General Information of Drug Combination (ID: DCTG5LS)

Drug Combination Name
Romidepsin Azacitidine
Indication
Disease Entry Status REF
Malignant melanoma Investigative [1]
Component Drugs Romidepsin   DMT5GNL Azacitidine   DMTA5OE
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: UACC62
Zero Interaction Potency (ZIP) Score: 4.03
Bliss Independence Score: 2.84
Loewe Additivity Score: 2.26
LHighest Single Agent (HSA) Score: 5.68

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Romidepsin
Disease Entry ICD 11 Status REF
Cutaneous T-cell lymphoma 2B01 Approved [2]
Gastrin-producing neuroendocrine tumor N.A. Approved [3]
Glucagonoma N.A. Approved [3]
Insulinoma 2C10.1 Approved [3]
Lung carcinoid tumor N.A. Approved [3]
Melanoma 2C30 Approved [3]
Primary cutaneous peripheral T-cell lymphoma not otherwise specified N.A. Approved [3]
Primary cutaneous T-cell lymphoma N.A. Approved [3]
Urethral cancer 2C93 Approved [3]
Peripheral T-cell lymphoma 2A90.C Phase 3 [4]
Renal cell carcinoma 2C90 Phase 3 [2]
Romidepsin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Histone deacetylase 1 (HDAC1) TT6R7JZ HDAC1_HUMAN Inhibitor [9]
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Romidepsin Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [10]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [10]
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Romidepsin Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [11]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [12]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Metabolism [13]
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Romidepsin Interacts with 41 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Increases Expression [14]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Affects Expression [15]
E3 SUMO-protein ligase CBX4 (CBX4) OT4XVRRF CBX4_HUMAN Increases Expression [16]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Increases Expression [17]
Bcl-2-like protein 11 (BCL2L11) OTNQQWFJ B2L11_HUMAN Increases Expression [18]
Growth arrest and DNA damage-inducible protein GADD45 beta (GADD45B) OTL9I7LO GA45B_HUMAN Increases Expression [19]
Serine/threonine-protein kinase 17B (STK17B) OT4NYNO8 ST17B_HUMAN Increases Expression [16]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Expression [20]
RAF proto-oncogene serine/threonine-protein kinase (RAF1) OT51LSFO RAF1_HUMAN Decreases Expression [20]
Receptor tyrosine-protein kinase erbB-2 (ERBB2) OTOAUNCK ERBB2_HUMAN Decreases Expression [20]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Decreases Phosphorylation [20]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [21]
Clusterin (CLU) OTQGG0JM CLUS_HUMAN Increases Expression [16]
G2/mitotic-specific cyclin-B1 (CCNB1) OT19S7E5 CCNB1_HUMAN Decreases Expression [20]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Phosphorylation [8]
Transcription factor JunD (JUND) OTNKACJD JUND_HUMAN Increases Expression [16]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Increases Expression [21]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [20]
NF-kappa-B inhibitor alpha (NFKBIA) OTFT924M IKBA_HUMAN Increases Expression [21]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [8]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [8]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Increases Phosphorylation [22]
Receptor-type tyrosine-protein kinase FLT3 (FLT3) OTMSRYMK FLT3_HUMAN Decreases Phosphorylation [8]
Sterol regulatory element-binding protein 1 (SREBF1) OTWBRPAI SRBP1_HUMAN Increases Expression [16]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [23]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Activity [20]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Increases Cleavage [21]
Friend leukemia integration 1 transcription factor (FLI1) OT0EV3LX FLI1_HUMAN Decreases Expression [24]
RNA-binding protein EWS (EWSR1) OT7SRHV3 EWS_HUMAN Decreases Expression [24]
DNA repair protein RAD51 homolog 1 (RAD51) OTNVWGC1 RAD51_HUMAN Decreases Expression [8]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Increases Expression [22]
Bcl-2-interacting killer (BIK) OTTH1T3D BIK_HUMAN Increases Expression [16]
Spectrin alpha chain, non-erythrocytic 1 (SPTAN1) OT6VY3A3 SPTN1_HUMAN Increases Expression [16]
Nuclear receptor subfamily 1 group I member 3 (NR1I3) OTS3SGH7 NR1I3_HUMAN Increases Expression [25]
Bcl-2 homologous antagonist/killer (BAK1) OTDP6ILW BAK_HUMAN Increases Expression [22]
Histone H3.1t (H3-4) OTY6ITYF H31T_HUMAN Increases Acetylation [25]
Sodium/iodide cotransporter (SLC5A5) OTU7E9G7 SC5A5_HUMAN Increases Expression [26]
Mitogen-activated protein kinase kinase kinase 3 (MAP3K3) OT53LJGW M3K3_HUMAN Increases Expression [16]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Affects Metabolism [27]
Multidrug resistance-associated protein 1 (ABCC1) OTGUN89S MRP1_HUMAN Decreases Response To Substance [28]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Decreases Response To Substance [21]
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⏷ Show the Full List of 41 DOT(s)
Indication(s) of Azacitidine
Disease Entry ICD 11 Status REF
Acute myelogenous leukaemia 2A41 Approved [5]
Chronic myelomonocytic leukemia N.A. Approved [5]
Leukemia N.A. Approved [5]
Myelodysplastic syndrome 2A37 Approved [6]
Myeloproliferative neoplasm 2A20 Approved [5]
Plasma cell myeloma 2A83.1 Approved [5]
Azacitidine Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
