloboma
  Colorectal carcinoma
  Esophageal squamous cell carcinoma
  Gastric cancer
  Myelodysplastic syndrome
  Nervous system inflammation
  Osteosarcoma
  Pancreatic cancer
  Plasma cell myeloma
  Promyelocytic leukaemia
  Prostate carcinoma
  Prostate neoplasm
  Sensorineural hearing loss disorder
  Stomach cancer
  T-cell acute lymphoblastic leukaemia
  Transitional cell carcinoma
  Urinary bladder cancer
  Urinary bladder neoplasm
  Diabetic kidney disease
  Medulloblastoma
  Kabuki syndrome
  Adult lymphoma
  Glioblastoma multiforme
  leukaemia
  Leukemia
  Lung cancer
  Lung carcinoma
  Lymphoma
  Melanoma
  Pediatric lymphoma
  Prostate cancer
  Renal cell carcinoma
  Turner syndrome
• UniProt ID: KDM6A_HUMAN
• PDB ID: 3AVR; 3AVS; 6FUK; 6FUL
• EC Number: 1.14.11.68
• Pfam ID: PF02373 ; PF21322 ; PF21326 ; PF13432 ; PF13181
• Sequence:
  MKSCGVSLATAAAAAAAFGDEEKKMAAGKASGESEEASPSLTAEEREALGGLDSRLFGFV
  RFHEDGARTKALLGKAVRCYESLILKAEGKVESDFFCQLGHFNLLLEDYPKALSAYQRYY
  SLQSDYWKNAAFLYGLGLVYFHYNAFQWAIKAFQEVLYVDPSFCRAKEIHLRLGLMFKVN
  TDYESSLKHFQLALVDCNPCTLSNAEIQFHIAHLYETQRKYHSAKEAYEQLLQTENLSAQ
  VKATVLQQLGWMHHTVDLLGDKATKESYAIQYLQKSLEADPNSGQSWYFLGRCYSSIGKV
  QDAFISYRQSIDKSEASADTWCSIGVLYQQQNQPMDALQAYICAVQLDHGHAAAWMDLGT
  LYESCNQPQDAIKCYLNATRSKSCSNTSALAARIKYLQAQLCNLPQGSLQNKTKLLPSIE
  EAWSLPIPAELTSRQGAMNTAQQNTSDNWSGGHAVSHPPVQQQAHSWCLTPQKLQHLEQL
  RANRNNLNPAQKLMLEQLESQFVLMQQHQMRPTGVAQVRSTGIPNGPTADSSLPTNSVSG
  QQPQLALTRVPSVSQPGVRPACPGQPLANGPFSAGHVPCSTSRTLGSTDTILIGNNHITG
  SGSNGNVPYLQRNALTLPHNRTNLTSSAEEPWKNQLSNSTQGLHKGQSSHSAGPNGERPL
  SSTGPSQHLQAAGSGIQNQNGHPTLPSNSVTQGAALNHLSSHTATSGGQQGITLTKESKP
  SGNILTVPETSRHTGETPNSTASVEGLPNHVHQMTADAVCSPSHGDSKSPGLLSSDNPQL
  SALLMGKANNNVGTGTCDKVNNIHPAVHTKTDNSVASSPSSAISTATPSPKSTEQTTTNS
  VTSLNSPHSGLHTINGEGMEESQSPMKTDLLLVNHKPSPQIIPSMSVSIYPSSAEVLKAC
  RNLGKNGLSNSSILLDKCPPPRPPSSPYPPLPKDKLNPPTPSIYLENKRDAFFPPLHQFC
  TNPNNPVTVIRGLAGALKLDLGLFSTKTLVEANNEHMVEVRTQLLQPADENWDPTGTKKI
  WHCESNRSHTTIAKYAQYQASSFQESLREENEKRSHHKDHSDSESTSSDNSGRRRKGPFK
  TIKFGTNIDLSDDKKWKLQLHELTKLPAFVRVVSAGNLLSHVGHTILGMNTVQLYMKVPG
  SRTPGHQENNNFCSVNINIGPGDCEWFVVPEGYWGVLNDFCEKNNLNFLMGSWWPNLEDL
  YEANVPVYRFIQRPGDLVWINAGTVHWVQAIGWCNNIAWNVGPLTACQYKLAVERYEWNK
  LQSVKSIVPMVHLSWNMARNIKVSDPKLFEMIKYCLLRTLKQCQTLREALIAAGKEIIWH
  GRTKEEPAHYCSICEVEVFDLLFVTNESNSRKTYIVHCQDCARKTSGNLENFVVLEQYKM
  EDLMQVYDQFTLAPPLPSASS
• Function: Histone demethylase that specifically demethylates 'Lys-27' of histone H3, thereby playing a central role in histone code. Demethylates trimethylated and dimethylated but not monomethylated H3 'Lys-27'. Plays a central role in regulation of posterior development, by regulating HOX gene expression. Demethylation of 'Lys-27' of histone H3 is concomitant with methylation of 'Lys-4' of histone H3, and regulates the recruitment of the PRC1 complex and monoubiquitination of histone H2A. Plays a demethylase-independent role in chromatin remodeling to regulate T-box family member-dependent gene expression.
• KEGG Pathway: Transcriptio.l misregulation in cancer (hsa05202)
• Reactome Pathway:
  Activation of anterior HOX genes in hindbrain development during early embryogenesis (R-HSA-5617472)
  Formation of WDR5-containing histone-modifying complexes (R-HSA-9772755)
  Chromatin modifications during the maternal to zygotic transition (MZT) (R-HSA-9821002)
  HDMs demethylate histones (R-HSA-3214842)
• BioCyc Pathway: MetaCyc:ENSG00000147050-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

47 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Kabuki syndrome 2	DISHI24Y	Definitive	X-linked	[1]
Neoplasm	DISZKGEW	Definitive	Genetic Variation	[2]
Acute myelogenous leukaemia	DISCSPTN	Strong	Genetic Variation	[2]
Advanced cancer	DISAT1Z9	Strong	Genetic Variation	[3]
Autoimmune disease	DISORMTM	Strong	Altered Expression	[4]
Benign neoplasm	DISDUXAD	Strong	Biomarker	[5]
Bladder cancer	DISUHNM0	Strong	Altered Expression	[6]
Bone osteosarcoma	DIST1004	Strong	Altered Expression	[7]
Breast cancer	DIS7DPX1	Strong	Biomarker	[8]
Breast carcinoma	DIS2UE88	Strong	Biomarker	[8]
Breast neoplasm	DISNGJLM	Strong	Biomarker	[9]
Castration-resistant prostate carcinoma	DISVGAE6	Strong	Biomarker	[10]
Chronic myelomonocytic leukemia	DISIL8UR	Strong	Genetic Variation	[11]
Clear cell renal carcinoma	DISBXRFJ	Strong	Biomarker	[12]
Coloboma	DISP39N5	Strong	Biomarker	[13]
Colorectal carcinoma	DIS5PYL0	Strong	Biomarker	[14]
Esophageal squamous cell carcinoma	DIS5N2GV	Strong	Biomarker	[15]
Gastric cancer	DISXGOUK	Strong	Biomarker	[16]
Myelodysplastic syndrome	DISYHNUI	Strong	Biomarker	[17]
Nervous system inflammation	DISB3X5A	Strong	Biomarker	[4]
Osteosarcoma	DISLQ7E2	Strong	Altered Expression	[7]
Pancreatic cancer	DISJC981	Strong	Biomarker	[18]
Plasma cell myeloma	DIS0DFZ0	Strong	Genetic Variation	[19]
Promyelocytic leukaemia	DISYGG13	Strong	Biomarker	[20]
Prostate carcinoma	DISMJPLE	Strong	Biomarker	[21]
Prostate neoplasm	DISHDKGQ	Strong	Biomarker	[22]
Sensorineural hearing loss disorder	DISJV45Z	Strong	Biomarker	[23]
Stomach cancer	DISKIJSX	Strong	Biomarker	[16]
T-cell acute lymphoblastic leukaemia	DIS17AI2	Strong	Biomarker	[24]
Transitional cell carcinoma	DISWVVDR	Strong	Biomarker	[25]
Urinary bladder cancer	DISDV4T7	Strong	Altered Expression	[6]
Urinary bladder neoplasm	DIS7HACE	Strong	Altered Expression	[6]
Diabetic kidney disease	DISJMWEY	moderate	Biomarker	[26]
Medulloblastoma	DISZD2ZL	moderate	Altered Expression	[27]
Kabuki syndrome	DISZN97H	Supportive	Autosomal dominant	[28]
Adult lymphoma	DISK8IZR	Limited	Genetic Variation	[29]
Glioblastoma multiforme	DISK8246	Limited	Altered Expression	[30]
leukaemia	DISS7D1V	Limited	Biomarker	[31]
Leukemia	DISNAKFL	Limited	Biomarker	[31]
Lung cancer	DISCM4YA	Limited	Altered Expression	[32]
Lung carcinoma	DISTR26C	Limited	Altered Expression	[32]
Lymphoma	DISN6V4S	Limited	Genetic Variation	[29]
Melanoma	DIS1RRCY	Limited	Genetic Variation	[33]
Pediatric lymphoma	DIS51BK2	Limited	Genetic Variation	[29]
Prostate cancer	DISF190Y	Limited	Biomarker	[21]
Renal cell carcinoma	DISQZ2X8	Limited	Biomarker	[12]
Turner syndrome	DIS2035C	Limited	Biomarker	[34]