DNA [cytosine-5]-methyltransferase (DNMT) TTHVCUP NOUNIPROTAC Inhibitor [33]
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Azacitidine Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytidine aminohydrolase (CDA) DEKEDRC CDD_HUMAN Metabolism [34]
Cytidine deaminase (cdd) DEYILK4 E0TLJ6_MYCHH Metabolism [35]
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Azacitidine Interacts with 275 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Affects Expression [36]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Expression [37]
Cytochrome P450 1A2 (CYP1A2) OTLLBX48 CP1A2_HUMAN Increases Expression [37]
Aryl hydrocarbon receptor (AHR) OTFE4EYE AHR_HUMAN Increases Expression [37]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Increases Expression [37]
Sulfotransferase 1C2 (SULT1C2) OT07MMZS ST1C2_HUMAN Increases Expression [29]
Phospholipid phosphatase 1 (PLPP1) OT0IIMI5 PLPP1_HUMAN Increases Expression [29]
Tectonin beta-propeller repeat-containing protein 2 (TECPR2) OT1UFECZ TCPR2_HUMAN Increases Expression [29]
TBC1 domain family member 4 (TBC1D4) OTK66C40 TBCD4_HUMAN Decreases Expression [29]
Multiple epidermal growth factor-like domains protein 6 (MEGF6) OTEUYTP1 MEGF6_HUMAN Decreases Expression [29]
Stanniocalcin-2 (STC2) OT86YP8G STC2_HUMAN Decreases Expression [29]
Integrin beta-2 (ITGB2) OTEKPEPR ITB2_HUMAN Decreases Expression [29]
Protein S100-A9 (S100A9) OTOARHCS S10A9_HUMAN Increases Expression [29]
Receptor-type tyrosine-protein phosphatase C (PTPRC) OT6KOR77 PTPRC_HUMAN Increases Expression [29]
Delta-aminolevulinic acid dehydratase (ALAD) OTHM9GSH HEM2_HUMAN Decreases Expression [29]
Hepatocyte growth factor (HGF) OTGHUA23 HGF_HUMAN Increases Expression [29]
Heat shock 70 kDa protein 6 (HSPA6) OTH4S7WB HSP76_HUMAN Increases Expression [29]
Gamma-aminobutyric acid receptor subunit beta-1 (GABRB1) OT4L2SSB GBRB1_HUMAN Increases Expression [29]
Transcription factor E3 (TFE3) OTM99ZWH TFE3_HUMAN Increases Expression [29]
Pro-thyrotropin-releasing hormone (TRH) OT02UY2V TRH_HUMAN Decreases Expression [29]
Protein S100-P (S100P) OTJCXNJG S100P_HUMAN Increases Expression [29]
Protein PML (PML) OT6SM2GD PML_HUMAN Increases Expression [29]
DNA-binding protein inhibitor ID-1 (ID1) OTKGNZN5 ID1_HUMAN Increases Expression [29]
Cyclin-dependent kinase 4 inhibitor B (CDKN2B) OTAG24N1 CDN2B_HUMAN Decreases Methylation [29]
LIM and senescent cell antigen-like-containing domain protein 1 (LIMS1) OT729S0T LIMS1_HUMAN Increases Expression [29]
E3 SUMO-protein ligase RanBP2 (RANBP2) OTFG5CVF RBP2_HUMAN Increases Expression [29]
Cyclin-dependent kinase inhibitor 1C (CDKN1C) OTASTJ3Q CDN1C_HUMAN Increases Expression [29]
Ras-related protein Rab-13 (RAB13) OTIQ484I RAB13_HUMAN Decreases Methylation [29]
Lysozyme C (LYZ) OTD7H0G6 LYSC_HUMAN Increases Expression [29]
Claudin-10 (CLDN10) OT2CVAKY CLD10_HUMAN Decreases Expression [29]
Sushi repeat-containing protein SRPX (SRPX) OT5B9LXS SRPX_HUMAN Decreases Expression [29]
Protein delta homolog 1 (DLK1) OTE1VLNB DLK1_HUMAN Decreases Methylation [29]
DNA-binding protein inhibitor ID-3 (ID3) OTUULW5Z ID3_HUMAN Increases Expression [29]
Collagen alpha-1(XIV) chain (COL14A1) OTLNJ13O COEA1_HUMAN Increases Expression [29]
Equilibrative nucleoside transporter 2 (SLC29A2) OTUAOB8T S29A2_HUMAN Decreases Expression [29]
Cytohesin-1 (CYTH1) OTYH9NRJ CYH1_HUMAN Increases Expression [29]
C3a anaphylatoxin chemotactic receptor (C3AR1) OT8J0TF8 C3AR_HUMAN Increases Expression [29]
DNA dC->dU-editing enzyme APOBEC-3F (APOBEC3F) OT750IJM ABC3F_HUMAN Increases Expression [29]
Angiogenic factor with G patch and FHA domains 1 (AGGF1) OTA7U2T8 AGGF1_HUMAN Increases Expression [29]
E3 ubiquitin-protein ligase Praja-1 (PJA1) OTFKTMEI PJA1_HUMAN Increases Expression [29]
Caspase-10 (CASP10) OTE6J88E CASPA_HUMAN Increases Expression [29]
Tetraspanin-32 (TSPAN32) OTSXW7EW TSN32_HUMAN Decreases Expression [29]
Tribbles homolog 1 (TRIB1) OTPEO17G TRIB1_HUMAN Decreases Expression [29]
Lipopolysaccharide-induced tumor necrosis factor-alpha factor (LITAF) OTT5JX1F LITAF_HUMAN Decreases Expression [29]
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha (PIP5K1A) OTVTB5R5 PI51A_HUMAN Decreases Expression [29]
Centromere protein O (CENPO) OTXAH83Y CENPO_HUMAN Increases Expression [29]
Iron-sulfur cluster assembly 1 homolog, mitochondrial (ISCA1) OTU230MC ISCA1_HUMAN Increases Expression [29]
E3 ubiquitin-protein ligase TRIM8 (TRIM8) OTS6JFR0 TRIM8_HUMAN Increases Expression [29]
Uncharacterized protein C6orf62 (C6ORF62) OTGK4G35 CF062_HUMAN Increases Expression [29]
Metal transporter CNNM2 (CNNM2) OTZHO8WU CNNM2_HUMAN Decreases Expression [29]
Pantothenate kinase 3 (PANK3) OT77CFJ6 PANK3_HUMAN Decreases Expression [29]
DNA dC->dU-editing enzyme APOBEC-3G (APOBEC3G) OT410VP5 ABC3G_HUMAN Increases Expression [29]
Neuritin (NRN1) OTWJG0SO NRN1_HUMAN Decreases Expression [29]
NTF2-related export protein 2 (NXT2) OTK82YVT NXT2_HUMAN Increases Expression [29]
THUMP domain-containing protein 1 (THUMPD1) OTKU8KWH THUM1_HUMAN Increases Expression [29]
Protein FAM8A1 (FAM8A1) OT1QVTGS FA8A1_HUMAN Increases Expression [29]
Type 2 lactosamine alpha-2,3-sialyltransferase (ST3GAL6) OTB17Q43 SIA10_HUMAN Increases Expression [29]
Methionine-R-sulfoxide reductase B2, mitochondrial (MSRB2) OTURGRA8 MSRB2_HUMAN Increases Expression [29]
Mitotic spindle assembly checkpoint protein MAD1 (MAD1L1) OTJCX8K9 MD1L1_HUMAN Decreases Expression [29]
Signal-regulatory protein beta-1 (SIRPB1) OTGHALWJ SIRB1_HUMAN Decreases Expression [30]
Syntenin-1 (SDCBP) OTS3NCC5 SDCB1_HUMAN Decreases Expression [30]
Complexin-1 (CPLX1) OT7UIGTP CPLX1_HUMAN Increases Expression [30]
Nephrocystin-1 (NPHP1) OTZHCFFQ NPHP1_HUMAN Increases Expression [30]
Phosphatase and actin regulator 2 (PHACTR2) OTWMX2A8 PHAR2_HUMAN Increases Expression [30]
Nuclear factor of activated T-cells, cytoplasmic 1 (NFATC1) OT4TMERS NFAC1_HUMAN Increases Expression [30]
Acyl-CoA 6-desaturase (FADS2) OTUX531P FADS2_HUMAN Decreases Expression [30]
Metalloproteinase inhibitor 1 (TIMP1) OTOXC51H TIMP1_HUMAN Increases Expression [30]
Cystatin-C (CST3) OTNZ6AO4 CYTC_HUMAN Increases Expression [30]
Cystatin-S (CST4) OTXXM8EH CYTS_HUMAN Increases Expression [30]
Interstitial collagenase (MMP1) OTI4I2V1 MMP1_HUMAN Increases Expression [30]
Integrin beta-1 (ITGB1) OT6G1IAR ITB1_HUMAN Decreases Expression [30]
Keratin, type II cytoskeletal 8 (KRT8) OTTM4X11 K2C8_HUMAN Increases Expression [30]
Neurofilament light polypeptide (NEFL) OTQESJV4 NFL_HUMAN Increases Expression [30]
Protein disulfide-isomerase (P4HB) OTTYNYPF PDIA1_HUMAN Increases Expression [30]
Decorin (DCN) OTWLJL7K PGS2_HUMAN Decreases Expression [30]
Profilin-1 (PFN1) OTHTGA1H PROF1_HUMAN Increases Expression [30]
Proto-oncogene tyrosine-protein kinase receptor Ret (RET) OTLU040A RET_HUMAN Decreases Expression [30]
Tropomyosin beta chain (TPM2) OTA1L0P8 TPM2_HUMAN Increases Expression [30]
Transcription factor Sp1 (SP1) OTISPT4X SP1_HUMAN Decreases Expression [30]
Keratin, type I cytoskeletal 19 (KRT19) OTDGDQ75 K1C19_HUMAN Increases Expression [30]
Insulin-like growth factor-binding protein 1 (IGFBP1) OT6UQV2K IBP1_HUMAN Increases Expression [30]
Small ribosomal subunit protein uS2 (RPSA) OTJZHEGT RSSA_HUMAN Decreases Expression [30]
Glycodelin (PAEP) OTQA0NV4 PAEP_HUMAN Decreases Expression [30]
E3 SUMO-protein ligase EGR2 (EGR2) OTAVQ78J EGR2_HUMAN Increases Expression [30]
Pregnancy-specific beta-1-glycoprotein 1 (PSG1) OT1U4ZZW PSG1_HUMAN Increases Expression [30]
Collagen alpha-3(VI) chain (COL6A3) OTAS6R6I CO6A3_HUMAN Decreases Expression [30]
Parathyroid hormone-related protein (PTHLH) OTI1JF13 PTHR_HUMAN Decreases Expression [30]
Plastin-3 (PLS3) OTYBM4PK PLST_HUMAN Decreases Expression [30]
Bifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase, mitochondrial (MTHFD2) OT1LQSGX MTDC_HUMAN Decreases Expression [30]
Pyruvate kinase PKM (PKM) OTLHHMC2 KPYM_HUMAN Increases Expression [30]
Carboxypeptidase E (CPE) OTXNTV79 CBPE_HUMAN Increases Expression [30]
High mobility group protein HMG-I/HMG-Y (HMGA1) OTQUSHPX HMGA1_HUMAN Increases Expression [30]
Gap junction alpha-1 protein (GJA1) OTT94MKL CXA1_HUMAN Decreases Expression [30]
Desmin (DES) OTI09KBW DESM_HUMAN Increases Expression [30]
Plasma membrane calcium-transporting ATPase 1 (ATP2B1) OT5MXG9W AT2B1_HUMAN Decreases Expression [30]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [30]
5'-nucleotidase (NT5E) OT7J5LT6 5NTD_HUMAN Increases Expression [30]
Fibroblast growth factor 7 (FGF7) OTGK6ANL FGF7_HUMAN Decreases Expression [30]
Insulin-like growth factor-binding protein 4 (IGFBP4) OT2HZRBD IBP4_HUMAN Increases Expression [30]
Transcription elongation factor A protein 1 (TCEA1) OTBFO594 TCEA1_HUMAN Decreases Expression [30]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Increases Expression [30]
Tenascin (TNC) OTK4FSHR TENA_HUMAN Decreases Expression [30]
V-type proton ATPase 16 kDa proteolipid subunit c (ATP6V0C) OTKPL09B VATL_HUMAN Increases Expression [30]
Protein ITPRID2 (ITPRID2) OTO3JDX5 ITPI2_HUMAN Increases Expression [30]
Dual specificity protein phosphatase 1 (DUSP1) OTN6BR75 DUS1_HUMAN Increases Expression [30]
Interleukin-12 subunit beta (IL12B) OT0JF8A3 IL12B_HUMAN Increases Expression [30]
Neurotensin/neuromedin N (NTS) OTPGDNQS NEUT_HUMAN Decreases Expression [30]
Guanylate-binding protein 2 (GBP2) OTVU4G07 GBP2_HUMAN Decreases Expression [30]
MHC class II transactivator (CIITA) OTRJNZFO C2TA_HUMAN Increases Expression [30]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [30]
Exosome RNA helicase MTR4 (MTREX) OTSQY30V MTREX_HUMAN Increases Expression [30]
Alpha-S1-casein (CSN1S1) OTXOW6XJ CASA1_HUMAN Increases Expression [30]
Nuclear receptor-interacting protein 1 (NRIP1) OTIZOJQV NRIP1_HUMAN Decreases Expression [30]
Homeobox protein Hox-A1 (HOXA1) OTMSOJ7D HXA1_HUMAN Increases Expression [30]
Ectonucleoside triphosphate diphosphohydrolase 1 (ENTPD1) OT6E2OW6 ENTP1_HUMAN Increases Expression [30]
Ephrin-A3 (EFNA3) OTJGOUMZ EFNA3_HUMAN Increases Expression [30]
GPI-linked NAD(P)(+)--arginine ADP-ribosyltransferase 1 (ART1) OT7FBG5W NAR1_HUMAN Increases Expression [30]
Branched-chain-amino-acid aminotransferase, cytosolic (BCAT1) OTYHXLWZ BCAT1_HUMAN Decreases Expression [30]
Microfibrillar-associated protein 2 (MFAP2) OTMHVBTV MFAP2_HUMAN Decreases Expression [30]
Laminin subunit beta-2 (LAMB2) OT71OI2Y LAMB2_HUMAN Increases Expression [30]
NHP2-like protein 1 (SNU13) OTH56TIH NH2L1_HUMAN Increases Expression [30]
Homeobox protein DLX-6 (DLX6) OT0FIJHY DLX6_HUMAN Increases Expression [30]
Neurotrypsin (PRSS12) OT1MYL3L NETR_HUMAN Decreases Expression [30]
Elongation factor 1-alpha 1 (EEF1A1) OT00THXS EF1A1_HUMAN Decreases Expression [30]
Microtubule-associated protein 1A (MAP1A) OTHO8K43 MAP1A_HUMAN Decreases Expression [30]
E3 ubiquitin-protein ligase Mdm2 (MDM2) OTOVXARF MDM2_HUMAN Increases Expression [30]
Cytochrome c oxidase subunit 6A2, mitochondrial (COX6A2) OTQR5SXD CX6A2_HUMAN Increases Expression [30]