This DOT Affected the Drug Response of 1 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Methotrexate	DM2TEOL	Approved	Lysine-specific demethylase 6A (KDM6A) affects the response to substance of Methotrexate.	[52]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate affects the expression of Lysine-specific demethylase 6A (KDM6A).	[35]
Ciclosporin	DMAZJFX	Approved	Ciclosporin increases the expression of Lysine-specific demethylase 6A (KDM6A).	[36]
Tretinoin	DM49DUI	Approved	Tretinoin increases the expression of Lysine-specific demethylase 6A (KDM6A).	[37]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[38]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate increases the expression of Lysine-specific demethylase 6A (KDM6A).	[39]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[40]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[41]
Triclosan	DMZUR4N	Approved	Triclosan decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[42]
Hydroquinone	DM6AVR4	Approved	Hydroquinone decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[43]
Testosterone enanthate	DMB6871	Approved	Testosterone enanthate affects the expression of Lysine-specific demethylase 6A (KDM6A).	[44]
Berberine	DMC5Q8X	Phase 4	Berberine increases the expression of Lysine-specific demethylase 6A (KDM6A).	[45]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 increases the expression of Lysine-specific demethylase 6A (KDM6A).	[47]
Leflunomide	DMR8ONJ	Phase 1 Trial	Leflunomide increases the expression of Lysine-specific demethylase 6A (KDM6A).	[48]
Geldanamycin	DMS7TC5	Discontinued in Phase 2	Geldanamycin increases the expression of Lysine-specific demethylase 6A (KDM6A).	[49]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[50]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde decreases the expression of Lysine-specific demethylase 6A (KDM6A).	[51]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene affects the methylation of Lysine-specific demethylase 6A (KDM6A).	[46]

References

• [1] Technical standards for the interpretation and reporting of constitutional copy-number variants: a joint consensus recommendation of the American College of Medical Genetics and Genomics (ACMG) and the Clinical Genome Resource (ClinGen). Genet Med. 2020 Feb;22(2):245-257. doi: 10.1038/s41436-019-0686-8. Epub 2019 Nov 6.
• [2] Loss of KDM6A confers drug resistance in acute myeloid leukemia.Leukemia. 2020 Jan;34(1):50-62. doi: 10.1038/s41375-019-0497-6. Epub 2019 Jun 14.
• [3] UTX Mutations in Human Cancer.Cancer Cell. 2019 Feb 11;35(2):168-176. doi: 10.1016/j.ccell.2019.01.001.
• [4] X-tra X: An escape to autoimmunity.J Clin Invest. 2019 Aug 12;129(9):3536-3538. doi: 10.1172/JCI130312. eCollection 2019 Aug 12.
• [5] Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer.Nat Genet. 2009 May;41(5):521-3. doi: 10.1038/ng.349. Epub 2009 Mar 29.
• [6] Loss of tumor suppressor KDM6A amplifies PRC2-regulated transcriptional repression in bladder cancer and can be targeted through inhibition of EZH2.Sci Transl Med. 2017 Feb 22;9(378):eaai8312. doi: 10.1126/scitranslmed.aai8312.
• [7] Epigenetic Profiling Identifies LIF as a Super-enhancer-Controlled Regulator of Stem Cell-like Properties in Osteosarcoma.Mol Cancer Res. 2020 Jan;18(1):57-67. doi: 10.1158/1541-7786.MCR-19-0470. Epub 2019 Oct 15.