cAMP-responsive element modulator (CREM) OTJIJ5AL CREM_HUMAN Decreases Expression [30]
Caldesmon (CALD1) OTNJKJ6Q CALD1_HUMAN Increases Expression [30]
ATP-dependent RNA helicase A (DHX9) OT5AAOQI DHX9_HUMAN Decreases Expression [30]
Serine/threonine-protein kinase PAK 1 (PAK1) OT17LZNZ PAK1_HUMAN Increases Expression [30]
Dual specificity mitogen-activated protein kinase kinase 5 (MAP2K5) OT6T408U MP2K5_HUMAN Decreases Expression [30]
Chitotriosidase-1 (CHIT1) OTPQR0A6 CHIT1_HUMAN Increases Expression [30]
Ras and Rab interactor 1 (RIN1) OTPBROUD RIN1_HUMAN Increases Expression [30]
Keratin, type I cuticular Ha2 (KRT32) OTZCGZYT K1H2_HUMAN Increases Expression [30]
Semaphorin-3A (SEMA3A) OTQJSV7W SEM3A_HUMAN Increases Expression [30]
Ras GTPase-activating protein 3 (RASA3) OT9C54MN RASA3_HUMAN Increases Expression [30]
Mediator of DNA damage checkpoint protein 1 (MDC1) OTEUQH4J MDC1_HUMAN Increases Expression [30]
Transmembrane glycoprotein NMB (GPNMB) OTB7KQKV GPNMB_HUMAN Decreases Expression [30]
Mortality factor 4-like protein 2 (MORF4L2) OT8OI3EC MO4L2_HUMAN Decreases Expression [30]
kinase isozyme 1, mitochondrial (PDK1) OTMABK9Z PDK1_HUMAN Increases Expression [30]
Serine/threonine-protein kinase 38 (STK38) OTKMYCYR STK38_HUMAN Decreases Expression [30]
Serine/threonine-protein phosphatase 2A activator (PTPA) OTRGFOI7 PTPA_HUMAN Increases Expression [30]
Reticulocalbin-1 (RCN1) OT3JBGAG RCN1_HUMAN Decreases Expression [30]
Olfactory receptor 8B8 (OR8B8) OTCISNYV OR8B8_HUMAN Increases Expression [30]
Leukotriene B4 receptor 1 (LTB4R) OT3SRH4H LT4R1_HUMAN Decreases Expression [30]
Serine/arginine-rich splicing factor 7 (SRSF7) OTRS4W4S SRSF7_HUMAN Decreases Expression [30]
Guanylate kinase (GUK1) OTLI0HRU KGUA_HUMAN Increases Expression [30]
Filamin A-interacting protein 1-like (FILIP1L) OTPY8IMS FIL1L_HUMAN Decreases Expression [30]
Nucleolar MIF4G domain-containing protein 1 (NOM1) OTWZSJJC NOM1_HUMAN Decreases Expression [30]
Opioid growth factor receptor-like protein 1 (OGFRL1) OT6QGBYE OGRL1_HUMAN Increases Expression [30]
Serine/threonine-protein kinase MRCK alpha (CDC42BPA) OTCPFOSA MRCKA_HUMAN Decreases Expression [30]
Extracellular sulfatase Sulf-1 (SULF1) OTJCNCO0 SULF1_HUMAN Decreases Expression [30]
N-acetyllactosaminide beta-1,6-N-acetylglucosaminyl-transferase (GCNT2) OTRUIMC4 GNT2A_HUMAN Decreases Expression [30]
Oxidation resistance protein 1 (OXR1) OTPIDMT3 OXR1_HUMAN Increases Expression [30]
Alpha-2,8-sialyltransferase 8B (ST8SIA2) OTRBBBD8 SIA8B_HUMAN Decreases Expression [30]
Type II iodothyronine deiodinase (DIO2) OTGPNSLH IOD2_HUMAN Decreases Expression [30]
G-patch domain and KOW motifs-containing protein (GPKOW) OTGS3H0M GPKOW_HUMAN Increases Expression [30]
Rho guanine nucleotide exchange factor 2 (ARHGEF2) OTBQTFRT ARHG2_HUMAN Decreases Expression [30]
Homogentisate 1,2-dioxygenase (HGD) OTTKLQOO HGD_HUMAN Increases Expression [30]
Secretory carrier-associated membrane protein 4 (SCAMP4) OTSCZTJ5 SCAM4_HUMAN Increases Expression [30]
Protein bicaudal D homolog 1 (BICD1) OT78IYPF BICD1_HUMAN Decreases Expression [30]
Ankyrin repeat and SOCS box protein 2 (ASB2) OTF9LV7L ASB2_HUMAN Increases Expression [30]
Eyes absent homolog 1 (EYA1) OTHU807A EYA1_HUMAN Decreases Expression [30]
Bcl-2-like protein 13 (BCL2L13) OT2VRFTM B2L13_HUMAN Increases Expression [30]
RNA helicase Mov10l1 (MOV10L1) OTP978LK M10L1_HUMAN Increases Expression [30]
Rac GTPase-activating protein 1 (RACGAP1) OTQE8IEH RGAP1_HUMAN Increases Expression [30]
Ras-related protein Rab-1B (RAB1B) OTAFCUAS RAB1B_HUMAN Increases Expression [30]
Semaphorin-6C (SEMA6C) OT1N59T5 SEM6C_HUMAN Increases Expression [30]
Sentrin-specific protease 3 (SENP3) OTFQDOMC SENP3_HUMAN Increases Expression [30]
Ribonuclease P protein subunit p21 (RPP21) OT53MDNE RPP21_HUMAN Increases Expression [30]
Protocadherin-18 (PCDH18) OTTLQWRN PCD18_HUMAN Decreases Expression [30]
Protein S100-A14 (S100A14) OTVFJJ91 S10AE_HUMAN Decreases Expression [30]
Tryptase gamma (TPSG1) OTDESHKT TRYG1_HUMAN Decreases Expression [30]
Rho GTPase-activating protein 35 (ARHGAP35) OTJ8POG0 RHG35_HUMAN Increases Expression [30]
Neuroligin-3 (NLGN3) OTKDEC1Q NLGN3_HUMAN Increases Expression [30]
Polycystin-2-like protein 1 (PKD2L1) OT1KJDAT PK2L1_HUMAN Increases Expression [30]
A disintegrin and metalloproteinase with thrombospondin motifs 1 (ADAMTS1) OTTLJH8W ATS1_HUMAN Decreases Expression [30]
Cytoplasmic phosphatidylinositol transfer protein 1 (PITPNC1) OT64TTGC PITC1_HUMAN Decreases Expression [30]
Transcription factor SOX-13 (SOX13) OTCIF6KC SOX13_HUMAN Decreases Expression [30]
Afadin- and alpha-actinin-binding protein (SSX2IP) OTEIZ7N1 ADIP_HUMAN Increases Expression [30]
Transmembrane emp24 domain-containing protein 3 (TMED3) OTNOPHHC TMED3_HUMAN Increases Expression [30]
Protocadherin beta-4 (PCDHB4) OTF665E0 PCDB4_HUMAN Decreases Expression [30]
Protocadherin beta-14 (PCDHB14) OTFZF1ST PCDBE_HUMAN Decreases Expression [30]
Adenylate kinase isoenzyme 5 (AK5) OTTGXLOT KAD5_HUMAN Increases Expression [30]
Albumin (ALB) OTVMM513 ALBU_HUMAN Increases Expression [38]
Alpha-fetoprotein (AFP) OT9GG3ZI FETA_HUMAN Increases Expression [38]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Expression [38]
Tyrosine aminotransferase (TAT) OT2CJ91O ATTY_HUMAN Increases Expression [38]
Hepatocyte nuclear factor 4-alpha (HNF4A) OTY1TOAB HNF4A_HUMAN Increases Expression [38]
CCAAT/enhancer-binding protein alpha (CEBPA) OTOM9OE4 CEBPA_HUMAN Increases Expression [38]
Hematopoietically-expressed homeobox protein HHEX (HHEX) OTLIUVYX HHEX_HUMAN Increases Expression [38]
Suppressor of cytokine signaling 3 (SOCS3) OTY183WJ SOCS3_HUMAN Affects Expression [36]
Telomerase reverse transcriptase (TERT) OT085VVA TERT_HUMAN Decreases Expression [39]
Aquaporin-9 (AQP9) OTLGH5ZY AQP9_HUMAN Increases Expression [40]
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-7 (GNG7) OTHS1L0E GBG7_HUMAN Affects Methylation [41]
Claudin-7 (CLDN7) OTNE0XHQ CLD7_HUMAN Decreases Expression [42]
Claudin-9 (CLDN9) OTCKI2IZ CLD9_HUMAN Increases Expression [43]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [39]
Calcitonin (CALCA) OTZ11LHB CALC_HUMAN Decreases Methylation [44]
Tumor necrosis factor (TNF) OT4IE164 TNFA_HUMAN Increases Response To Substance [45]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Increases Expression [46]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Affects Activity [47]
Interleukin-4 (IL4) OTOXBWAU IL4_HUMAN Affects Methylation [48]
Interleukin-6 (IL6) OTUOSCCU IL6_HUMAN Affects Methylation [48]
Tyrosine-protein kinase Fyn (FYN) OTLSLVZS FYN_HUMAN Increases Expression [49]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Increases Expression [50]
L-lactate dehydrogenase B chain (LDHB) OT9B1CT3 LDHB_HUMAN Increases Expression [51]
Thyroid peroxidase (TPO) OTJJLL20 PERT_HUMAN Increases Expression [52]
Prostate-specific antigen (KLK3) OTFGSBFJ KLK3_HUMAN Increases Expression [50]
Histone H1.0 (H1-0) OTRLJK4Z H10_HUMAN Increases Expression [53]
Interleukin-6 receptor subunit alpha (IL6R) OTCQL07Z IL6RA_HUMAN Affects Expression [36]
Gamma-enolase (ENO2) OTRODL0T ENOG_HUMAN Decreases Expression [54]
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Increases Expression [50]
Microtubule-associated protein tau (MAPT) OTMTP2Z7 TAU_HUMAN Decreases Expression [55]
Chromogranin-A (CHGA) OTXYX5JH CMGA_HUMAN Decreases Expression [54]
Cyclin-dependent kinase 4 (CDK4) OT7EP05T CDK4_HUMAN Decreases Expression [50]
Cadherin-1 (CDH1) OTFJMXPM CADH1_HUMAN Increases Expression [56]
G2/mitotic-specific cyclin-B1 (CCNB1) OT19S7E5 CCNB1_HUMAN Increases Expression [54]
15-hydroxyprostaglandin dehydrogenase (HPGD) OTYZI6JB PGDH_HUMAN Decreases Methylation [57]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [58]
Methylated-DNA--protein-cysteine methyltransferase (MGMT) OT40A9WH MGMT_HUMAN Increases Expression [59]
Thyrotropin receptor (TSHR) OT0BC8LB TSHR_HUMAN Increases Expression [52]
Hepatocyte nuclear factor 1-alpha (HNF1A) OT9DOUKL HNF1A_HUMAN Increases Expression [40]
Fibulin-1 (FBLN1) OT5MHHOP FBLN1_HUMAN Increases Expression [49]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [60]
Cyclin-dependent kinase 2 (CDK2) OTB5DYYZ CDK2_HUMAN Decreases Expression [50]
DNA cytosine-5)-methyltransferase 1 (DNMT1) OTM2DGTK DNMT1_HUMAN Decreases Expression [61]
G1/S-specific cyclin-D2 (CCND2) OTDULQF9 CCND2_HUMAN Affects Methylation [62]
Oxytocin receptor (OXTR) OT7WFW4U OXYR_HUMAN Decreases Expression [49]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Affects Expression [36]
Cyclin-dependent kinase inhibitor 2A (CDKN2A) OTN0ZWAE CDN2A_HUMAN Decreases Methylation [63]
Melanoma-associated antigen 1 (MAGEA1) OTXAO193 MAGA1_HUMAN Decreases Methylation [63]
Melanoma-associated antigen 3 (MAGEA3) OTW3Y5M4 MAGA3_HUMAN Increases Expression [64]
Killer cell immunoglobulin-like receptor 2DL1 (KIR2DL1) OTL1LBQJ KI2L1_HUMAN Increases Expression [65]
Killer cell immunoglobulin-like receptor 2DL2 (KIR2DL2) OTOVUTJD KI2L2_HUMAN Increases Expression [65]
Killer cell immunoglobulin-like receptor 2DL3 (KIR2DL3) OTFCN53B KI2L3_HUMAN Increases Expression [65]
Killer cell immunoglobulin-like receptor 3DL1 (KIR3DL1) OTPOSXFX KI3L1_HUMAN Increases Expression [65]
Killer cell immunoglobulin-like receptor 2DS4 (KIR2DS4) OT00N6UJ KI2S4_HUMAN Increases Expression [65]
Tumor necrosis factor ligand superfamily member 6 (FASLG) OTZARCHH TNFL6_HUMAN Increases Response To Substance [45]
Stromal cell-derived factor 1 (CXCL12) OT2QX5LL SDF1_HUMAN Increases Expression [66]
Tuberin (TSC2) OT47LWI9 TSC2_HUMAN Increases Expression [67]
Tumor necrosis factor ligand superfamily member 10 (TNFSF10) OT4PXBTA TNF10_HUMAN Increases Response To Substance [45]
High mobility group protein HMGI-C (HMGA2) OTBMBHHL HMGA2_HUMAN Increases Expression [49]
Homeobox protein Nkx-2.5 (NKX2-5) OTS1SAWM NKX25_HUMAN Increases Expression [68]
Death-associated protein kinase 1 (DAPK1) OTNCNUCO DAPK1_HUMAN Affects Methylation [69]
Claudin-6 (CLDN6) OTEN8ID2 CLD6_HUMAN Increases Expression [43]
Claudin-8 (CLDN8) OT7IIWXG CLD8_HUMAN Increases Expression [43]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [49]
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform (PPP2CA) OT83PT85 PP2AA_HUMAN Increases Expression [70]
Cyclin-A1 (CCNA1) OTX4HD45 CCNA1_HUMAN Decreases Expression [71]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Decreases Activity [72]
Transcription factor p65 (RELA) OTUJP9CN TF65_HUMAN Affects Localization [36]
Tight junction protein ZO-1 (TJP1) OTBDCUPK ZO1_HUMAN Increases Expression [43]
Dihydropyrimidine dehydrogenase (DPYD) OTWRF2NR DPYD_HUMAN Decreases Methylation [73]
BCL2/adenovirus E1B 19 kDa protein-interacting protein 3 (BNIP3) OT4SO7J4 BNIP3_HUMAN Increases Expression [74]
N-myc-interactor (NMI) OTYVG3NM NMI_HUMAN Increases Expression [49]
NAD(P) transhydrogenase, mitochondrial (NNT) OTAIOGZK NNTM_HUMAN Increases Expression [42]