• [8] GATA3 recruits UTX for gene transcriptional activation to suppress metastasis of breast cancer.Cell Death Dis. 2019 Nov 4;10(11):832. doi: 10.1038/s41419-019-2062-7.
• [9] Histone-modifier gene expression profiles are associated with pathological and clinical outcomes in human breast cancer.Anticancer Res. 2011 Dec;31(12):4115-25.
• [10] Inhibitor of H3K27 demethylase JMJD3/UTX GSK-J4 is a potential therapeutic option for castration resistant prostate cancer.Oncotarget. 2017 Jul 8;8(37):62131-62142. doi: 10.18632/oncotarget.19100. eCollection 2017 Sep 22.
• [11] Utx loss causes myeloid transformation.Leukemia. 2018 Jun;32(6):1458-1465. doi: 10.1038/s41375-018-0011-6. Epub 2018 Feb 2.
• [12] Biochemical and Epigenetic Insights into L-2-Hydroxyglutarate, a Potential Therapeutic Target in Renal Cancer.Clin Cancer Res. 2018 Dec 15;24(24):6433-6446. doi: 10.1158/1078-0432.CCR-18-1727. Epub 2018 Aug 14.
• [13] A case of exudative vitreoretinopathy and chorioretinal coloboma associated with microcephaly in a female with contiguous Xp11.3-11.4 deletion.Ophthalmic Genet. 2018 Jun;39(3):396-398. doi: 10.1080/13816810.2018.1443342. Epub 2018 Apr 4.
• [14] A Specific Mutational Signature Associated with DNA 8-Oxoguanine Persistence in MUTYH-defective Colorectal Cancer.EBioMedicine. 2017 Jun;20:39-49. doi: 10.1016/j.ebiom.2017.04.022. Epub 2017 Apr 13.
• [15] The Prognostic Significance of Histone Demethylase UTX in Esophageal Squamous Cell Carcinoma.Int J Mol Sci. 2018 Jan 19;19(1):297. doi: 10.3390/ijms19010297.
• [16] Synergistic triad epistasis of epigenetic H3K27me modifier genes, EZH2, KDM6A, and KDM6B, in gastric cancer susceptibility.Gastric Cancer. 2019 May;22(3):640-644. doi: 10.1007/s10120-018-0888-9. Epub 2018 Oct 29.
• [17] Epigenetic drug library screening identified an LSD1 inhibitor to target UTX-deficient cells for differentiation therapy.Signal Transduct Target Ther. 2019 Apr 26;4:11. doi: 10.1038/s41392-019-0040-2. eCollection 2019.
• [18] Loss of KDM6A characterizes a poor prognostic subtype of human pancreatic cancer and potentiates HDAC inhibitor lethality.Int J Cancer. 2019 Jul 1;145(1):192-205. doi: 10.1002/ijc.32072. Epub 2018 Dec 30.
• [19] UTX/KDM6A Loss Enhances the Malignant Phenotype of Multiple Myeloma and Sensitizes Cells to EZH2 inhibition.Cell Rep. 2017 Oct 17;21(3):628-640. doi: 10.1016/j.celrep.2017.09.078.
• [20] Sequencing a mouse acute promyelocytic leukemia genome reveals genetic events relevant for disease progression.J Clin Invest. 2011 Apr;121(4):1445-55. doi: 10.1172/JCI45284. Epub 2011 Mar 23.
• [21] The histone demethylase UTX/KDM6A in cancer: Progress and puzzles.Int J Cancer. 2019 Aug 1;145(3):614-620. doi: 10.1002/ijc.32116. Epub 2019 Jan 28.
• [22] The long tail of oncogenic drivers in prostate cancer.Nat Genet. 2018 May;50(5):645-651. doi: 10.1038/s41588-018-0078-z. Epub 2018 Apr 2.
• [23] Clinical update on sensorineural hearing loss in Turner syndrome and the X-chromosome.Am J Med Genet C Semin Med Genet. 2019 Mar;181(1):18-24. doi: 10.1002/ajmg.c.31673. Epub 2019 Jan 10.
• [24] UTX inhibition as selective epigenetic therapy against TAL1-driven T-cell acute lymphoblastic leukemia.Genes Dev. 2016 Mar 1;30(5):508-21. doi: 10.1101/gad.276790.115.