Runt-related transcription factor 3 (RUNX3) OTITK1XD RUNX3_HUMAN Affects Methylation [75]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Increases Expression [76]
Cyclin-G2 (CCNG2) OTII38K2 CCNG2_HUMAN Decreases Expression [49]
Occludin (OCLN) OTSUTVWL OCLN_HUMAN Increases Expression [43]
kinase isozyme 4, mitochondrial (PDK4) OTCMHMBZ PDK4_HUMAN Decreases Methylation [77]
Dual specificity protein phosphatase 6 (DUSP6) OT4H6RKW DUS6_HUMAN Increases Expression [49]
Ribonucleoside-diphosphate reductase subunit M2 B (RRM2B) OTE8GBUR RIR2B_HUMAN Increases Expression [78]
Sodium/iodide cotransporter (SLC5A5) OTU7E9G7 SC5A5_HUMAN Increases Expression [26]
Krueppel-like factor 6 (KLF6) OTQY9S7F KLF6_HUMAN Increases Expression [49]
Killer cell immunoglobulin-like receptor 2DL4 (KIR2DL4) OTXN18OA KI2L4_HUMAN Increases Expression [65]
Protein Niban 1 (NIBAN1) OTYOLI12 NIBA1_HUMAN Increases Expression [49]
Calcium homeostasis modulator protein 2 (CALHM2) OTWWM6HI CAHM2_HUMAN Increases Expression [42]
Homeobox protein SIX2 (SIX2) OTYOVGSC SIX2_HUMAN Decreases Expression [42]
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase beta-1 (PLCB1) OT9HYT7A PLCB1_HUMAN Increases Expression [79]
Sal-like protein 4 (SALL4) OTC08PR5 SALL4_HUMAN Affects Methylation [32]
Transcription factor MafB (MAFB) OTH2N3T8 MAFB_HUMAN Increases Expression [42]
Sodium/nucleoside cotransporter 1 (SLC28A1) OTXWVV9O S28A1_HUMAN Increases Response To Substance [80]
------------------------------------------------------------------------------------
⏷ Show the Full List of 275 DOT(s)

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Lymphoid Malignancies DC7JHI1 N. A. Phase 1 [81]
Glioma DCNK7V3 SF-295 Investigative [82]
Plasma cell myeloma DCNIJZQ RPMI-8226 Investigative [82]
Carcinoma DCECOP7 RXF 393 Investigative [83]
Large cell lung carcinoma DC9DK6H NCI-H460 Investigative [1]
------------------------------------------------------------------------------------

References

1 Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7006).
3 Romidepsin FDA Label
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Azacitidine FDA Label
6 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6796).
7 Inhibition of transcription, expression, and secretion of the vascular epithelial growth factor in human epithelial endometriotic cells by romidepsin. Fertil Steril. 2011 Apr;95(5):1579-83. doi: 10.1016/j.fertnstert.2010.12.058. Epub 2011 Feb 4.
8 Inhibitors of class I HDACs and of FLT3 combine synergistically against leukemia cells with mutant FLT3. Arch Toxicol. 2022 Jan;96(1):177-193. doi: 10.1007/s00204-021-03174-1. Epub 2021 Oct 19.
9 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
10 Population pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphoma. Clin Cancer Res. 2009 Feb 15;15(4):1496-503.
11 A phase I/II trial of the histone deacetylase inhibitor romidepsin for adults with recurrent malignant glioma: North American Brain Tumor Consortium Study 03-03. Neuro Oncol. 2011 May;13(5):509-16.
12 Population pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphoma. Clin Cancer Res. 2009 Feb 15;15(4):1496-503.
13 FDA Label of Romidepsin. The 2020 official website of the U.S. Food and Drug Administration.
14 Chemoresistance to depsipeptide FK228 [(E)-(1S,4S,10S,21R)-7-[(Z)-ethylidene]-4,21-diisopropyl-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8,7,6]-tricos-16-ene-3,6,9,22-pentanone] is mediated by reversible MDR1 induction in human cancer cell lines. J Pharmacol Exp Ther. 2005 Jul;314(1):467-75. doi: 10.1124/jpet.105.083956. Epub 2005 Apr 15.
15 Aberrant promoter methylation of the ABCG2 gene in renal carcinoma. Mol Cell Biol. 2006 Nov;26(22):8572-85.
16 5-Aza-2'-deoxycytidine and depsipeptide synergistically induce expression of BIK (BCL2-interacting killer). Biochem Biophys Res Commun. 2006 Dec 15;351(2):455-61. doi: 10.1016/j.bbrc.2006.10.055. Epub 2006 Oct 18.
17 Bortezomib and depsipeptide sensitize tumors to tumor necrosis factor-related apoptosis-inducing ligand: a novel method to potentiate natural killer cell tumor cytotoxicity. Cancer Res. 2006 Jul 15;66(14):7317-25. doi: 10.1158/0008-5472.CAN-06-0680.
18 Histone deacetylase inhibitors FK228, N-(2-aminophenyl)-4-[N-(pyridin-3-yl-methoxycarbonyl)amino- methyl]benzamide and m-carboxycinnamic acid bis-hydroxamide augment radiation-induced cell death in gastrointestinal adenocarcinoma cells. Int J Cancer. 2004 Jun 10;110(2):301-8. doi: 10.1002/ijc.20117.
19 A sequential treatment of depsipeptide followed by 5-azacytidine enhances Gadd45beta expression in hepatocellular carcinoma cells. Anticancer Res. 2007 Nov-Dec;27(6B):3783-9.
20 Abrogation of p21 expression by flavopiridol enhances depsipeptide-mediated apoptosis in malignant pleural mesothelioma cells. Clin Cancer Res. 2004 Mar 1;10(5):1813-25. doi: 10.1158/1078-0432.ccr-0901-3.
21 Interactions between bortezomib and romidepsin and belinostat in chronic lymphocytic leukemia cells. Clin Cancer Res. 2008 Jan 15;14(2):549-58. doi: 10.1158/1078-0432.CCR-07-1934.
22 Blocking downstream signaling pathways in the context of HDAC inhibition promotes apoptosis preferentially in cells harboring mutant Ras. Oncotarget. 2016 Oct 25;7(43):69804-69815. doi: 10.18632/oncotarget.12001.
23 Up-regulation of MDR1 and induction of doxorubicin resistance by histone deacetylase inhibitor depsipeptide (FK228) and ATRA in acute promyelocytic leukemia cells. Blood. 2006 Feb 15;107(4):1546-54. doi: 10.1182/blood-2004-10-4126. Epub 2005 Oct 13.
24 Antitumor effects of histone deacetylase inhibitor on Ewing's family tumors. Int J Cancer. 2005 Sep 20;116(5):784-92. doi: 10.1002/ijc.21069.
25 Enhanced transgene expression in urothelial cancer gene therapy with histone deacetylase inhibitor. J Urol. 2005 Aug;174(2):747-52. doi: 10.1097/01.ju.0000164723.20555.e6.
26 Enhancement of sodium/iodide symporter expression in thyroid and breast cancer. Endocr Relat Cancer. 2006 Sep;13(3):797-826. doi: 10.1677/erc.1.01143.
27 Identification of cytochrome P450 enzymes involved in the metabolism of FK228, a potent histone deacetylase inhibitor, in human liver microsomes. Biol Pharm Bull. 2005 Jan;28(1):124-9.
28 Involvement of P-glycoprotein and MRP1 in resistance to cyclic tetrapeptide subfamily of histone deacetylase inhibitors in the drug-resistant osteosarcoma and Ewing's sarcoma cells. Int J Cancer. 2006 Jan 1;118(1):90-7. doi: 10.1002/ijc.21297.
29 The DNA methyltransferase inhibitors azacitidine, decitabine and zebularine exert differential effects on cancer gene expression in acute myeloid leukemia cells. Leukemia. 2009 Jun;23(6):1019-28.
30 The effect of DNA methylation inhibitor 5-Aza-2'-deoxycytidine on human endometrial stromal cells. Hum Reprod. 2010 Nov;25(11):2859-69.
31 Combination of DNA methylation inhibitor 5-azacytidine and arsenic trioxide has synergistic activity in myeloma. Eur J Haematol. 2009 Mar;82(3):176-83. doi: 10.1111/j.1600-0609.2008.01189.x. Epub 2008 Dec 5.
32 Novel approach for detecting global epigenetic alterations associated with tumor cell aneuploidy. Int J Cancer. 2007 Oct 1;121(7):1487-93. doi: 10.1002/ijc.22847.
33 The DNA methyltransferase inhibitors azacitidine, decitabine and zebularine exert differential effects on cancer gene expression in acute myeloid l... Leukemia. 2009 Jun;23(6):1019-28.
34 A pilot pharmacokinetic study of oral azacitidine. Leukemia. 2008 Sep;22(9):1680-4.
35 Mycoplasma hyorhinis-encoded cytidine deaminase efficiently inactivates cytosine-based anticancer drugs. FEBS Open Bio. 2015 Aug 3;5:634-9.
36 The effect of azacitidine on interleukin-6 signaling and nuclear factor-kappaB activation and its in vitro and in vivo activity against multiple myeloma. Haematologica. 2008 Jun;93(6):860-9. doi: 10.3324/haematol.12261. Epub 2008 Apr 28.
37 Effects of histone deacetylation and DNA methylation on the constitutive and TCDD-inducible expressions of the human CYP1 family in MCF-7 and HeLa cells. Toxicol Lett. 2003 Sep 30;144(2):247-56.
38 Self-assembled 3D spheroids and hollow-fibre bioreactors improve MSC-derived hepatocyte-like cell maturation in vitro. Arch Toxicol. 2017 Apr;91(4):1815-1832.
39 Alpha anomer of 5-aza-2'-deoxycytidine down-regulates hTERT mRNA expression in human leukemia HL-60 cells. Biochem Pharmacol. 2008 Feb 15;75(4):965-72. doi: 10.1016/j.bcp.2007.10.018. Epub 2007 Oct 22.
40 Azacytidine sensitizes acute myeloid leukemia cells to arsenic trioxide by up-regulating the arsenic transporter aquaglyceroporin 9. J Hematol Oncol. 2015 May 8;8:46. doi: 10.1186/s13045-015-0143-3.
41 Clinical significance of the reduced expression of G protein gamma 7 (GNG7) in oesophageal cancer. Br J Cancer. 2008 Jan 29;98(2):410-7. doi: 10.1038/sj.bjc.6604124. Epub 2008 Jan 22.
42 CRISPR-based DNA methylation editing of NNT rescues the cisplatin resistance of lung cancer cells by reducing autophagy. Arch Toxicol. 2023 Feb;97(2):441-456. doi: 10.1007/s00204-022-03404-0. Epub 2022 Nov 6.
43 Prevention of murine experimental corneal trauma by epigenetic events regulating claudin 6 and claudin 9. Jpn J Ophthalmol. 2008 May-Jun;52(3):195-203. doi: 10.1007/s10384-008-0524-z. Epub 2008 Jul 27.
44 Intriguing response to azacitidine in a patient with juvenile myelomonocytic leukemia and monosomy 7. Blood. 2009 Mar 19;113(12):2867-8. doi: 10.1182/blood-2008-12-195693.
45 Sensitization by 5-azacytidine toward death receptor-induced hepatic apoptosis. J Pharmacol Exp Ther. 2009 Jan;328(1):107-15. doi: 10.1124/jpet.108.143560. Epub 2008 Sep 30.
46 Arsenic induces functional re-expression of estrogen receptor by demethylation of DNA in estrogen receptor-negative human breast cancer. PLoS One. 2012;7(4):e35957. doi: 10.1371/journal.pone.0035957. Epub 2012 Apr 27.
47 Identification of environmental chemicals that activate p53 signaling after in vitro metabolic activation. Arch Toxicol. 2022 Jul;96(7):1975-1987. doi: 10.1007/s00204-022-03291-5. Epub 2022 Apr 18.
48 Hypomethylation of interleukin-4 and -6 promoters in T cells from systemic lupus erythematosus patients. Acta Pharmacol Sin. 2008 Jan;29(1):105-12. doi: 10.1111/j.1745-7254.2008.00739.x.
49 Differential regulation of the p73 cistrome by mammalian target of rapamycin reveals transcriptional programs of mesenchymal differentiation and tumorigenesis. Proc Natl Acad Sci U S A. 2011 Feb 1;108(5):2076-81. doi: 10.1073/pnas.1011936108. Epub 2011 Jan 18.
50 Chronic azacitidine treatment results in differentiating effects, sensitizes against bicalutamide in androgen-independent prostate cancer cells. Prostate. 2008 May 15;68(7):793-801. doi: 10.1002/pros.20748.
51 Lactate dehydrogenase-B is silenced by promoter methylation in a high frequency of human breast cancers. PLoS One. 2013;8(2):e57697. doi: 10.1371/journal.pone.0057697. Epub 2013 Feb 21.
52 The comparative effects of gene modulators on thyroid-specific genes and radioiodine uptake. Cancer Biother Radiopharm. 2007 Jun;22(3):443-9. doi: 10.1089/cbr.2006.319.A.
53 Characterisation of human histone H1x. Biol Chem. 2005 Jun;386(6):541-51. doi: 10.1515/BC.2005.064.
54 Azacytidine induces cell cycle arrest and suppression of neuroendocrine markers in carcinoids. Int J Clin Exp Med. 2010 Mar 28;3(2):95-102.
55 Pharmacologic reductions of total tau levels; implications for the role of microtubule dynamics in regulating tau expression. Mol Neurodegener. 2006 Jul 26;1:6. doi: 10.1186/1750-1326-1-6.