• [25] Contingencies of UTX/KDM6A Action in Urothelial Carcinoma.Cancers (Basel). 2019 Apr 4;11(4):481. doi: 10.3390/cancers11040481.
• [26] Histone demethylase UTX is a therapeutic target for diabetic kidney disease.J Physiol. 2019 Mar;597(6):1643-1660. doi: 10.1113/JP277367. Epub 2018 Dec 25.
• [27] Trimethylation of H3K27 during human cerebellar development in relation to medulloblastoma.Oncotarget. 2017 Sep 8;8(45):78978-78988. doi: 10.18632/oncotarget.20741. eCollection 2017 Oct 3.
• [28] Kabuki Syndrome. 2011 Sep 1 [updated 2024 Apr 25]. In: Adam MP, Feldman J, Mirzaa GM, Pagon RA, Wallace SE, Bean LJH, Gripp KW, Amemiya A, editors. GeneReviews(?) [Internet]. Seattle (WA): University of Washington, Seattle; 1993C2024.
• [29] Epstein-Barr virus-negative extranodal "true" natural killer-cell lymphoma harbouring a KDM6A mutation.Hematol Oncol. 2018 Feb;36(1):328-335. doi: 10.1002/hon.2459. Epub 2017 Jul 10.
• [30] Increased expression of the histone H3 lysine 4 methyltransferase MLL4 and the histone H3 lysine 27 demethylase UTX prolonging the overall survival of patients with glioblastoma and a methylated MGMT promoter.J Neurosurg. 2017 May;126(5):1461-1471. doi: 10.3171/2016.4.JNS1652. Epub 2016 Jul 1.
• [31] MBD3/NuRD loss participates with KDM6A program to promote DOCK5/8 expression and Rac GTPase activation in human acute myeloid leukemia.FASEB J. 2019 Apr;33(4):5268-5286. doi: 10.1096/fj.201801035R. Epub 2019 Jan 22.
• [32] Epigenetic regulation of epithelial-mesenchymal transition by KDM6A histone demethylase in lung cancer cells.Biochem Biophys Res Commun. 2017 Sep 2;490(4):1407-1413. doi: 10.1016/j.bbrc.2017.07.048. Epub 2017 Jul 8.
• [33] Identification of gene expression levels in primary melanoma associated with clinically meaningful characteristics.Melanoma Res. 2018 Oct;28(5):380-389. doi: 10.1097/CMR.0000000000000473.
• [34] Congenital Hyperinsulinism in Infants with Turner Syndrome: Possible Association with Monosomy X and KDM6A Haploinsufficiency.Horm Res Paediatr. 2018;89(6):413-422. doi: 10.1159/000488347. Epub 2018 Jun 14.
• [35] Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
• [36] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [37] 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.
• [38] Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
• [39] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [40] Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
• [41] The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
• [42] Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
• [43] Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
• [44] Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
• [45] Berberine acts as a putative epigenetic modulator by affecting the histone code. Toxicol In Vitro. 2016 Oct;36:10-17. doi: 10.1016/j.tiv.2016.06.004. Epub 2016 Jun 13.
• [46] Effect of aflatoxin B(1), benzo[a]pyrene, and methapyrilene on transcriptomic and epigenetic alterations in human liver HepaRG cells. Food Chem Toxicol. 2018 Nov;121:214-223. doi: 10.1016/j.fct.2018.08.034. Epub 2018 Aug 26.
• [47] BET bromodomain inhibition as a novel strategy for reactivation of HIV-1. J Leukoc Biol. 2012 Dec;92(6):1147-54. doi: 10.1189/jlb.0312165. Epub 2012 Jul 16.
• [48] Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
• [49] Identification of transcriptome signatures and biomarkers specific for potential developmental toxicants inhibiting human neural crest cell migration. Arch Toxicol. 2016 Jan;90(1):159-80.
• [50] A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
• [51] Gene expression changes in primary human nasal epithelial cells exposed to formaldehyde in vitro. Toxicol Lett. 2010 Oct 5;198(2):289-95.
• [52] Gene expression profiling of 30 cancer cell lines predicts resistance towards 11 anticancer drugs at clinically achieved concentrations. Int J Cancer. 2006 Apr 1;118(7):1699-712. doi: 10.1002/ijc.21570.