56 Promoter methylation as a common mechanism for inactivating E-cadherin in human salivary gland adenoid cystic carcinoma. Cancer. 2007 Jul 1;110(1):87-95. doi: 10.1002/cncr.22758.
57 15-hydroxyprostaglandin dehydrogenase is down-regulated in gastric cancer. Clin Cancer Res. 2009 Jul 15;15(14):4572-80. doi: 10.1158/1078-0432.CCR-08-2518. Epub 2009 Jul 7.
58 DNA methylation inhibitor 5-Aza-2'-deoxycytidine induces reversible genome-wide DNA damage that is distinctly influenced by DNA methyltransferases 1 and 3B. Mol Cell Biol. 2008 Jan;28(2):752-71. doi: 10.1128/MCB.01799-07. Epub 2007 Nov 8.
59 CpG methylation-dependent repression of the human O6-methylguanine-DNA methyltransferase gene linked to chromatin structure alteration. Carcinogenesis. 2003 Aug;24(8):1337-45. doi: 10.1093/carcin/bgg086. Epub 2003 May 22.
60 Methylation-mediated repression of GADD45alpha in prostate cancer and its role as a potential therapeutic target. Cancer Res. 2009 Feb 15;69(4):1527-35. doi: 10.1158/0008-5472.CAN-08-3609. Epub 2009 Feb 3.
61 The antitumor effects of arsenic trioxide in mantle cell lymphoma via targeting Wnt/?catenin pathway and DNA methyltransferase-1. Oncol Rep. 2017 Nov;38(5):3114-3120. doi: 10.3892/or.2017.5945. Epub 2017 Sep 7.
62 Hypermethylation of Cyclin D2 is associated with loss of mRNA expression and tumor development in prostate cancer. J Mol Med (Berl). 2006 Nov;84(11):911-8. doi: 10.1007/s00109-006-0099-4. Epub 2006 Sep 22.
63 Hydroxycarbamide in combination with azacitidine or decitabine is antagonistic on DNA methylation inhibition. Br J Haematol. 2007 Sep;138(5):616-23. doi: 10.1111/j.1365-2141.2007.06707.x.
64 Epigenetic modulation of MAGE-A3 antigen expression in multiple myeloma following treatment with the demethylation agent 5-azacitidine and the histone deacetlyase inhibitor MGCD0103. Cytotherapy. 2011 May;13(5):618-28. doi: 10.3109/14653249.2010.529893. Epub 2010 Dec 20.
65 DNA methylation inhibition increases T cell KIR expression through effects on both promoter methylation and transcription factors. Clin Immunol. 2009 Feb;130(2):213-24. doi: 10.1016/j.clim.2008.08.009. Epub 2008 Oct 22.
66 Tamoxifen epigenetically modulates CXCL12 expression in MCF-7 breast cancer cells. Biomed Pharmacother. 2010 Jan;64(1):54-7. doi: 10.1016/j.biopha.2009.04.041. Epub 2009 Sep 2.
67 Aberrant expression of TSC2 gene in the newly diagnosed acute leukemia. Leuk Res. 2009 Jul;33(7):891-7. doi: 10.1016/j.leukres.2009.01.041. Epub 2009 Feb 27.
68 5-Azacytidine-treated human mesenchymal stem/progenitor cells derived from umbilical cord, cord blood and bone marrow do not generate cardiomyocytes in vitro at high frequencies. Vox Sang. 2008 Aug;95(2):137-48. doi: 10.1111/j.1423-0410.2008.01076.x. Epub 2008 Jun 28.
69 Epigenetic dysregulation of the death-associated protein kinase/p14/HDM2/p53/Apaf-1 apoptosis pathway in multiple myeloma. J Clin Pathol. 2007 Jun;60(6):664-9. doi: 10.1136/jcp.2006.038331.
70 Methylation status of CpG islands flanking a cAMP response element motif on the protein phosphatase 2Ac alpha promoter determines CREB binding and activity. J Immunol. 2009 Feb 1;182(3):1500-8. doi: 10.4049/jimmunol.182.3.1500.
71 Homocysteine inhibits endothelial cell growth via DNA hypomethylation of the cyclin A gene. Blood. 2007 Nov 15;110(10):3648-55. doi: 10.1182/blood-2007-06-096701. Epub 2007 Aug 13.
72 A Gene Expression Biomarker Predicts Heat Shock Factor 1 Activation in a Gene Expression Compendium. Chem Res Toxicol. 2021 Jul 19;34(7):1721-1737. doi: 10.1021/acs.chemrestox.0c00510. Epub 2021 Jun 25.
73 Aberrant methylation of DPYD promoter, DPYD expression, and cellular sensitivity to 5-fluorouracil in cancer cells. Clin Cancer Res. 2004 Oct 15;10(20):7100-7. doi: 10.1158/1078-0432.CCR-04-0337.
74 Synergism of arsenic trioxide and MG132 in Raji cells attained by targeting BNIP3, autophagy, and mitochondria with low doses of valproic acid and vincristine. Eur J Cancer. 2014 Dec;50(18):3243-61. doi: 10.1016/j.ejca.2014.09.012. Epub 2014 Oct 13.
75 Promoter hypermethylation of the RUNX3 gene in esophageal squamous cell carcinoma. Cancer Invest. 2007 Dec;25(8):685-90. doi: 10.1080/07357900701561131.
76 [5-azacytidine enhances anti-tumor efficacy of doxorubicin to neuroblastoma cell lines]. Zhongguo Dang Dai Er Ke Za Zhi. 2007 Dec;9(6):577-9.
77 Pyruvate Dehydrogenase Kinase 4 Deficiency Results in Expedited Cellular Proliferation through E2F1-Mediated Increase of Cyclins. Mol Pharmacol. 2017 Mar;91(3):189-196. doi: 10.1124/mol.116.106757. Epub 2016 Dec 21.
78 p53-inducible ribonucleotide reductase (p53R2/RRM2B) is a DNA hypomethylation-independent decitabine gene target that correlates with clinical response in myelodysplastic syndrome/acute myelogenous leukemia. Cancer Res. 2008 Nov 15;68(22):9358-66. doi: 10.1158/0008-5472.CAN-08-1860.
79 Reduction of phosphoinositide-phospholipase C beta1 methylation predicts the responsiveness to azacitidine in high-risk MDS. Proc Natl Acad Sci U S A. 2009 Sep 29;106(39):16811-6. doi: 10.1073/pnas.0907109106. Epub 2009 Sep 10.
80 Human concentrative nucleoside transporter 1-mediated uptake of 5-azacytidine enhances DNA demethylation. Mol Cancer Ther. 2009 Jan;8(1):225-31. doi: 10.1158/1535-7163.MCT-08-0743.
81 ClinicalTrials.gov (NCT01998035) Romidepsin Plus Oral 5-Azacitidine in Relapsed/Refractory Lymphoid Malignancies
82 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
83 Biologically active neutrophil chemokine pattern in tonsillitis.Clin Exp Immunol. 2004 Mar;135(3):511-8. doi: 10.1111/j.1365-2249.2003.02390.x.